868540-17-4,MFCD11040997
Catalog No.:AA0039HG

868540-17-4 | (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide

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Purity
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5mg
≥98%
in stock  
$46.00   $32.00
- +
10mg
≥98%
in stock  
$69.00   $48.00
- +
25mg
≥98%
in stock  
$112.00   $78.00
- +
50mg
≥98%
in stock  
$156.00   $109.00
- +
250mg
95%
in stock  
$502.00   $352.00
- +
1g
95%
in stock  
$1,258.00   $880.00
- +
  • Technical Information
  • Properties
  • Literature
  • Request for Quotation
  • Download SDS
Technical Information
Catalog Number:
AA0039HG
Chemical Name:
(αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
CAS Number:
868540-17-4
Molecular Formula:
C40H57N5O7
Molecular Weight:
719.9099
MDL Number:
MFCD11040997
SMILES:
CC(C[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)[C@@]1(C)CO1)CC(C)C)Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN1CCOCC1)CCc1ccccc1)C
Properties
Computed Properties
 
Complexity:
1180  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
5  
Defined Bond Stereocenter Count:
0  
Formal Charge:
0  
Heavy Atom Count:
52  
Hydrogen Bond Acceptor Count:
8  
Hydrogen Bond Donor Count:
4  
Isotope Atom Count:
0  
Rotatable Bond Count:
20  
Undefined Atom Stereocenter Count:
0  
Undefined Bond Stereocenter Count:
0  
XLogP3:
4.7  

Literature

Title: Therapeutic potential of carfilzomib, an irreversible proteasome inhibitor, against acetaminophen-induced hepatotoxicity in mice.

Journal: Journal of biochemical and molecular toxicology 20170401

Title: Nephrotoxicity of epigenetic inhibitors used for the treatment of cancer.

Journal: Chemico-biological interactions 20161025

Title: Inhibition of chymotryptic-like standard proteasome activity exacerbates doxorubicin-induced cytotoxicity in primary cardiomyocytes.

Journal: Toxicology 20160415

Title: Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

Journal: Chemistry & biology 20150618

Title: Suppression of BRCA1 sensitizes cells to proteasome inhibitors.

Journal: Cell death & disease 20141201

Title: Possible role of selective, irreversible, proteasome inhibitor (carfilzomib) in the treatment of rat hepatocellular carcinoma.

Journal: Chemico-biological interactions 20140525

Title: Parathyroid hormone receptor mediates the anti-myeloma effect of proteasome inhibitors.

Journal: Bone 20140401

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: Carfilzomib.

Journal: Blood 20130207

Title: Molecular mechanisms of acquired proteasome inhibitor resistance.

Journal: Journal of medicinal chemistry 20121213

Title: Carfilzomib: in relapsed, or relapsed and refractory, multiple myeloma.

Journal: Drugs 20121022

Title: Carfilzomib and ONX 0912 inhibit cell survival and tumor growth of head and neck cancer and their activities are enhanced by suppression of Mcl-1 or autophagy.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20121015

Title: A phase 2 study of single-agent carfilzomib (PX-171-003-A1) in patients with relapsed and refractory multiple myeloma.

Journal: Blood 20121004

Title: Carfilzomib in multiple myeloma: gold, silver, or bronze?

Journal: Blood 20121004

Title: An open-label single-arm pilot phase II study (PX-171-003-A0) of low-dose, single-agent carfilzomib in patients with relapsed and refractory multiple myeloma.

Journal: Clinical lymphoma, myeloma & leukemia 20121001

Title: A phase I single-agent study of twice-weekly consecutive-day dosing of the proteasome inhibitor carfilzomib in patients with relapsed or refractory multiple myeloma or lymphoma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120901

Title: An open-label, single-arm, phase 2 study of single-agent carfilzomib in patients with relapsed and/or refractory multiple myeloma who have been previously treated with bortezomib.

Journal: British journal of haematology 20120901

Title: Emerging biological insights and novel treatment strategies in multiple myeloma.

Journal: Expert opinion on emerging drugs 20120901

Title: Evolving chemotherapy options for the treatment of myeloma kidney: a 40-year perspective.

Journal: Advances in chronic kidney disease 20120901

Title: Carfilzomib in multiple myeloma.

Journal: Clinical advances in hematology & oncology : H&O 20120901

Title: A phase 1/2 study of carfilzomib in combination with lenalidomide and low-dose dexamethasone as a frontline treatment for multiple myeloma.

Journal: Blood 20120830

Title: Proteasome inhibitors in multiple myeloma: 10 years later.

Journal: Blood 20120802

Title: Novel agents derived from the currently approved treatments for MM: novel proteasome inhibitors and novel IMIDs.

Journal: Expert opinion on investigational drugs 20120801

Title: Role of carfilzomib in the treatment of multiple myeloma.

Journal: Expert review of hematology 20120801

Title: The immunoproteasome as a target in hematologic malignancies.

Journal: Seminars in hematology 20120701

Title: The future of therapy for relapsed/refractory multiple myeloma: emerging agents and novel treatment strategies.

Journal: Seminars in hematology 20120701

Title: An open-label, single-arm, phase 2 (PX-171-004) study of single-agent carfilzomib in bortezomib-naive patients with relapsed and/or refractory multiple myeloma.

Journal: Blood 20120614

Title: Proteasome inhibitors in mantle cell lymphoma.

Journal: Best practice & research. Clinical haematology 20120601

Title: Obatoclax interacts synergistically with the irreversible proteasome inhibitor carfilzomib in GC- and ABC-DLBCL cells in vitro and in vivo.

Journal: Molecular cancer therapeutics 20120501

Title: Proteasome inhibition and combination therapy for non-Hodgkin's lymphoma: from bench to bedside.

Journal: The oncologist 20120501

Title: Inactivating PSMB5 mutations and P-glycoprotein (multidrug resistance-associated protein/ATP-binding cassette B1) mediate resistance to proteasome inhibitors: ex vivo efficacy of (immuno)proteasome inhibitors in mononuclear blood cells from patients with rheumatoid arthritis.

Journal: The Journal of pharmacology and experimental therapeutics 20120401

Title: Novel therapeutics in multiple myeloma.

Journal: Hematology (Amsterdam, Netherlands) 20120401

Title: Novel therapies in monoclonal gammopathies.

Journal: Hematology (Amsterdam, Netherlands) 20120401

Title: Targeted therapy of multiple myeloma.

Journal: Hematology (Amsterdam, Netherlands) 20120401

Title: Beneficial effect of novel proteasome inhibitors in murine lupus via dual inhibition of type I interferon and autoantibody-secreting cells.

Journal: Arthritis and rheumatism 20120201

Title: The 39th David A. Karnofsky Lecture: bench-to-bedside translation of targeted therapies in multiple myeloma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120201

Title: Next-generation proteasome blockers promise safer cancer therapy.

Journal: Nature medicine 20120106

Title: Ovarian cancer: opportunity for targeted therapy.

Journal: Journal of oncology 20120101

Title: Analysing properties of proteasome inhibitors using kinetic and X-ray crystallographic studies.

Journal: Methods in molecular biology (Clifton, N.J.) 20120101

Title: Blocking autophagy prevents bortezomib-induced NF-κB activation by reducing I-κBα degradation in lymphoma cells.

Journal: PloS one 20120101

Title: Novel therapies for aggressive B-cell lymphoma.

Journal: Advances in hematology 20120101

Title: On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53.

Journal: PloS one 20120101

Title: Lenalidomide before and after Autologous Hematopoietic Stem Cell Transplantation in Multiple Myeloma.

Journal: Advances in hematology 20120101

Title: Carfilzomib: a novel treatment in relapsed and refractory multiple myeloma.

Journal: OncoTargets and therapy 20120101

Title: Drugs: More shots on target.

Journal: Nature 20111214

Title: Advances in the understanding of mechanisms and therapeutic use of bortezomib.

Journal: Discovery medicine 20111201

Title: Pharmacokinetics, pharmacodynamics, metabolism, distribution, and excretion of carfilzomib in rats.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20111001

Title: Pharmacogenomics of bortezomib test-dosing identifies hyperexpression of proteasome genes, especially PSMD4, as novel high-risk feature in myeloma treated with Total Therapy 3.

Journal: Blood 20110929

Title: Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo.

Journal: Molecular cancer therapeutics 20110901

Title: [Development of novel agents for multiple myeloma; now and the future].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20110801

Title: Novel proteasome inhibitors to overcome bortezomib resistance.

Journal: Journal of the National Cancer Institute 20110706

Title: A genetic interaction network of five genes for human polycystic kidney and liver diseases defines polycystin-1 as the central determinant of cyst formation.

Journal: Nature genetics 20110619

Title: How to treat patients with relapsed/refractory multiple myeloma: evidence-based information and opinions.

Journal: Expert opinion on investigational drugs 20110601

Title: Alkaline phosphatase variation during carfilzomib treatment is associated with best response in multiple myeloma patients.

Journal: European journal of haematology 20110601

Title: Specific cell-permeable inhibitor of proteasome trypsin-like sites selectively sensitizes myeloma cells to bortezomib and carfilzomib.

Journal: Chemistry & biology 20110527

Title: Nonproteasomal targets of the proteasome inhibitors bortezomib and carfilzomib: a link to clinical adverse events.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110501

Title: Carfilzomib: a novel second-generation proteasome inhibitor.

Journal: Future oncology (London, England) 20110501

Title: RNAi screen of the druggable genome identifies modulators of proteasome inhibitor sensitivity in myeloma including CDK5.

Journal: Blood 20110407

Title: Recent advances in myeloma treatment.

Journal: Transfusion and apheresis science : official journal of the World Apheresis Association : official journal of the European Society for Haemapheresis 20110401

Title: Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110401

Title: Second generation proteasome inhibitors: carfilzomib and immunoproteasome-specific inhibitors (IPSIs).

Journal: Current cancer drug targets 20110301

Title: Unfolded protein response in cancer: the physician's perspective.

Journal: Journal of hematology & oncology 20110101

Title: Histone deacetylase turnover and recovery in sulforaphane-treated colon cancer cells: competing actions of 14-3-3 and Pin1 in HDAC3/SMRT corepressor complex dissociation/reassembly.

Journal: Molecular cancer 20110101

Title: Emerging role of carfilzomib in treatment of relapsed and refractory lymphoid neoplasms and multiple myeloma.

Journal: Core evidence 20110101

Title: Therapeutic strategies to enhance the anticancer efficacy of histone deacetylase inhibitors.

Journal: Journal of biomedicine & biotechnology 20110101

Title: Light chain (AL) amyloidosis: update on diagnosis and management.

Journal: Journal of hematology & oncology 20110101

Title: Molecular mechanisms of bortezomib resistant adenocarcinoma cells.

Journal: PloS one 20110101

Title: Targeting histone deacetyalses in the treatment of B- and T-cell malignancies.

Journal: Investigational new drugs 20101201

Title: New twists on proteasome inhibitors.

Journal: Nature biotechnology 20101201

Title: Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.

Journal: The Biochemical journal 20100915

Title: Novel disease targets and management approaches for diffuse large B-cell lymphoma.

Journal: Leukemia & lymphoma 20100801

Title: Peripheral neuropathy during bortezomib treatment of multiple myeloma: a review of recent studies.

Journal: Leukemia & lymphoma 20100701

Title: The pan-HDAC inhibitor vorinostat potentiates the activity of the proteasome inhibitor carfilzomib in human DLBCL cells in vitro and in vivo.

Journal: Blood 20100603

Title: Activation of mutant enzyme function in vivo by proteasome inhibitors and treatments that induce Hsp70.

Journal: PLoS genetics 20100101

Title: Bortezomib.

Journal: Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer 20100101

Title: Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry.

Journal: Current topics in medicinal chemistry 20100101

Title: State-of-the-Art Management of Complications of Myeloma and Its Treatment.

Journal: Advances in hematology 20100101

Title: Proteasome inhibition and its therapeutic potential in multiple myeloma.

Journal: Biologics : targets & therapy 20100101

Title: Relapsed multiple myeloma.

Journal: Hematology. American Society of Hematology. Education Program 20100101

Title: Ubiquitin Drug Discovery & Diagnostics 2009 - First Annual Conference.

Journal: IDrugs : the investigational drugs journal 20091201

Title: A phase 1 dose escalation study of the safety and pharmacokinetics of the novel proteasome inhibitor carfilzomib (PR-171) in patients with hematologic malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20091115

Title: Acquisition of a multidrug-resistant phenotype with a proteasome inhibitor in multiple myeloma.

Journal: Leukemia 20091101

Title: Proteasome inhibitors in the treatment of multiple myeloma.

Journal: Leukemia 20091101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20091101

Title: Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome.

Journal: Blood 20091015

Title: Clinical development of novel proteasome inhibitors for cancer treatment.

Journal: Expert opinion on investigational drugs 20090701

Title: Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).

Journal: Journal of medicinal chemistry 20090514

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20090401

Title: Antiproliferative and proapoptotic effects of proteasome inhibitors and their combination with histone deacetylase inhibitors on leukemia cells.

Journal: Cardiovascular & hematological disorders drug targets 20090301

Title: New drugs in multiple myeloma and the significance of autologous stem cell transplants.

Journal: Clinical advances in hematology & oncology : H&O 20090301

Title: Novel therapies for relapsed myeloma.

Journal: Hematology. American Society of Hematology. Education Program 20090101

Title: Future novel single agent and combination therapies.

Journal: Cancer journal (Sudbury, Mass.) 20090101

Title: Discovery of novel proteasome inhibitors using a high-content cell-based screening system.

Journal: PloS one 20090101

Title: The development and pharmacology of proteasome inhibitors for the management and treatment of cancer.

Journal: Advances in pharmacology (San Diego, Calif.) 20090101

Title: Lenalidomide in multiple myeloma: an evidence-based review of its role in therapy.

Journal: Core evidence 20090101

Title: The BH3-only mimetic ABT-737 synergizes the antineoplastic activity of proteasome inhibitors in lymphoid malignancies.

Journal: Blood 20081001

Title: Practical considerations for multiple myeloma: an overview of recent data and current options.

Journal: Clinical lymphoma & myeloma 20080801

Title: Targeting Bcl-2 family members with the BH3 mimetic AT-101 markedly enhances the therapeutic effects of chemotherapeutic agents in in vitro and in vivo models of B-cell lymphoma.

Journal: Blood 20080601

Title: The potential of proteasome inhibitors in cancer therapy.

Journal: Expert opinion on investigational drugs 20080601

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20080301

Title: Mechanisms of proteasome inhibitor action and resistance in cancer.

Journal: Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy 20080101

Title: Targeting the UPS as therapy in multiple myeloma.

Journal: BMC biochemistry 20080101

Title: Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma.

Journal: Blood 20071101

Title: Epoxomicin, a new antitumor agent of microbial origin.

Journal: The Journal of antibiotics 19921101

Title: Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90.

Title: Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2011 Sep;10(9):1686-97.

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Tags:868540-17-4 Molecular Formula|868540-17-4 MDL|868540-17-4 SMILES|868540-17-4 (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
Catalog No.: AA0039HG
868540-17-4,MFCD11040997
868540-17-4 | (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
Pack Size: 5mg
Purity: ≥98%
in stock
$46.00 $32.00
Pack Size: 10mg
Purity: ≥98%
in stock
$69.00 $48.00
Pack Size: 25mg
Purity: ≥98%
in stock
$112.00 $78.00
Pack Size: 50mg
Purity: ≥98%
in stock
$156.00 $109.00
Pack Size: 250mg
Purity: 95%
in stock
$502.00 $352.00
Pack Size: 1g
Purity: 95%
in stock
$1,258.00 $880.00
Quantity
- +
Add to Card
Order Now
bulk Quotation Request
Technical Information
Catalog Number: AA0039HG
Chemical Name: (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
CAS Number: 868540-17-4
Molecular Formula: C40H57N5O7
Molecular Weight: 719.9099
MDL Number: MFCD11040997
SMILES: CC(C[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)[C@@]1(C)CO1)CC(C)C)Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN1CCOCC1)CCc1ccccc1)C
Properties
Complexity: 1180  
Covalently-Bonded Unit Count: 1  
Defined Atom Stereocenter Count: 5  
Defined Bond Stereocenter Count: 0  
Formal Charge: 0  
Heavy Atom Count: 52  
Hydrogen Bond Acceptor Count: 8  
Hydrogen Bond Donor Count: 4  
Isotope Atom Count: 0  
Rotatable Bond Count: 20  
Undefined Atom Stereocenter Count: 0  
Undefined Bond Stereocenter Count: 0  
XLogP3: 4.7  
Literature fold

Title: Therapeutic potential of carfilzomib, an irreversible proteasome inhibitor, against acetaminophen-induced hepatotoxicity in mice.

Journal: Journal of biochemical and molecular toxicology20170401

Title: Nephrotoxicity of epigenetic inhibitors used for the treatment of cancer.

Journal: Chemico-biological interactions20161025

Title: Inhibition of chymotryptic-like standard proteasome activity exacerbates doxorubicin-induced cytotoxicity in primary cardiomyocytes.

Journal: Toxicology20160415

Title: Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

Journal: Chemistry & biology20150618

Title: Suppression of BRCA1 sensitizes cells to proteasome inhibitors.

Journal: Cell death & disease20141201

Title: Possible role of selective, irreversible, proteasome inhibitor (carfilzomib) in the treatment of rat hepatocellular carcinoma.

Journal: Chemico-biological interactions20140525

Title: Parathyroid hormone receptor mediates the anti-myeloma effect of proteasome inhibitors.

Journal: Bone20140401

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters20130801

Title: Carfilzomib.

Journal: Blood20130207

Title: Molecular mechanisms of acquired proteasome inhibitor resistance.

Journal: Journal of medicinal chemistry20121213

Title: Carfilzomib: in relapsed, or relapsed and refractory, multiple myeloma.

Journal: Drugs20121022

Title: Carfilzomib and ONX 0912 inhibit cell survival and tumor growth of head and neck cancer and their activities are enhanced by suppression of Mcl-1 or autophagy.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20121015

Title: A phase 2 study of single-agent carfilzomib (PX-171-003-A1) in patients with relapsed and refractory multiple myeloma.

Journal: Blood20121004

Title: Carfilzomib in multiple myeloma: gold, silver, or bronze?

Journal: Blood20121004

Title: An open-label single-arm pilot phase II study (PX-171-003-A0) of low-dose, single-agent carfilzomib in patients with relapsed and refractory multiple myeloma.

Journal: Clinical lymphoma, myeloma & leukemia20121001

Title: A phase I single-agent study of twice-weekly consecutive-day dosing of the proteasome inhibitor carfilzomib in patients with relapsed or refractory multiple myeloma or lymphoma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20120901

Title: An open-label, single-arm, phase 2 study of single-agent carfilzomib in patients with relapsed and/or refractory multiple myeloma who have been previously treated with bortezomib.

Journal: British journal of haematology20120901

Title: Emerging biological insights and novel treatment strategies in multiple myeloma.

Journal: Expert opinion on emerging drugs20120901

Title: Evolving chemotherapy options for the treatment of myeloma kidney: a 40-year perspective.

Journal: Advances in chronic kidney disease20120901

Title: Carfilzomib in multiple myeloma.

Journal: Clinical advances in hematology & oncology : H&O20120901

Title: A phase 1/2 study of carfilzomib in combination with lenalidomide and low-dose dexamethasone as a frontline treatment for multiple myeloma.

Journal: Blood20120830

Title: Proteasome inhibitors in multiple myeloma: 10 years later.

Journal: Blood20120802

Title: Novel agents derived from the currently approved treatments for MM: novel proteasome inhibitors and novel IMIDs.

Journal: Expert opinion on investigational drugs20120801

Title: Role of carfilzomib in the treatment of multiple myeloma.

Journal: Expert review of hematology20120801

Title: The immunoproteasome as a target in hematologic malignancies.

Journal: Seminars in hematology20120701

Title: The future of therapy for relapsed/refractory multiple myeloma: emerging agents and novel treatment strategies.

Journal: Seminars in hematology20120701

Title: An open-label, single-arm, phase 2 (PX-171-004) study of single-agent carfilzomib in bortezomib-naive patients with relapsed and/or refractory multiple myeloma.

Journal: Blood20120614

Title: Proteasome inhibitors in mantle cell lymphoma.

Journal: Best practice & research. Clinical haematology20120601

Title: Obatoclax interacts synergistically with the irreversible proteasome inhibitor carfilzomib in GC- and ABC-DLBCL cells in vitro and in vivo.

Journal: Molecular cancer therapeutics20120501

Title: Proteasome inhibition and combination therapy for non-Hodgkin's lymphoma: from bench to bedside.

Journal: The oncologist20120501

Title: Inactivating PSMB5 mutations and P-glycoprotein (multidrug resistance-associated protein/ATP-binding cassette B1) mediate resistance to proteasome inhibitors: ex vivo efficacy of (immuno)proteasome inhibitors in mononuclear blood cells from patients with rheumatoid arthritis.

Journal: The Journal of pharmacology and experimental therapeutics20120401

Title: Novel therapeutics in multiple myeloma.

Journal: Hematology (Amsterdam, Netherlands)20120401

Title: Novel therapies in monoclonal gammopathies.

Journal: Hematology (Amsterdam, Netherlands)20120401

Title: Targeted therapy of multiple myeloma.

Journal: Hematology (Amsterdam, Netherlands)20120401

Title: Beneficial effect of novel proteasome inhibitors in murine lupus via dual inhibition of type I interferon and autoantibody-secreting cells.

Journal: Arthritis and rheumatism20120201

Title: The 39th David A. Karnofsky Lecture: bench-to-bedside translation of targeted therapies in multiple myeloma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology20120201

Title: Next-generation proteasome blockers promise safer cancer therapy.

Journal: Nature medicine20120106

Title: Ovarian cancer: opportunity for targeted therapy.

Journal: Journal of oncology20120101

Title: Analysing properties of proteasome inhibitors using kinetic and X-ray crystallographic studies.

Journal: Methods in molecular biology (Clifton, N.J.)20120101

Title: Blocking autophagy prevents bortezomib-induced NF-κB activation by reducing I-κBα degradation in lymphoma cells.

Journal: PloS one20120101

Title: Novel therapies for aggressive B-cell lymphoma.

Journal: Advances in hematology20120101

Title: On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53.

Journal: PloS one20120101

Title: Lenalidomide before and after Autologous Hematopoietic Stem Cell Transplantation in Multiple Myeloma.

Journal: Advances in hematology20120101

Title: Carfilzomib: a novel treatment in relapsed and refractory multiple myeloma.

Journal: OncoTargets and therapy20120101

Title: Drugs: More shots on target.

Journal: Nature20111214

Title: Advances in the understanding of mechanisms and therapeutic use of bortezomib.

Journal: Discovery medicine20111201

Title: Pharmacokinetics, pharmacodynamics, metabolism, distribution, and excretion of carfilzomib in rats.

Journal: Drug metabolism and disposition: the biological fate of chemicals20111001

Title: Pharmacogenomics of bortezomib test-dosing identifies hyperexpression of proteasome genes, especially PSMD4, as novel high-risk feature in myeloma treated with Total Therapy 3.

Journal: Blood20110929

Title: Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo.

Journal: Molecular cancer therapeutics20110901

Title: [Development of novel agents for multiple myeloma; now and the future].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology20110801

Title: Novel proteasome inhibitors to overcome bortezomib resistance.

Journal: Journal of the National Cancer Institute20110706

Title: A genetic interaction network of five genes for human polycystic kidney and liver diseases defines polycystin-1 as the central determinant of cyst formation.

Journal: Nature genetics20110619

Title: How to treat patients with relapsed/refractory multiple myeloma: evidence-based information and opinions.

Journal: Expert opinion on investigational drugs20110601

Title: Alkaline phosphatase variation during carfilzomib treatment is associated with best response in multiple myeloma patients.

Journal: European journal of haematology20110601

Title: Specific cell-permeable inhibitor of proteasome trypsin-like sites selectively sensitizes myeloma cells to bortezomib and carfilzomib.

Journal: Chemistry & biology20110527

Title: Nonproteasomal targets of the proteasome inhibitors bortezomib and carfilzomib: a link to clinical adverse events.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20110501

Title: Carfilzomib: a novel second-generation proteasome inhibitor.

Journal: Future oncology (London, England)20110501

Title: RNAi screen of the druggable genome identifies modulators of proteasome inhibitor sensitivity in myeloma including CDK5.

Journal: Blood20110407

Title: Recent advances in myeloma treatment.

Journal: Transfusion and apheresis science : official journal of the World Apheresis Association : official journal of the European Society for Haemapheresis20110401

Title: Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20110401

Title: Second generation proteasome inhibitors: carfilzomib and immunoproteasome-specific inhibitors (IPSIs).

Journal: Current cancer drug targets20110301

Title: Unfolded protein response in cancer: the physician's perspective.

Journal: Journal of hematology & oncology20110101

Title: Histone deacetylase turnover and recovery in sulforaphane-treated colon cancer cells: competing actions of 14-3-3 and Pin1 in HDAC3/SMRT corepressor complex dissociation/reassembly.

Journal: Molecular cancer20110101

Title: Emerging role of carfilzomib in treatment of relapsed and refractory lymphoid neoplasms and multiple myeloma.

Journal: Core evidence20110101

Title: Therapeutic strategies to enhance the anticancer efficacy of histone deacetylase inhibitors.

Journal: Journal of biomedicine & biotechnology20110101

Title: Light chain (AL) amyloidosis: update on diagnosis and management.

Journal: Journal of hematology & oncology20110101

Title: Molecular mechanisms of bortezomib resistant adenocarcinoma cells.

Journal: PloS one20110101

Title: Targeting histone deacetyalses in the treatment of B- and T-cell malignancies.

Journal: Investigational new drugs20101201

Title: New twists on proteasome inhibitors.

Journal: Nature biotechnology20101201

Title: Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.

Journal: The Biochemical journal20100915

Title: Novel disease targets and management approaches for diffuse large B-cell lymphoma.

Journal: Leukemia & lymphoma20100801

Title: Peripheral neuropathy during bortezomib treatment of multiple myeloma: a review of recent studies.

Journal: Leukemia & lymphoma20100701

Title: The pan-HDAC inhibitor vorinostat potentiates the activity of the proteasome inhibitor carfilzomib in human DLBCL cells in vitro and in vivo.

Journal: Blood20100603

Title: Activation of mutant enzyme function in vivo by proteasome inhibitors and treatments that induce Hsp70.

Journal: PLoS genetics20100101

Title: Bortezomib.

Journal: Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer20100101

Title: Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry.

Journal: Current topics in medicinal chemistry20100101

Title: State-of-the-Art Management of Complications of Myeloma and Its Treatment.

Journal: Advances in hematology20100101

Title: Proteasome inhibition and its therapeutic potential in multiple myeloma.

Journal: Biologics : targets & therapy20100101

Title: Relapsed multiple myeloma.

Journal: Hematology. American Society of Hematology. Education Program20100101

Title: Ubiquitin Drug Discovery & Diagnostics 2009 - First Annual Conference.

Journal: IDrugs : the investigational drugs journal20091201

Title: A phase 1 dose escalation study of the safety and pharmacokinetics of the novel proteasome inhibitor carfilzomib (PR-171) in patients with hematologic malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20091115

Title: Acquisition of a multidrug-resistant phenotype with a proteasome inhibitor in multiple myeloma.

Journal: Leukemia20091101

Title: Proteasome inhibitors in the treatment of multiple myeloma.

Journal: Leukemia20091101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology20091101

Title: Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome.

Journal: Blood20091015

Title: Clinical development of novel proteasome inhibitors for cancer treatment.

Journal: Expert opinion on investigational drugs20090701

Title: Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).

Journal: Journal of medicinal chemistry20090514

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology20090401

Title: Antiproliferative and proapoptotic effects of proteasome inhibitors and their combination with histone deacetylase inhibitors on leukemia cells.

Journal: Cardiovascular & hematological disorders drug targets20090301

Title: New drugs in multiple myeloma and the significance of autologous stem cell transplants.

Journal: Clinical advances in hematology & oncology : H&O20090301

Title: Novel therapies for relapsed myeloma.

Journal: Hematology. American Society of Hematology. Education Program20090101

Title: Future novel single agent and combination therapies.

Journal: Cancer journal (Sudbury, Mass.)20090101

Title: Discovery of novel proteasome inhibitors using a high-content cell-based screening system.

Journal: PloS one20090101

Title: The development and pharmacology of proteasome inhibitors for the management and treatment of cancer.

Journal: Advances in pharmacology (San Diego, Calif.)20090101

Title: Lenalidomide in multiple myeloma: an evidence-based review of its role in therapy.

Journal: Core evidence20090101

Title: The BH3-only mimetic ABT-737 synergizes the antineoplastic activity of proteasome inhibitors in lymphoid malignancies.

Journal: Blood20081001

Title: Practical considerations for multiple myeloma: an overview of recent data and current options.

Journal: Clinical lymphoma & myeloma20080801

Title: Targeting Bcl-2 family members with the BH3 mimetic AT-101 markedly enhances the therapeutic effects of chemotherapeutic agents in in vitro and in vivo models of B-cell lymphoma.

Journal: Blood20080601

Title: The potential of proteasome inhibitors in cancer therapy.

Journal: Expert opinion on investigational drugs20080601

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology20080301

Title: Mechanisms of proteasome inhibitor action and resistance in cancer.

Journal: Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy20080101

Title: Targeting the UPS as therapy in multiple myeloma.

Journal: BMC biochemistry20080101

Title: Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma.

Journal: Blood20071101

Title: Epoxomicin, a new antitumor agent of microbial origin.

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Title: Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90.

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