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167465-36-3,MFCD00942300
Catalog No.:AA007VUF

167465-36-3 | Zosuquidar trihydrochloride

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1mg
98%
in stock  
$43.00   $30.00
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5mg
98%
in stock  
$96.00   $68.00
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10mg
98%
in stock  
$155.00   $109.00
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25mg
98%
in stock  
$243.00   $171.00
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA007VUF
Chemical Name:
Zosuquidar trihydrochloride
CAS Number:
167465-36-3
Molecular Formula:
C32H34Cl3F2N3O2
Molecular Weight:
636.9871
MDL Number:
MFCD00942300
SMILES:
OC(CN1CCN(CC1)[C@@H]1c2ccccc2[C@@H]2[C@H](c3c1cccc3)C2(F)F)COc1cccc2c1cccn2.Cl.Cl.Cl
Properties
Computed Properties
 
Complexity:
806  
Covalently-Bonded Unit Count:
4  
Defined Atom Stereocenter Count:
3  
Heavy Atom Count:
42  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
4  
Rotatable Bond Count:
6  

Literature

Title: Clinical disposition, metabolism and in vitro drug-drug interaction properties of omadacycline.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20170801

Title: The inhibitory and combinative mechanism of HZ08 with P-glycoprotein expressed on the membrane of Caco-2 cell line.

Journal: Toxicology and applied pharmacology 20140115

Title: Interactions with selected drug renal transporters and transporter-mediated cytotoxicity in antiviral agents from the group of acyclic nucleoside phosphonates.

Journal: Toxicology 20130915

Title: Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin.

Journal: Breast cancer research and treatment 20120701

Title: Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry.

Journal: Journal of pharmaceutical and biomedical analysis 20120701

Title: Excretion of the dipeptidyl peptidase-4 inhibitor linagliptin in rats is primarily by biliary excretion and P-gp-mediated efflux.

Journal: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20120411

Title: Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.

Journal: Journal of medicinal chemistry 20110825

Title: P-glycoprotein (ABCB1) transports the primary active tamoxifen metabolites endoxifen and 4-hydroxytamoxifen and restricts their brain penetration.

Journal: The Journal of pharmacology and experimental therapeutics 20110601

Title: Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.

Journal: Journal of medicinal chemistry 20110324

Title: Endoxifen, the active metabolite of tamoxifen, is a substrate of the efflux transporter P-glycoprotein (multidrug resistance 1).

Journal: Drug metabolism and disposition: the biological fate of chemicals 20110301

Title: Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20110201

Title: Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999.

Journal: Blood 20101118

Title: A randomized, placebo-controlled, double-blind phase 2 study of docetaxel compared to docetaxel plus zosuquidar (LY335979) in women with metastatic or locally recurrent breast cancer who have received one prior chemotherapy regimen.

Journal: Cancer chemotherapy and pharmacology 20090901

Title: P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib.

Journal: The Journal of pharmacology and experimental therapeutics 20090901

Title: A phase I trial of continuous infusion of the multidrug resistance inhibitor zosuquidar with daunorubicin and cytarabine in acute myeloid leukemia.

Journal: Leukemia research 20090801

Title: Leukemic blast and natural killer cell P-glycoprotein function and inhibition in a clinical trial of zosuquidar infusion in acute myeloid leukemia.

Journal: Leukemia research 20090601

Title: P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients.

Journal: BMC cancer 20090101

Title: Characterization of substrates and inhibitors for the in vitro assessment of Bcrp mediated drug-drug interactions.

Journal: Pharmaceutical research 20081001

Title: Vectorial transport of the plant alkaloid berberine by double-transfected cells expressing the human organic cation transporter 1 (OCT1, SLC22A1) and the efflux pump MDR1 P-glycoprotein (ABCB1).

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20080201

Title: Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML).

Journal: BMC cancer 20080101

Title: P-glycoprotein-mediated active efflux of the anti-HIV1 nucleoside abacavir limits cellular accumulation and brain distribution.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20071101

Title: Modulation of the brain distribution of imatinib and its metabolites in mice by valspodar, zosuquidar and elacridar.

Journal: Pharmaceutical research 20070901

Title: Inhibition of P-glycoprotein activity at the primate blood-brain barrier increases the distribution of nelfinavir into the brain but not into the cerebrospinal fluid.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20070901

Title: Influence of breast cancer resistance protein (Abcg2) and p-glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec) across the mouse blood-brain barrier.

Journal: Journal of neurochemistry 20070901

Title: Multidrug resistance in lymphoma: is it time for clinical trials?

Journal: Leukemia & lymphoma 20070401

Title: Phase I/II trial of a P-glycoprotein inhibitor, Zosuquidar.3HCl trihydrochloride (LY335979), given orally in combination with the CHOP regimen in patients with non-Hodgkin's lymphoma.

Journal: Leukemia & lymphoma 20070401

Title: Trabectedin (ET-743, Yondelis) is a substrate for P-glycoprotein, but only high expression of P-glycoprotein confers the multidrug resistance phenotype.

Journal: Investigational new drugs 20070201

Title: Role of drug efflux carriers in the healthy and diseased brain.

Journal: Annals of neurology 20061101

Title: Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20060401

Title: Phase I study of the multidrug resistance inhibitor zosuquidar administered in combination with vinorelbine in patients with advanced solid tumours.

Journal: Cancer chemotherapy and pharmacology 20050801

Title: Phase I study of docetaxel in combination with the P-glycoprotein inhibitor, zosuquidar, in resistant malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20041101

Title: Stereochemistry of C-6 nucleophilic displacements on 1,1-difluorocyclopropyldibenzosuberanyl substrates. An improved synthesis of multidrug resistance modulator LY335979 trihydrochloride.

Journal: The Journal of organic chemistry 20041029

Title: New insights into drug absorption: studies with sirolimus.

Journal: Therapeutic drug monitoring 20041001

Title: Efficacy of novel P-glycoprotein inhibitors to increase the oral uptake of paclitaxel in mice.

Journal: Investigational new drugs 20040801

Title: Clinical effects and P-glycoprotein inhibition in patients with acute myeloid leukemia treated with zosuquidar trihydrochloride, daunorubicin and cytarabine.

Journal: Haematologica 20040701

Title: A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxorubicin in patients with advanced malignancy.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040515

Title: Bioanalysis of zosuquidar trihydrochloride (LY335979) in small volumes of human and murine plasma by ion-pairing reversed-phase high-performance liquid chromatography.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20031205

Title: A population pharmacokinetic model for paclitaxel in the presence of a novel P-gp modulator, Zosuquidar Trihydrochloride (LY335979).

Journal: British journal of clinical pharmacology 20030701

Title: Inhibition of P-glycoprotein by newer antidepressants.

Journal: The Journal of pharmacology and experimental therapeutics 20030401

Title: Modulation of P-glycoprotein but not MRP1- or BCRP-mediated drug resistance by LY335979.

Journal: International journal of cancer 20030101

Title: The role of the efflux transporter P-glycoprotein in brain penetration of prednisolone.

Journal: The Journal of endocrinology 20021001

Title: Evidence of P-glycoprotein mediated apical to basolateral transport of flunisolide in human broncho-tracheal epithelial cells (Calu-3).

Journal: British journal of pharmacology 20011201

Title: Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells.

Journal: Biochemical pharmacology 20010601

Title: Effect of capillary efflux transport inhibition on the determination of probe recovery during in vivo microdialysis in the brain.

Journal: The Journal of pharmacology and experimental therapeutics 20010601

Title: Assessment of active transport of HIV protease inhibitors in various cell lines and the in vitro blood--brain barrier.

Journal: AIDS (London, England) 20010309

Title: Reversal of multidrug resistance by the P-glycoprotein modulator, LY335979, from the bench to the clinic.

Journal: Current medicinal chemistry 20010101

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