Home Other Building Blocks 572924-54-0
572924-54-0,MFCD13184816
Catalog No.:AA00IMNH

572924-54-0 | Deforolimus

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
≥95%
in stock  
$59.00   $41.00
- +
5mg
≥95%
in stock  
$165.00   $115.00
- +
10mg
≥95%
in stock  
$234.00   $164.00
- +
25mg
≥95%
in stock  
$456.00   $319.00
- +
50mg
in stock  
$593.00   $415.00
- +
200mg
in stock  
$1,354.00   $948.00
- +
  • Technical Information
  • Properties
  • Upstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Upstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00IMNH
Chemical Name:
Deforolimus
CAS Number:
572924-54-0
Molecular Formula:
C53H84NO14P
Molecular Weight:
990.2061
MDL Number:
MFCD13184816
SMILES:
CO[C@@H]1C[C@@H](CC[C@H]1OP(=O)(C)C)C[C@H]([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H](CC[C@H]2C)C[C@H](OC)/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C1)C)/C)O)OC)C)C)/C)C
Properties
Properties
 
BP:
996.16°C at 760 mmHg  
Form:
Solid  
MP:
95 - 98°C  
Storage:
Inert atmosphere;-20 ℃;  

Computed Properties
 
Complexity:
1940  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
15  
Defined Bond Stereocenter Count:
4  
Heavy Atom Count:
69  
Hydrogen Bond Acceptor Count:
14  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
8  
XLogP3:
5.9  

Upstream Synthesis Route

[1]Patent:US2004/73024,2004,A1,.Locationinpatent:Page38

[2]Patent:US2004/73024,2004,A1,.Locationinpatent:Page39

[1]Patent:US2014/58081,2014,A1,.Locationinpatent:Paragraph0049;0050

[1]Patent:US2014/58081,2014,A1,.Locationinpatent:Paragraph0047

[1]Patent:US2014/58081,2014,A1,

[2]Patent:US2014/58081,2014,A1,

[1]Patent:US2014/58081,2014,A1,

Literature

Title: A single supratherapeutic dose of ridaforolimus does not prolong the QTc interval in patients with advanced cancer.

Journal: Cancer chemotherapy and pharmacology 20121001

Title: Dual targeting of the Akt/mTOR signaling pathway inhibits castration-resistant prostate cancer in a genetically engineered mouse model.

Journal: Cancer research 20120901

Title: Clinical trial end points for assessing efficacy of novel therapies for soft-tissue sarcomas.

Journal: Expert review of anticancer therapy 20120901

Title: A role for maintenance therapy in managing sarcoma.

Journal: Cancer treatment reviews 20120801

Title: Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models.

Journal: International journal of oncology 20120801

Title: [Soft-tissue sarcoma: recent developments].

Journal: Deutsche medizinische Wochenschrift (1946) 20120801

Title: The minimal impact of food on the pharmacokinetics of ridaforolimus.

Journal: Cancer chemotherapy and pharmacology 20120701

Title: Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a phase 1 clinical trial.

Journal: Cancer chemotherapy and pharmacology 20120501

Title: The effect of multiple doses of rifampin and ketoconazole on the single-dose pharmacokinetics of ridaforolimus.

Journal: Cancer chemotherapy and pharmacology 20120501

Title: Ridaforolimus for patients with progressive or recurrent malignant glioma: a perisurgical, sequential, ascending-dose trial.

Journal: Cancer chemotherapy and pharmacology 20120401

Title: Phase I study for ridaforolimus, an oral mTOR inhibitor, in Japanese patients with advanced solid tumors.

Journal: Cancer chemotherapy and pharmacology 20120401

Title: Regulation of physiologic actions of LRRK2: focus on autophagy.

Journal: Neuro-degenerative diseases 20120401

Title: mTOR inhibitors and its role in the treatment of head and neck squamous cell carcinoma.

Journal: Current treatment options in oncology 20120301

Title: [PI3K-AKT-mTOR pathway and cancer].

Journal: Bulletin du cancer 20120201

Title: Phase II study of the mammalian target of rapamycin inhibitor ridaforolimus in patients with advanced bone and soft tissue sarcomas.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120101

Title: Antitumor activity of ridaforolimus and potential cell-cycle determinants of sensitivity in sarcoma and endometrial cancer models.

Journal: Molecular cancer therapeutics 20111001

Title: Clinical presentation and management of mTOR inhibitor-associated stomatitis.

Journal: Oral oncology 20111001

Title: Ridaforolimus: a promising drug in the treatment of soft-tissue sarcoma and other malignancies.

Journal: Future oncology (London, England) 20110701

Title: Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens.

Journal: Molecular cancer therapeutics 20110601

Title: Phase I studies of drug combinations.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20101020

Title: Phase IB study of the mTOR inhibitor ridaforolimus with capecitabine.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20101020

Title: Ridaforolimus.

Journal: Drugs in R&D 20100901

Title: Phase Ib study of weekly mammalian target of rapamycin inhibitor ridaforolimus (AP23573; MK-8669) with weekly paclitaxel.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20100601

Title: Emergent toxicities associated with the use of mTOR inhibitors in patients with advanced renal carcinoma.

Journal: Anti-cancer drugs 20100601

Title: [Treatment of adult patients with metastatic sarcoma: current shift in concepts].

Journal: Bulletin du cancer 20100601

Title: Preliminary characterization of oral lesions associated with inhibitors of mammalian target of rapamycin in cancer patients.

Journal: Cancer 20100101

Title: Targeted therapy in lymphoma.

Journal: Journal of hematology & oncology 20100101

Title: Exploring mammalian target of rapamycin (mTOR) inhibition for treatment of mantle cell lymphoma and other hematologic malignancies.

Journal: Leukemia & lymphoma 20091201

Title: [Targeted therapies and their indications in solid neoplasias].

Journal: La Revue de medecine interne 20090501

Title: The applicability of mTOR inhibition in solid tumors.

Journal: Current cancer drug targets 20090501

Title: The pharmacology of mTOR inhibition.

Journal: Science signaling 20090421

Title: Targeting the mTOR pathway using deforolimus in cancer therapy.

Journal: Future oncology (London, England) 20090401

Title: A phase I trial to determine the safety, tolerability, and maximum tolerated dose of deforolimus in patients with advanced malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090215

Title: [Topics in mTOR pathway and its inhibitors].

Journal: Bulletin du cancer 20090101

Title: NCCN Task Force Report: mTOR inhibition in solid tumors.

Journal: Journal of the National Comprehensive Cancer Network : JNCCN 20080901

Title: A phase 2 clinical trial of deforolimus (AP23573, MK-8669), a novel mammalian target of rapamycin inhibitor, in patients with relapsed or refractory hematologic malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080501

Title: Molecular target therapies in endometrial cancer: from the basic research to the clinic.

Journal: Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology 20080501

Title: Drug essentials mTOR inhibitors.

Journal: Oncology (Williston Park, N.Y.) 20080401

Title: Phospho-S6 ribosomal protein: a potential new predictive sarcoma marker for targeted mTOR therapy.

Journal: Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc 20080301

Title: The potential role of mTOR inhibitors in non-small cell lung cancer.

Journal: The oncologist 20080201

Title: mTOR: the mammalian target of replication.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20080120

Title: Phase I trial of the novel mammalian target of rapamycin inhibitor deforolimus (AP23573; MK-8669) administered intravenously daily for 5 days every 2 weeks to patients with advanced malignancies.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20080120

Title: Mammalian target of rapamycin as a target in hematological malignancies.

Journal: Current problems in cancer 20080101

Title: [mTOR signal pathway and its inhibitors in antitumor therapy: a review].

Journal: Ai zheng = Aizheng = Chinese journal of cancer 20071201

Title: The biology behind mTOR inhibition in sarcoma.

Journal: The oncologist 20070801

Title: Mechanisms of mammalian target of rapamycin inhibition in sarcoma: present and future.

Journal: Expert review of anticancer therapy 20070801

Title: The role of mTOR inhibitors for treatment of sarcomas.

Journal: Current oncology reports 20070701

Title: Clinical development of mTOR inhibitors: a focus on lymphoma.

Journal: Reviews on recent clinical trials 20070501

Title: New therapeutics for soft-tissue sarcomas in adults.

Journal: Oncology (Williston Park, N.Y.) 20070101

Title: Drug evaluation: AP-23573--an mTOR inhibitor for the treatment of cancer.

Journal: IDrugs : the investigational drugs journal 20060901

Title: Recent developments in targeting the mammalian target of rapamycin (mTOR) kinase pathway.

Journal: Anti-cancer drugs 20060601

Title: Rivera VM, et al. Deforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens. Mol Cancer Ther. 2011 Jun;10(6):1059-71.

Title: Brandt M, et al. mTORC1 Inactivation Promotes Colitis-Induced Colorectal Cancer but Protects from APC Loss-Dependent Tumorigenesis. Cell Metab. 2018 Jan 9;27(1):118-135.e8.

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