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MedKoo product information:
KOS-1584
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MedKoo Code#: 201650
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Name: KOS-1584
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CAS#: 1032119-44-0
Synonym:
KOS 1584；9,10-didehydroepothilone D; R1645.
IUPAC/Chemical name:
(4S,7R,8R,9S,10Z,13Z,16S)-4,8-dihydroxy-5,5,7,9,13-pentamethyl-16-((E)-1-(2-methylthiazol-4-yl)prop-1-en-2-yl)oxacyclohexadeca-10,13-diene-2,6-dione
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Chemical structure |
Theoretical analysis
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Chemical Formula: C27H39NO5S
Exact Mass: 489.25489
Molecular Weight: 489.67
m/z: 489.25489 (100.0%), 490.25825 (29.2%),
491.25069 (4.5%), 491.26160 (4.1%), 492.25405 (1.3%), 491.25914
(1.0%)
Elemental Analysis: C, 66.23; H, 8.03; N,
2.86; O, 16.34; S, 6.55
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Availability and price:
This agent is not in stock, which may be available through custom synthesis.
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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KOS-1584 is a
second-generation epothilone with potential antineoplastic activity.
Epothilone KOS-1584 binds to tubulin and induces microtubule
polymerization and stabilizes microtubules against depolymerization,
which may result in the inhibition of cell division, the induction of
G2/M arrest, and apoptosis. Compared to first-generation epothilones,
this agent exhibits greater safety and efficacy with an enhanced
pharmaceutical profile, including enhanced water solubility and tumor
penetration, and reduced CNS exposure. In addition, epothilone KOS-1584
is a poor substrate for the P-glycoprotein (P-gp) drug efflux pump.
Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
Current developer:
Kosan Biosciences Inc
1: Cheng KL, Bradley T, Budman DR. Novel
microtubule-targeting agents - the epothilones. Biologics. 2008
Dec;2(4):789-811. PubMed PMID: 19707459; PubMed Central PMCID:
PMC2727900.
2: Cigler T, Vahdat L. Integrating epothilones into the treatment of
patients with metastatic breast cancer: clinical perspectives on
incorporating recent data in the practice setting. Clin Breast Cancer.
2008 Dec;8 Suppl 4:S166-70. Review. PubMed PMID: 19158037.
3: Lee JJ, Kelly WK. Epothilones: tubulin polymerization as a novel
target for prostate cancer therapy. Nat Clin Pract Oncol. 2009
Feb;6(2):85-92. Epub 2008 Dec 2. Review. PubMed PMID: 19048010.
4: Trivedi M, Budihardjo I, Loureiro K, Reid TR, Ma JD. Epothilones: a
novel class of microtubule-stabilizing drugs for the treatment of
cancer. Future Oncol. 2008 Aug;4(4):483-500. Review. PubMed PMID:
18684060.
5: Donovan D, Vahdat LT. Epothilones: clinical update and future
directions. Oncology (Williston Park). 2008 Apr 15;22(4):408-16;
discussion 416, 421, 424 passim. Review. PubMed PMID: 18472615.
6: Vahdat LT. Clinical studies with epothilones for the treatment of
metastatic breast cancer. Semin Oncol. 2008 Apr;35(2 Suppl 2):S22-30;
quiz S40. Review. PubMed PMID: 18410796.
7: Burris HA 3rd. Preclinical investigations with epothilones in breast
cancer models. Semin Oncol. 2008 Apr;35(2 Suppl 2):S15-21; quiz S39.
Review. PubMed PMID: 18410795.
8: Vahdat L. Ixabepilone: a novel antineoplastic agent with low
susceptibility to multiple tumor resistance mechanisms. Oncologist. 2008
Mar;13(3):214-21. Review. PubMed PMID: 18378531.
9: Pronzato P. New therapeutic options for chemotherapy-resistant
metastatic breast cancer: the epothilones. Drugs. 2008;68(2):139-46.
Review. PubMed PMID: 18197722.
10: Fumoleau P, Coudert B, Isambert N, Ferrant E. Novel tubulin-targeting
agents: anticancer activity and pharmacologic profile of epothilones and
related analogues. Ann Oncol. 2007 Jul;18 Suppl 5:v9-15. Review. PubMed
PMID: 17656562.
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