Epothilone B Inhibitor CAS No. 152044-54-7

Cat. No.	Name	Size	Price
KI0051	Epothilone B	2 mg	$112
	Epothilone B	5 mg	$192
	Epothilone B	10 mg	$302.4
	Epothilone B	25 mg	$676.8

Chemical Characteristic

Product Name	Epothilone B
Synonyms	EPO906, Patupilone, CGP047906
CAS No.	152044-54-7
Molecular Weight	507.68
Formula	C₂₇H₄₁NO₆S
Chemical Name	(1S,3S,7S,10R,11S,12S,16R,E)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-(1-(2-methylthiazol-4-yl)prop-1-en-2-yl)-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione
Smiles	[C@@]12(C[C@H](OC(=O)C[C@@H](C(C(=O)[C@@H]([C@H]([C@H](CCC[C@]1(O2)C)C)O)C)(C)C)O)/C=C/c1nc(sc1)C)C
Chemical Structure

Biological activities

Epothilone B is a highly potent non-taxane microtubule stabilizing agent with a K_{i of 0.75 µM. Epothilone B directly inhibits growth and survival of multiple myeloma (MM) cells. Epothilone B induces G2M arrest of MM cells, with subsequent apoptosis. Epothilone B inhibits proliferation of MM cells induced by adherence to bone marrow stromal cells (BMSCs). Epothilone B in a dose-dependent manner decreases the survival of RPMI 8226, U266, Dex-sensitive MM.1S, Dex-resistant MM.1R cells. Treatment with epothilone B modulates expression of apoptosis-regulating proteins. Epothilone B inhibits tumor cell adhesion-induced up-regulation of vascular endothelial growth factor (VEGF) secretion. Coincubation of epothilone B with IL-6 or IGF-1 results in enhanced reduction in the fraction of proliferating MM.1S cells. ^[1] Epothilone B inhibits the antiproliferative for prostate cancer cell line DU 145 and PC-3M cancer cells with IC50s of 0.31 and 0.52 nM, respectively. Epothilone B (5 mg/kg) produces protracted growth inhibition of subcutaneous PC-3M tumors, with transient body weight loss. Importantly, epothilone B retains activity against paclitaxel-refractory cells overexpressing the P-gp efflux pump (MDR1 gene product) or harboring mutations in β-tubulin. ^[2] Epothilone B inhibits the growth of paclitaxel-sensitive human epidermoid carcinoma cells KB-31 and KB-8511 with IC50s of 0.19 and 0.18 nM, respectively. ^[3] In addition, epothilone B is effective in slowing tumor growth and prolonging median survival of mice that receive orthotopical transplants with MM tumor cells. ^[1] In mice with orthotopic PC-3M tumors, 4 or 5 mg/kg/week epothilone B impaires primary tumor growth, abrogates metastases and enhances survival, with only transient body weight loss. ^[2]}

Protocols

Epothilone B is dissolved in DMSO and stored as 10 mM and 100 mM stock solutions, respectively, at -20°C until use. ^[1]

References

[1] Lin B, et al. Patupilone (epothilone B) inhibits growth and survival of multiple myeloma cells in vitro and in vivo. Blood. 2005, 105(1): 350-357. [2] O'Reilly T, et al. Patupilone (epothilone B, EPO906) inhibits growth and metastasis of experimental prostate tumors in vivo. Prostate. 2005, 65(3): 231-240. [3] Altmann KH, et al. Synthesis and biological evaluation of highly potent analogues of epothilones B and D. Bioorg Med Chem Lett. 2000, 10(24): 2765-2768.

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