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BMS-641988

Chemical Structure : BMS-641988

CAS No.: 573738-99-5

BMS-641988 (BMS 641988;BMS641988)

Catalog No.: PC-61086Not For Human Use, Lab Use Only.

BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM; displays high selectivity over the glucocorticoid and progesterone receptors; displayed 3-7-fold increased antagonist activity of AR transactivation compared with bicalutamide; strongly inhibits androgen-dependent growth of the ventral prostate and seminal vesicles in rats, and is efficacious in CWR-22-BMSLD1 tumors initially refractory to treatment with bicalutamide.

Prostate Cancer

Phase 1 Clinical

Physicochemical Properties

M.Wt 471.45
Formula C20H20F3N3O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((3aR,4R,5R,7R,7aS)-2-(4-cyano-3-(trifluoromethyl)phenyl)-4,7-dimethyl-1,3-dioxooctahydro-1H-4,7-epoxyisoindol-5-yl)ethanesulfonamide

References

1. Balog A, et al. ACS Med Chem Lett. 2015 Jun 19;6(8):908-12.

2. Attar RM, et al. Cancer Res. 2009 Aug 15;69(16):6522-30.

3. Rathkopf D, et al. Clin Cancer Res. 2011 Feb 15;17(4):880-7.

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