BIIB021

Catalog #

27046

$130 *

Size: 5 mg

Qty

Bulk/Custom

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Description

BIIB021 is an orally available, synthetic small-molecule Hsp90 inhibitor. It binds in the ATP-binding pocket of Hsp90 (Ki = 1.7 ± 0.4 nM) and induces HER-2 degradation with an EC50 of 38 ± 10 nM in MCF-7 cells. It ncreases expression of the heat shock proteins Hsp90α and Hsp70, but has no effect on expression of the nonclient protein phosphatidylinositol 3-kinase p85 subunit. BIIB021 inhibits the proliferation of N87, MCF-7, and BT474 tumor cells with IC50 values of 0.06, 0.31, and 0.14 µM, respectively. It has significant antitumor activity in N87 stomach, BT474 breast, CWR22 prostate, U87 glioblastoma, SKOV3 ovarian, and Panc-1 pancreatic tumor xenograft models.

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Synonyms

CNF2024

Product Info

Storage and Usage

Citations

Purity

≥99%

Format

Off-white or light brown powder

Formula

C₁₄H₁₅ClN₆O

318.8 Da

Solubility

Soluble in DMSO at 65 mg/ml; soluble in ethanol at 3 mg/ml with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM.

CAS Registry #

848695-25-0

References

Lundgren, K., et al. Mol. Cancer Ther. 8: 921-929 (2009).

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