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BIIB021

Chemical Structure : BIIB021

CAS No.: 848695-25-0

BIIB021 (CNF2024;BIIB-021;BIIB 021;CNF 2024;CNF-2024)

Catalog No.: PC-42459Not For Human Use, Lab Use Only.

BIIB021 is a potent, selective, orally available HSP90 inhibitor with Ki of 1.7 nM for Hsp90α.

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Biological Activity

BIIB021 is a potent, selective, orally available HSP90 inhibitor with Ki of 1.7 nM for Hsp90α.
BIIB021 displays no significant activity against a broad panel of protein kinases, and Na+K+ ATPase.
BIIB021 induces the degradation of Hsp90 client proteins including HER-2, AKT, and Raf-1 and upregulates expression of Hsp70 and Hsp27 in tumor cells.
BIIB021 inhibits cell growth and induces cell death in cell lines from a variety of tumor types at nanomolar concentrations (IC50=60 nM in N87 cells).
BIIB021 exhibits antitumor effects in vivo.

Physicochemical Properties

M.Wt 318.7615
Formula C14H15ClN6O
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

DMSO: ≥ 45 mg/mL

Chemical Name/SMILES

9H-Purin-2-amine, 6-chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-

References

1. Kasibhatla SR, et al. J Med Chem. 2007 Jun 14;50(12):2767-78.

2. Lundgren K, et al. Mol Cancer Ther. 2009 Apr;8(4):921-9.

3. Böll B, et al. Clin Cancer Res. 2009 Aug 15;15(16):5108-16.

4. Gopalakrishnan R, et al. Clin Cancer Res. 2013 Sep 15;19(18):5016-26.

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