BIIB 021

• CAT Number: I005088
• CAS Number: 848695-25-0
• Molecular Formula: C₁₄H₁₅ClN₆O
• Molecular Weight: 318.76
• Purity: ≥95%
• Synonyms: 6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]purin-2-amine
• Target: HSP
• Solubility: DMSO: ≥ 45 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 1.7 nM(Ki)
• InChI: InChI=1S/C14H15ClN6O/c1-7-4-17-9(8(2)11(7)22-3)5-21-6-18-10-12(15)19-14(16)20-13(10)21/h4,6H,5H2,1-3H3,(H2,16,19,20)
• InChIKey: QULDDKSCVCJTPV-UHFFFAOYSA-N
• SMILES: CC1=CN=C(C(=C1OC)C)CN2C=NC3=C2N=C(N=C3Cl)N

BIIB 021（Cat No.:I005088）is a potent and selective inhibitor of heat shock protein 90 (Hsp90), a molecular chaperone that stabilizes and activates various client proteins involved in cancer cell growth and survival. By inhibiting Hsp90, BIIB 021 promotes the degradation of these client proteins, leading to the disruption of multiple oncogenic pathways, cell cycle arrest, and apoptosis in cancer cells. BIIB 021 has demonstrated efficacy in preclinical and clinical studies for treating various cancers, including breast and lung cancers. Its targeted mechanism makes it a promising candidate for cancer therapy.

Reference

[1]. Lundgren, Karen; Zhang, Hong; Brekken, John; BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Molecular Cancer Therapeutics (2009), 8(4), 921-929.
[2]. Kasibhatla, Srinivas R.; Hong, Kevin; Biamonte, Marco A.; Rationally Designed High-Affinity 2-Amino-6-halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity. Journal of Medicinal Chemistry (2007), 50(12), 2767-2778.
[3]. Dickson MA, Okuno SH, Keohan ML, Maki RG, D/’Adamo DR, Akhurst TJ, Antonescu CR, Schwartz GK.Phase II study of the HSP90-inhibitor BIIB021 in gastrointestinal stromal tumors.Ann Oncol. 2012 Aug 16.
[4]. Xu L, Woodward C, Khan S, Prakash C.In vitro metabolism of BIIB021, an inhibitor of heat shock protein 90, in liver microsomes and hepatocytes of rats, dogs, and humans and recombinant human cytochrome P450 isoforms.Drug Metab Dispos. 2012 Apr;40(4):680-93. Epub 2012 Jan 4.
[5]. Zhang H, Neely L, Lundgren K, Yang YC, Lough R, Timple N, Burrows F.BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance.Int J Cancer. 2010 Mar 1;126(5):1226-34.