BIIB 021

• CAT Number: I005088
• CAS Number: 848695-25-0
• Molecular Formula: C₁₄H₁₅ClN₆O
• Molecular Weight: 318.76
• Purity: ≥95%
• Target: HSP
• Solubility: DMSO: ≥ 45 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 1.7 nM(Ki)
• IUPAC Name: 6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]purin-2-amine
• 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

BIIB021 (Cat.No:I005088) is an orally available inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor BIIB021 selectively binds to Hsp90 and inhibits its chaperone function, which leads to the degradation of oncogenic signaling proteins, cell cycle kinases, and transcription factors involved in cancer cell growth and survival. This may result in the induction of tumor cell apoptosis and the inhibition of tumor cell proliferation. BIIB021 has shown promising results in preclinical studies of various types of cancer.

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.