BIIB 021 | 2291

A synthetic, small molecule Hsp90 inhibitor that binds competitively with geldanamycin in the ATP-binding pocket of Hsp90. In tumor cells, BIIB021 induces the degradation of Hsp90 client proteins including HER-2, AKT, and Raf-1 and up-regulates expression of the heat shock proteins Hsp70 and Hsp27. 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.

BIIB 021 is a synthetic, small molecule Hsp90 inhibitor that binds competitively with geldanamycin in the ATP-binding pocket of Hsp90. In tumor cells, BIIB021 induces the degradation of Hsp90 client proteins including HER-2, AKT, and Raf-1 and up-regulates expression of the heat shock proteins Hsp70 and Hsp27.

2291 | BIIB 021 DataSheet

Alternate Name/Synonyms: 6-Chloro-9-[(4-methoxy-3,5-dimethyl­-2-pyridinyl)methyl]-9H-purin-2-amine; CNF2024

Appearance: White to off-white solid

Formulation: N/A

CAS Number: 848695-25-0

Structure Available?: Yes

Peptide sequence: No

Salt Form: No

Molecular Formula: C₁₄H₁₅ClN₆O

Molecular Weight: 318.76

Cell-Permeable?: Yes

Purity: ≥99% by HPLC

Solubilities: DMSO (~65 mg/ml) or EtOH (~3 mg/ml)

Handling: Protect from light and moisture

Country of Origin: USA

Tag Line: A potent Hsp90 inhibitor

MDL Number: MFCD15528939

PubChem CID: 16736529

SMILES: CC1=CN=C(C(=C1OC)C)CN2C=NC3=C2N=C(N=C3Cl)N

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)

InChi Key: QULDDKSCVCJTPV-UHFFFAOYSA-N