BIIB 021 is a selective, Hsp90 competitive inhibitor (K_i = 1.7 nM). Displays no significant activity at a range of ATP-binding kinases or Na⁺K⁺ ATPase. Induces degradation of HER-2 in vitro (EC₅₀ = 38 nM in MCF-7 cells). Inhibits growth and promotes cell death in a variety of human tumor cells. Orally bioavailable.

Product Specifications

Molecular Weight

318.76

Formula

C₁₄H₁₅ClN₆O

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

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

CAS Number

848695-25-0

PubChem ID

16736529

InChI Key

QULDDKSCVCJTPV-UHFFFAOYSA-N

SMILES

ClC1=C2C(N(CC3=NC=C(C)C(OC)=C3C)C=N2)=NC(N)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	31.88	100

Preparing Stock Solutions for BIIB 021

The following data is based on the product molecular weight 318.76

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.14 mL	15.69 mL	31.37 mL
5 mM	0.63 mL	3.14 mL	6.27 mL
10 mM	0.31 mL	1.57 mL	3.14 mL
50 mM	0.06 mL	0.31 mL	0.63 mL

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Background References

References are publications that support the biological activity of the product.

Yin BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy. Int.J.Cancer 2010 PMID: 19662650
Lundgren BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol.Cancer Ther. 2009 PMID: 19372565

BIIB 021

Tocris Bioscience, part of Bio-Techne | Catalog # 4608

Key Product Details

Description

Alternative Names

View all HSP90 Inhibitors »

Product Description