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SML4248

BIIB021

≥98% (HPLC), powder, Hsp90 inhibitor

Synonym(s):

6-Chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine, 6-Chloro-9-(4-methoxy-3,5-dimethylpyridin-2-ylmethyl)-9Hpurin-2-ylamine, [6-Chloro-9-(4-methoxy-3,5-dimethylpyridin-2-ylmethyl)-9H-purin-2-yl]amine, BIIB 021, BIIB-021, CNF 2024, CNF-2024,CNF2024

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About This Item

Empirical Formula (Hill Notation):
C14H15ClN6O
CAS Number:
848695-25-0
Molecular Weight:
318.76
MDL number:
MFCD15528939
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

General description

BIIB021 is a purine scaffold-based second-generation heat shock protein 90 (Hsp90) inhibitor.

Application

BIIB021 may be used to study its effect on growth of natural killer (NK) cells and T cell lymphomas.

Biochem/physiol Actions

BIIB021 (CNF2024) is an orally active, potent and selective heat shock protein 90 (Hsp90) inhibitor that targets the ATP site of Hsp90 (Ki = 1.7 nM against 2 nM FITC-geldanamycin in competitive binding for 0.8 nM rhHsp90α), but not those of 20 cellular kinases or Na+/K+ ATPase. BIIB021 induces Her-2 degradation in MCF7 cells (IC50 = 38 nM post 16h incubation) and exhibits anti-cancer efficacy in cultures (IC50 = 60-310 nM among 8 cancer lines) and in mice in vivo (51-94% tumor growth inhibition among 6 human tumor models; 75-125 mg/kg/d 5x per wk for 5 wks).

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302,H317

Hazard Classifications

Acute Tox. 4 Oral - Skin Sens. 1B

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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