BIIB-021 Property

Melting point:

192-193℃

Boiling point:

588.5±60.0 °C(Predicted)

Density 

1.50

storage temp. 

-20°C

solubility 

Soluble in DMSO (>25 mg/ml)

pka

6.07±0.40(Predicted)

form 

solid

color 

White

Stability:

Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 montha.

Safety

HS Code 

2921490090

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

BIIB-021 Chemical Properties,Usage,Production

Description

BIIB021 is a potent HSP90 inhibitor (IC50 = 30 nM HER-2 degradation).1 It inhibited the proliferation of MCF7 and BT474 breast cancer cell lines (IC50 = 100 nM for each).? BIIB021 has shown efficacy as a therapeutic in multiple cancer models.2-5

Uses

BIIB 021 an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Studies show that BIIB 021 adminisitration led to degradation of Hsp90 client proteins measured in tumor tissue and resulted in the inhibition of tumor growth in several human tumor xenograft models.

Definition

ChEBI: A member of the class of 2-aminopurines that is 2-aminopurine which is substituted by a chlorine at position 6 and by a (4-methoxy-3,5-dimethylpyridin-2-yl)methyl group at position 9.

References

Kasibhatla et al. (2007), Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity; J. Med. Chem. 50 2767 Lundgren et al. (2009), BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90; Mol. Cancer Ther. 8 921 Boll et al. (2009), Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin’s lymphoma cells for natural killer cell-mediated cytotoxicity; Clin. Cancer Res. 15 5108 Zhang et al. (2010), BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance; Int. J. Cancer 126 1226 Wang et al. (2014), BIIB021, a novel Hsp90 inhibitor, sensitizes esophageal squamous cell carcinoma to radiation; Biochem. Biophys. Res. Commun. 452 945