Chemical Property of 6-chloro-9-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-9H-purin-2-amine
Chemical Property:
- Melting Point:192-193℃
- Boiling Point:588.5±60.0 °C(Predicted)
- PKA:6.07±0.40(Predicted)
- PSA：91.74000
- Density:1.50
- LogP:2.71180
- Storage Temp.:-20°C
- Solubility.:Soluble in DMSO (>25 mg/ml)
- XLogP3:1.9
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:3
- Exact Mass:318.0995868
- Heavy Atom Count:22
- Complexity:388
- Purity/Quality:
-
99%, *data from raw suppliers
BIIB 021 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=CN=C(C(=C1OC)C)CN2C=NC3=C2N=C(N=C3Cl)N
- Recent ClinicalTrials:Once or Twice Daily Administration of BIIB021 to Subjects With Advanced Solid Tumors
- Recent EU Clinical Trials:Phase 2a, open-label, randomized, noncomparative study of BIIB021 in combination with exemestane in women with hormone receptor-positive, advanced metatatic breast cancer who have progressed on a nonsteroidal aromatase inhibitor
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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
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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.
