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Tocris Bioscience™ CCS 1477

Catalog No. 889210
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Catalog No. Quantity
88-921-0 10 mg
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Catalog No. 88-921-0 Supplier Tocris Bioscience™ Supplier No. 8892/10
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Description

Selective p300/CBP bromodomain inhibitor

CCS 1477 is a selective p300/CBP bromodomain inhibitor. CCS 1477 binds with high affinity to p300 and CBP (Kd values are 1.3 and 1.7 nM, respectively), and with 170/130-fold selectivity compared with BRD4 (Kd = 222 nM). In vitro, CCS 1477 inhibits the proliferation of OPM-2 multiple myeloma cells (GI50 = 5 nM). Also, CCS 1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC-regulated gene expression. In vivo, CCS 1477 significantly improves survival and reduces tumor size in MOLM16 AML and OPM2 myeloma tumors in subcutaneous xenograft models. CCS 1477 is orally bioavailable.

Specifications

Chemical Name or Material (6S)-1-(3,4-Difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-2-piperidinone
CAS 2222941-37-7
Quantity 10 mg
Target Bromodomain Inhibitors
Molecular Formula C30H32F2N4O3
Purity 98%
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