CPI-637

CPI-637 is a potent and selective CBP/ EP300 bromodomain inhibitor. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM). CPI-637 demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM). CPI-637 inhibits MYC expression in AMO-1 cells (EC50 = 0.60 μM). CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology.

Product information

CAS Number: 1884712-47-3

Molecular Weight: 386.45

Formula: C22H22N6O

Synonym:

CPI-637

CPI 637

CPI637

Chemical Name:  (R)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one

Smiles: C[C@@H]1CC(=O)NC2=CC=CC(=C2N1)C1C=C2C(=NN(C)C2=CC=1)C1C=NN(C)C=1

InChiKey: BFTKDWYIRJGJCA-CYBMUJFWSA-N

InChi: InChI=1S/C22H22N6O/c1-13-9-20(29)25-18-6-4-5-16(22(18)24-13)14-7-8-19-17(10-14)21(26-28(19)3)15-11-23-27(2)12-15/h4-8,10-13,24H,9H2,1-3H3,(H,25,29)/t13-/m1/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Taylor AM, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6.

Products are for research use only. Not for human use.