CPI-203

(+)-JQ1 (Cay-11187) binds to the acetyl-lysine recognition pocket of bromodomains 1 and 2 on BRD4 with Kd values of ~50 and 90 nM, respectively. This displaces BRD4 from nuclear chromatin in cells, inducing differentiation and growth arrest in midline carcinoma cells. CPI-203 is a primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration. It is comparable or superior to (+)-JQ1 in inhibiting BRD4 binding and action in vitro or in cells. CPI-203 arrests the growth of leukemic T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice.Formal Name: (6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide. CAS Number: 1446144-04-2. Molecular Formula: C19H18ClN5OS. Formula Weight: 399.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 25 mg/ml, Ethanol: 20 mg/ml. lambdamax: 255 nm. SMILES: ClC1=CC=C(C=C1)C2=N[C@@H](CC(N)=O)C3=NN=C(C)N3C4=C2C(C)=C(C)S4. InChi Code: InChI=1S/C19H18ClN5OS/c1-9-10(2)27-19-16(9)17(12-4-6-13(20)7-5-12)22-14(8-15(21)26)18-24-23-11(3)25(18)19/h4-7,14H,8H2,1-3H3,(H2,21,26)/t14-/m0/s1. InChi Key: QECMENZMDBOLDR-AWEZNQCLSA-N.