TGR-1202

TGR-1202 is an inhibitor of PI3K p110delta (IC50 = 22 nM). It is selective for p110delta over p110alpha, p110beta, and p110gamma (IC50s = >10,000, 1,116, and 1,065 nM, respectively). TGR-1202 induces apoptosis in patient-derived chronic lymphocytic leukemia lymphocytes when used at concentrations ranging from 0.1 to 25.6 µM. In vivo, TGR-1202 (150 mg/kg) reduces tumor growth in a MOLT-4 T cell acute lymphoblastic leukemia (T-ALL) mouse xenograft model.Formal Name: 2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-4H-1-benzopyran-4-one. CAS Number: 1532533-67-7. Synonyms: RP 5264, Umbralisib. Molecular Formula: C31H24F3N5O3. Formula Weight: 571.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml. lambdamax: 232, 291 nm. SMILES: C[C@@H](C1=C(C2=CC(F)=CC=C2)C(C3=CC(F)=CC=C3O1)=O)N4N=C(C5=CC=C(OC(C)C)C(F)=C5)C6=C(N)N=CN=C46. InChi Code: InChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1. InChi Key: IUVCFHHAEHNCFT-INIZCTEOSA-N.