MK-1775

MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM). It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint. In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.Formal Name: 1,2-dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-(2-propen-1-yl)-3H-pyrazolo[3,4-d]pyrimidin-3-one. CAS Number: 955365-80-7. Synonyms: AZD 1775. Molecular Formula: C27H32N8O2. Formula Weight: 500.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: ~80 mg/ml. lambdamax: 229, 257, 292 nm. SMILES: CN1CCN(C2=CC=C(NC3=NC=C(C(N(CC=C)N4C5=CC=CC(C(C)(O)C)=N5)=O)C4=N3)C=C2)CC1. InChi Code: InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31). InChi Key: BKWJAKQVGHWELA-UHFFFAOYSA-N.