CP 724,714

CP 724,714 is a selective inhibitor of HER2/ErbB2 with an IC50 value of 10 nM. It demonstrates greater than 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, and c-Met. CP 724,714 has been shown to inhibit the proliferation of ErbB2-amplified cells, including BT474 and SK-BR-3 with IC50 values of 0.25 and 0.95 µM, respectively. It also demonstrates antitumor activity in various human tumor xenograft models. However, CP 724,714 was discontinued from clinical development due to hepatotoxicity caused by its ability to inhibit hepatic efflux transporters at low micromolar concentrations.Formal Name: 2-methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]-acetamide. CAS Number: 383432-38-0. Molecular Formula: C27H27N5O3. Formula Weight: 469.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 3 mg/ml, Ethanol: 2 mg/ml. lambdamax: 243, 317, 347 nm. SMILES: O=C(COC)NC/C=C/C1=CC=C(N=CN=C2NC3=CC=C(OC4=CN=C(C)C=C4)C(C)=C3)C2=C1. InChi Code: InChI=1S/C27H27N5O3/c1-18-13-21(8-11-25(18)35-22-9-6-19(2)29-15-22)32-27-23-14-20(7-10-24(23)30-17-31-27)5-4-12-28-26(33)16-34-3/h4-11,13-15,17H,12,16H2,1-3H3,(H,28,33)(H,30,31,32)/b5-4+. InChi Key: LLVZBTWPGQVVLW-SNAWJCMRSA-N.