XL147

XL147 is an inhibitor of class I PI3Ks (IC50s = 0.039, 0.036, 0.023, and 0.383 µM for p110alpha, -delta, -gamma, and -beta, respectively). It is selective for class I PI3Ks over the class III PI3K vacuolar protein sorting 34 (Vps34, IC50 = 6.974 µM), as well as DNA protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC50s = 4.75 and >15 µM, respectively). XL147 inhibits the proliferation of MCF-7 breast and PC3 prostate cancer cells (IC50s = 9.669 and 16.492 µM, respectively). It reduces tumor growth in a BT474 breast cancer mouse xenograft model when administered alone or in combination with trastuzumab or lapatinib (Cay-11493).Formal Name: 2-amino-N-[3-[[[3-[(2-chloro-5-methoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-2-methyl-propanamide. CAS Number: 934526-89-3. Synonyms: Pilaralisib, SAR245408. Molecular Formula: C25H25ClN6O4S. Formula Weight: 541.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:30): 0.03 mg/ml. lambdamax: 237, 272, 369 nm. SMILES: COC1=CC(NC2=NC3=CC=CC=C3N=C2NS(C4=CC=CC(NC(C(C)(N)C)=O)=C4)(=O)=O)=C(Cl)C=C1. InChi Code: InChI=1S/C25H25ClN6O4S/c1-25(2,27)24(33)28-15-7-6-8-17(13-15)37(34,35)32-23-22(29-19-9-4-5-10-20(19)30-23)31-21-14-16(36-3)11-12-18(21)26/h4-14H,27H2,1-3H3,(H,28,33)(H,29,31)(H,30,32). InChi Key: QINPEPAQOBZPOF-UHFFFAOYSA-N.