TAS 120

TAS 120 is an orally bioavailable inhibitor of fibroblast growth factor receptors (FGFRs) that irreversibly inhibits all four FGFR subtypes at nanomolar concentrations. It prevents phosphorylation of FGFRs and impedes downstream signaling pathways in cells. TAS 120 blocks the proliferation of human cancer cell lines with FGFR gene abnormalities but does not alter the growth of cell lines with wild-type FGFR. It inhibits FGFR phosphorylation in tumors and tumor growth in human xenograft mouse models in a dose-dependent manner.Formal Name: 1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one. CAS Number: 1448169-71-8. Molecular Formula: C22H22N6O3. Formula Weight: 418.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml, DMSO: 1 mg/ml, Ethanol: 1 mg/ml. lambdamax: 210, 301 nm. SMILES: COC1=CC(OC)=CC(C#CC2=NN([C@H]3CCN(C(C=C)=O)C3)C4=NC=NC(N)=C42)=C1. InChi Code: InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1. InChi Key: KEIPNCCJPRMIAX-HNNXBMFYSA-N.