MET protein kinase inhibitor SU 11274, 1 mg

SU11274 is a ATP-competitive small molecule inhibitor of the catalytic activity of Met kinase which exhibited a selectivity for Met enzyme versus a panel of other tyrosine kinases (Met IC50 = 0.02 µM, Flk IC50 = 1.3, EGFRI C50 = >100 µM, PDGFRβ IC50 = >20 µM, Tie2 IC50 = >100 µM, c-src IC50 = >10 µM, cdk2 IC50 = >10 µM,  FGFR-1 IC50 = 9.7 µM). Inhibition of the Met kinase activity by SU11274 led to time- and dose-dependent reduced cell growth and induced G1 cell cycle arrest and apoptosis.

Formula: C28H30CIN5O4S, Molecular Weight:  568.09 g/mol, Purity: 98 %, Appearance:  Orange powder, Solubility:  Soluble in DMSO 10 mg/ml at 60 °C. CAS Number: 658084-23-2

Product specific literature references:

Sattler M, Pride YB, Ma P, Gramlich JL, Chu SC, Quinnan LA, Shirazian S, Liang C, Podar K, Christensen JG, Salgia R. (2003) " A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase." Cancer Res. 63(17):5462-9.

Berthou S, Aebersold DM, Schmidt LS, Stroka D, Heigl C, Streit B, Stalder D, Gruber G, Liang C, Howlett AR, Candinas D, Greiner RH, Lipson KE, Zimmer Y. (2004) " The Met kinase inhibitor SU11274 exhibits a selective inhibition pattern toward different receptor mutated variants." Oncogene.23(31):5387-93.

Ma PC, Jagadeeswaran R, Jagadeesh S, Tretiakova MS, Nallasura V, Fox EA, Hansen M, Schaefer E, Naoki K, Lader A, Richards W, Sugarbaker D, Husain AN, Christensen JG, Salgia R. (2005) " Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer" Cancer Res., 65(4):1479-88

Puri N, Ahmed S, Janamanchi V, Tretiakova M, Zumba O, Krausz T, Jagadeeswaran R, Salgia R. (2007) " c-Met is a potentially new therapeutic target for treatment of human melanoma." Clin Cancer Res;13(7):2246-53.

Product Citations:

Toiyama Y, Yasuda H, Saigusa S, Matushita K, Fujikawa H, Tanaka K, Mohri Y, Inoue Y, Goel A, Kusunoki M. (2012) "Co-expression of hepatocyte growth factor and c-Met predicts peritoneal dissemination established by autocrine hepatocyte growth factor/c-Met signaling in gastric cancer." Int J Cancer. 130(12):2912-21.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.