Cat PKISU 11274 005 SU 11274 15875 Gaither

Cat # PKI-SU 11274 -005 SU 11274 15875 Gaither Drive Gaithersburg, MD 20877 FAX. 301 -560 -4919 Size: 5. 0 mg M. W. =568. 09 Batch No. : 1 A/20050309 TEL. 301 -330 -5966 Email: info@signagenlabs. com Web: www. signagenlabs. com This product is for laboratory research ONLY and not for diagnostic use Description: SU 11274 is a ATP-competitive small molecule inhibitor of the catalytic activity of Met which exhibited a selectivity for Met enzyme versus a panel of other tyrosine kinases (Met IC 50 = 0. 02 µM, Flk IC 50 = 1. 3, EGFR IC 50 = >100 µM, PDGFßR IC 50 = >20 µM, Tie 2 IC 50 = >100 µM, c-src IC 50 = >10 µM, cdk 2 IC 50 = >10 µM, FGFR-1 IC 50 = 9. 7 µM). Inhibition of the Met kinase activity by SU 11274 led to timeand dose-dependent reduced cell growth and induced G 1 cell cycle arrest and apoptosis. Physical and Chemical Properties: Molecular Formula: C 28 H 30 CIN 5 O 4 S Molecular Weight: 568. 09 Physical appearance: orange solid powder Molecular Structure: Solubility: DMSO 10 mg/ml at 60 °C. Stability and Solubility Advice: 2006 Signa. Gen Laboratories Some solutions can be difficult to obtain and can be encouraged by rapid stirring, sonication or gentle warming (in a 45 -60°C water bath). Information concerning product stability, particularly in solution, has rarely been reported and in most cases we can only offer a general guide. Our standard recommendations are: SOLIDS: Provided storage is as stated on the product label and the vial is kept tightly sealed, the product can be stored for up to 6 months from date of receipt. SOLUTIONS: We recommend that stock solutions, once prepared, are stored aliquoted in tightly sealed vials at -20 0 C or below and used within 1 month. Wherever possible solutions should be made up and stored on the same day. References: 1. 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. 2. 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 SU 11274 exhibits a selective inhibition pattern toward different receptor mutated variants. " Oncogene. 23(31): 5387 -93. 3. 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 SU 11274 and small interfering RNA in non-small cell lung cancer" Cancer Res. , 65(4): 1479 -88 4. 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.