Cat # PKI-SU11274-005 SU 11274 Size: 5.0 mg M.W.=568.09 Batch No.: 1A/20050309 15875 Gaither Drive Gaithersburg, MD 20877 FAX. 301-560-4919 TEL. 301-330-5966.

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Cat # PKI-SU SU Size: 5.0 mg M.W.= Batch No.: 1A/ Gaither Drive Gaithersburg, MD FAX TEL Web: Description: SU11274 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 IC50 = 0.02 µM, Flk IC50 = 1.3, EGFR IC50 = >100 µM, PDGFßR 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. Physical and Chemical Properties: Molecular Formula: C28H30CIN5O4S Molecular Weight: Physical appearance: orange solid powder Molecular Structure: Solubility: DMSO 10 mg/ml at 60 °C. Stability and Solubility Advice: 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 C or below and used within 1 month. Wherever possible solutions should be made up and stored on the same day. This product is for laboratory research ONLY and not for diagnostic use  2006 SignaGen Laboratories 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): 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): 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): 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): Storage: Upon arrival store this product at 4 0 C. For long term, store the product at C. Product shipped at ambient temperature.