Su11274 Inhibitor CAS No. 658084-23-2

Cat. No.	Name	Size	Price
KI0107	Su11274	2 mg	$112
	Su11274	5 mg	$192
	Su11274	25 mg	$752
	Su11274	200 mg	$3472

Chemical Characteristic

Product Name	Su11274
CAS No.	658084-23-2
Molecular Weight	568.09
Formula	C₂₈H₃₀CIN₅O₄S
Chemical Name	N-(3-Chlorophenyl)-N-methyl-3-[[3,5-dimethyl-4-[(4-methylpiperazin-1-yl)carbonyl]-1H-pyrrol-2-yl]methylene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
Smiles	N1C(=O)/C(=C/c2[nH]c(c(c2C)C(=O)N2CCN(CC2)C)C)/c2cc(ccc12)S(=O)(=O)N(C)c1cc(ccc1)Cl
Chemical Structure
Documents	HPLC MS COA

Biological activities

Su11274 is a ATP-competitive c-Met specific inhibitor. The IC50 of Su11274 is 20 nM against c-Met while Su11274 inhibits Flk and FGFR-1 with IC50 of 1.3 and 9.7 µM, respectively. The IC50 of SU11274 for PDGFβR inhibition is more than 1000-fold higher, and that for FGFR-1 inhibition about 500 times higher than the IC50 of SU11274 for inhibition of Met. SU11274 inhibits BaF3.TPR-MET cell growth in a dose-dependent manner with an IC50 of less than 3 µM. SU11274 completely blocks cell growth in the absence of interleukin 3 in BaF3.TPR-MET. Interleukin 3 completely rescues the BaF3.TPR-MET cells from SU11274-dependent growth inhibition. Migration of BaF3.TPR-MET cells is inhibited with 1 µM SU11274 (44.8 % inhibition of the cell migration) and with 5 µM SU11274 (about 80% inhibition of the cell migration), compared with DMSO-treated cells. In cellular assays, SU11274 demonstrates inhibition of HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with a mean IC50 of 1??.5 µM. SU11274 specifically inhibits TPR-MET-induced tyrosine phosphorylation relative to BCR-ABL. SU11274 inhibits autophosphorylation at Tyr361/365/366 (autophosphorylation site), Tyr480 (Grb2 binding site), and Tyr496. SU11274 induces cell cycle arrest as well as apoptosis, and both events in combination are likely to contribute to the reduced cell growth of SU11274-treated TPR-MET-transformed cells.^[1] SU11274 inhibits hepatocellular carcinoma (HCC) cell growth by inhibiting the activation of c-Met. ^[2] Ovarian carcinoma cells treated with SU11274 demonstrates significantly decreased cell motility and invasion compared to untreated cells. ^[3] SU11274 inhibits cell viability in c-Met-expressing NSCLC cells. SU11274 also abrogates hepatocyte growth factor??nduced phosphorylation of c-Met and its downstream signaling.^[4] SU11274 significantly suppresses cell survival and proliferation as well as enhance the radiosensitivity of DU145 cells.^[5]

References

[1] Sattler M, et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res. 2003, 63(17): 5462-5469. [2] Inagaki Y, et al. Effect of c-Met inhibitor SU11274 on hepatocellular carcinoma cell growth.Biosci Trends. 2011, 5(2): 52-56. [3] Koon EC, et al. Effect of a c-Met-specific, ATP-competitive small-molecule inhibitor SU11274 on human ovarian carcinoma cell growth, motility, and invasion.Int J Gynecol Cancer. 2008, 18(5): 976-984. [4] Ma PC, et al. 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. 2005, 65(4): 1479-1488. [5] Yu H, et al. c-Met inhibitor SU11274 enhances the response of the prostate cancer cell line DU145 to ionizing radiation. Biochem Biophys Res Commun. 2012, 427(3): 659-665.

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