NPS-1034 is a dual inhibitor ofAXLandMETwithIC₅₀s of 10.3 and 48 nM, respectively.

IC50: 10.3 nM (AXL), 48 nM (MET)^[1]

NPS-1034 is a dual inhibitor of AXL and MET with IC₅₀s of 10.3 and 48 nM, respectively.The expression and activity of AXL is significantly increased in HCC827/ER cells, and NPS-1034 treatment effectively inhibits its tyrosine phosphorylation^[1]. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET (phosphorylated MET), with IC₅₀values of 112.7 and 190.3 nmol, respectively. In contrast, NPS-1034 inhibits AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell viability with IC₅₀values ranging from 1 μmol to more than 10 μmol. MET phosphorylation is dramatically decreased after treatment with NPS-1034 in the MKN45 cells, but not in the MKN28 cells. NPS-1034 inhibits hepatocyte growth factor (HGF)-stimulated MET autophosphorylation (Y1234/1235) in the AGS and MKN1 cell lines with IC₅₀values of<10 and<50 nmol, respectively. hgf-induced met phosphorylation is completely inhibited by 50 nmol nps-1034^[2].

NPS-1034 inhibits tumor proliferation, which highly expresses p-MET. NPS-1034 treatment induces a clear decrease in the vascularization of the tumors. The expression of alpha-smooth muscle actin (α-SMA) is decreased in the tumor sections of mice treated with NPS-1034. NPS-1034-treated mice show virtually no weight loss, indicating that NPS-1034 is generally well tolerated^[2].

551.54

Solid

C₃₁H₂₃F₂N₅O₃

1221713-92-3

Room temperature in continental US; may vary elsewhere.

DMSO : 34 mg/mL(61.65 mM;Need ultrasonic)

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