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NPS-1034

Chemical Structure : NPS-1034

CAS No.: 1221713-92-3

NPS-1034 (NPS1034)

Catalog No.: PC-20334Not For Human Use, Lab Use Only.

NPS-1034 (NPS1034) is a potent, dual MET and AXL inhibitor with IC50 of 48 and 10.3 nM, respectively.

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Biological Activity

NPS-1034 (NPS1034) is a potent, dual MET and AXL inhibitor with IC50 of 48 and 10.3 nM, respectively.
NPS-1034 also inhibits other kinases, such as FLT3, KIT, and DDR1.
Combined treatment with NPS-1034 and gefitinib overcomes the drug resistance caused by MET gene amplification.
Addition of NPS-1034 to gefitinib overcomes acquired resistance to gefitinib in a xenograft model.
Addition of NPS-1034 to erlotinib overcomes AXL-mediated drug resistance.
NPS-1034 treatment enhances sensitivity to EGFR-TKIs in H820 cells.
NPS-1034 inhibits ROS1 activity and cell proliferation in HCC78 cells.

Physicochemical Properties

M.Wt 551.55
Formula C31H23F2N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-fluorophenyl)-N-[3-fluoro-4-[(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dihydro-1,5-dimethyl-3-oxo-1H-pyrazole-4-carboxamide

References

1. Rho JK, et al. Cancer Res. 2014 Jan 1;74(1):253-62.

2. Shin JS, et al. Invest New Drugs. 2014 Jun;32(3):389-99.

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