[CAS NO. 1221713-92-3] NPS-1034
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PRODUCTS SPECIFICATIONS [1221713-92-3]
Catalog
SLK-S7669
Brand
Selleck
CAS
1221713-92-3
DESCRIPTION [1221713-92-3]
Overview
| MDL | MFCD29905447 |
|---|---|
| Molecular Weight | 551.54 |
| Molecular Formula | C31H23F2N5O3 |
| SMILES | O=C(C1=C(C)N(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NC=C5C6=CC=CC=C6)=NC=C4)C(F)=C3 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8131 mL | 9.0655 mL | 18.1311 mL |
| 5 mM | 0.3626 mL | 1.8131 mL | 3.6262 mL |
| 10 mM | 0.1813 mL | 0.9066 mL | 1.8131 mL |
| 50 mM | 0.0363 mL | 0.1813 mL | 0.3626 mL |
Description
NPS-1034 is a dual inhibitor with of 48 nM and 10.3 nM, respectively.
In vitro
In HCC827/GR cells, NPS-1034 does not show significant antiproliferative effects, while overcomes gefitinib resistance by inhibiting the phosphorylation of MET, Akt, and Erk. In H820 cells, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively.
In vivo
In SCID mice bearing HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth, and the combination of gefitinib and NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis.
References
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