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NPS-1034

Catalog No. T6907   CAS 1221713-92-3
Synonyms: NPS 1034, NPS1034

NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

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NPS-1034, CAS 1221713-92-3
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Targets&IC50 Axl:10.3 nM
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. [1] 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. [2]
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. [1] 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. [2]
Kinase Assay Kinase inhibition profile: The in vitro NPS-1034 profile of inhibition of RTKs is analyzed using RTK assay kits according to the manufacturer's protocols.
Cell Research To perform the MTT assay, cells (0.5 × 104/well) are plated in 96-well sterile plastic plates and allowed to attach overnight. Cells are exposed to varying doses of gefitinib, erlotinib, PHA-665752, and NPS-1034 in medium containing 1% FBS. After 72 hours, 15 μL of MTT solution (5 mg/mL) is added to each well and plates are incubated for 4 hours. Crystalline formazan is solubilized with 100 μL of a 10% (w/v) SDS solution for 24 hours. Absorbance at 595 nm is read spectrophotometrically using a microplate reader.(Only for Reference)
Synonyms NPS 1034, NPS1034
Molecular Weight 551.54
Formula C31H23F2N5O3
CAS No. 1221713-92-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 93 mg/mL (168.6 mM)

Ethanol: 4 mg/mL (7.25 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Rho JK, et al. Cancer Res. 2014, 74(1), 253-262. 2. Shin JS, et al. Invest New Drugs. 2014, 32(3), 389-399.

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Keywords

NPS-1034 1221713-92-3 Apoptosis Tyrosine Kinase/Adaptors TAM Receptor c-Met/HGFR Mer Tyro3 NPS 1034 Axl inhibit NPS1034 Inhibitor inhibitor