NPS-1034

SKU: orb1300357

Description

NPS-1034 is a potent small molecule inhibitor targeting both Met and Axl kinases, exhibiting IC50 values of 48 nM and 10.3 nM, respectively. It is a valuable research tool for studying oncogenic signaling in vitro and has shown efficacy in reducing tumor growth in preclinical in vivo cancer models.

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience, Signal Transduction

Key Properties

• CAS Number: 1221713-92-3
• MW: 551.54
• Purity: 98.48% (May vary between batches)
• Formula: C₃₁H₂₃F₂N₅O₃
• SMILES: Cc1c(C(=O)Nc2ccc(Oc3ccnc4[nH]cc(-c5ccccc5)c34)c(F)c2)c(=O)n(-c2ccc(F)cc2)n1C
• Target: AXL,TAM Receptor,Apoptosis,c-Met/HGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (168.62 mM);Ethanol:4 mg/mL (7.25 mM)

Bioactivity

• Target IC50:
  Axl:10.3 nM
• 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.
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cMet, c-Met, cMet/HGFR, c-Met/HGFR, Axl, AXL, Apoptosis, Inhibitor, HGFR, Met, inhibit, NPS1034, NPS-1034, NPS 1034, Mer, Tyro3, TAM Receptor, TAMReceptor

Compound Identifiers

PubChem CID

46194178