NPS-1034

Catalog No.S7669 Batch:S766901

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Technical Data

Formula

C31H23F2N5O3
Molecular Weight 551.54 CAS No. 1221713-92-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (181.31 mM)
Ethanol 4 mg/mL (7.25 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
PBS
11.0mg/ml
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Targets
Axl [1]
(Cell-free assay)		 Met [1]
(Cell-free assay)
10.3 nM 48 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]

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • Cell lines

    HCC827/GR, HCC-78 and H820 cells

  • Concentrations

    ~5 μM

  • Incubation Time

    72 h

  • Method

    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.
Animal Study:[1]
  • Animal Models

    SCID mice bearing HCC827/GR tumor xenografts

  • Dosages

    10 mg/kg, 5 days a week

  • Administration

    p.o.

Selleck's NPS-1034 has been cited by 3 publications

Inhibition of AXL receptor tyrosine kinase enhances brown adipose tissue functionality in mice [ Nat Commun, 2023, 14(1):4162] PubMed: 37443109
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy [ J Med Chem, 2021, 64(6):3165-3184] PubMed: 33683117
Contribution of p53 in sensitivity to EGFR tyrosine kinase inhibitors in non-small cell lung cancer [ Sci Rep, 2021, 11(1):19667] PubMed: 34608255

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.