1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. TAM Receptor
    c-Met/HGFR
    Apoptosis
  3. NPS-1034

NPS-1034 

Cat. No.: HY-100509 Purity: >98.0%
Handling Instructions

NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.

For research use only. We do not sell to patients.

NPS-1034 Chemical Structure

NPS-1034 Chemical Structure

CAS No. : 1221713-92-3

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Based on 1 publication(s) in Google Scholar

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Description

NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.

IC50 & Target

IC50: 10.3 nM (AXL), 48 nM (MET)[1]

In Vitro

NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.The expression and activity of AXL is significantly increased in HCC827/ER cells, and NPS-1034 treatment effectively inhibits its tyrosine phosphorylation[1]. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET (phosphorylated MET), with IC50 values of 112.7 and 190.3 nmol, respectively. In contrast, NPS-1034 inhibits AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell viability with IC50 values ranging from 1 μmol to more than 10 μmol. MET phosphorylation is dramatically decreased after treatment with NPS-1034 in the MKN45 cells, but not in the MKN28 cells. NPS-1034 inhibits hepatocyte growth factor (HGF)-stimulated MET autophosphorylation (Y1234/1235) in the AGS and MKN1 cell lines with IC50 values of <10 and <50 nmol, respectively. HGF-induced MET phosphorylation is completely inhibited by 50 nmol NPS-1034[2].

In Vivo

NPS-1034 inhibits tumor proliferation, which highly expresses p-MET. NPS-1034 treatment induces a clear decrease in the vascularization of the tumors. The expression of alpha-smooth muscle actin (α-SMA) is decreased in the tumor sections of mice treated with NPS-1034. NPS-1034-treated mice show virtually no weight loss, indicating that NPS-1034 is generally well tolerated[2].

Molecular Weight

551.54

Formula

C₃₁H₂₃F₂N₅O₃

CAS No.

1221713-92-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 34 mg/mL (61.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female severe combined immunodeficiency (SCID) mice (17 to 20 g, 6 weeks of age) are used. Tumors are grown by implanting 5×106 cells in Matrigel into the mouse flanks. Treatment of 5 mice per group is started when the tumors have reached a volume of 50 to 100 mm3 with vehicle control or NPS-1034 (10 mg/kg, 5 days a week). NPS-1034 is administered orally. Treatment is stopped at the indicated day and mice are followed-up for tumor recurrence. To measure tumor size, the length (L) and width (W) of the tumor are measured with calipers, and tumor volume (TV) is calculated as TV=(L×W2)/2. Immunohistochemical staining is performed using a specific primary antibody, the EnVision Plus staining kit, and the APO-Direct terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling assay kit, according to the suppliers' instructions. Quantitative analysis of section staining is performed by counting immunopositive cells in 5 arbitrarily selected fields at ×40 magnification[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

NPS-1034NPS1034NPS 1034TAM Receptorc-Met/HGFRApoptosisTyro3AxlMerInhibitorinhibitorinhibit

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