NPS-1034
Based on 1 publication(s) in Google Scholar
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.
- Purity : 98.0%
- CAS No.: 1221713-92-3
- Formula: C31H23F2N5O3
- Molecular Weight:551.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NPS-1034
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Biological Activity
Description
IC50 & Target
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Axl |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1221713-92-3
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Appearance Solid
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Molecular Weight 551.54
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Formula C31H23F2N5O3
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Medicina (Kaunas)
NPS-1034 Induce Cell Death with Suppression of TNFR1/NF-κB Signaling in Testicular Cancer. [Abstract]2022 Feb 27;58(3):355. PMID: 35334531
Solvent & Solubility
In Vitro:
DMSO : 34 mg/mL (61.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Rho JK, et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62. [Content Brief]
[2]. Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8131 mL | 9.0655 mL | 18.1311 mL | 45.3276 mL |
| 5 mM | 0.3626 mL | 1.8131 mL | 3.6262 mL | 9.0655 mL | |
| 10 mM | 0.1813 mL | 0.9066 mL | 1.8131 mL | 4.5328 mL | |
| 15 mM | 0.1209 mL | 0.6044 mL | 1.2087 mL | 3.0218 mL | |
| 20 mM | 0.0907 mL | 0.4533 mL | 0.9066 mL | 2.2664 mL | |
| 25 mM | 0.0725 mL | 0.3626 mL | 0.7252 mL | 1.8131 mL | |
| 30 mM | 0.0604 mL | 0.3022 mL | 0.6044 mL | 1.5109 mL | |
| 40 mM | 0.0453 mL | 0.2266 mL | 0.4533 mL | 1.1332 mL | |
| 50 mM | 0.0363 mL | 0.1813 mL | 0.3626 mL | 0.9066 mL | |
| 60 mM | 0.0302 mL | 0.1511 mL | 0.3022 mL | 0.7555 mL |
NPS-1034 Related Classifications
HY-100509 Related Classifications
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