c-Met-IN-2
c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
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- CAS. Nr.: 1635406-73-3
- Formel: C24H21FN10O
- Molecular Weight:484.49
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
IC50: 0.6 nM (c-Met)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1993 | IC50 |
0.6 nM
Compound: 14-2; Enantiomer-2
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Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
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[PMID: 28411455] |
| NCI-H1993 | IC50 |
0.7 nM
Compound: 14-1; Enantiomer-1
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Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
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[PMID: 28411455] |
| NCI-H1993 | IC50 |
1.1 nM
Compound: 14
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Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
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[PMID: 28411455] |
| SNU-5 | IC50 |
0.6 nM
Compound: 14-2; Enantiomer-2
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Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay
Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay
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[PMID: 28411455] |
| SNU-5 | IC50 |
0.8 nM
Compound: 14-1; Enantiomer-1
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Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay
Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay
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[PMID: 28411455] |
| SNU-5 | IC50 |
2 nM
Compound: 14
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Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay
Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay
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[PMID: 28411455] |
c-Met-IN-2 (Compound 14) is a potent and selective c-Met inhibitor, with an IC50 of 0.6 nM. c-Met-IN-2 also shows weak activity on other kinases, with IC50s of 1075 nM (AxI), 731 nM (RON), 18364 nM (VEGFR2), 5396 nM (c-Kit), 2357 nM (PDGFRa), 17056 nM (c-Src).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1635406-73-3
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Molecular Weight 484.49
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Formel C24H21FN10O
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SMILES
OCCN1N=CC(C2=CN=C3C(N(C(C4=C(F)C=C(N=CC(C5=CN(C)N=C5)=C6)C6=C4)C)N=N3)=N2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
NCI-H1993 cell line and SNU-5 cell line are maintained in RPMI 1640 media and supplemented with 10% fetal bovine serum. NCI-H1993 cells are seeded at 5000 cells/well in 96-well plates and incubated overnight. On the next day, the cells are exposed to various concentrations of c-Met-IN-2 and further cultured for 72 h. After chromogenic reaction with CCK-8, the OD450 (with reference of OD650) is measured using a Flexstation 3 reader. IC50 values are calculated using the GraphPad Prism Software. Each experiment is carried out thrice, each time in duplicate. The SNU-5 cell line assay is operated in a similar procedure as NCI-H1993 assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
The SNU-5 at a density of 6 × 106 tumor cells in 200 μL or NCI-H1993 at a density of 7 × 106 tumor cells in 140 μL are injected s. c. into the right flank of nude mice. Tumor-bearing animals are sorted into groups with similar mean tumor volumes prior to treatment (usually 100-200 mm3 for SNU-5 and 150-250 mm3 for NCI-H1993). The mice are randomly assigned into control and treatment groups (n = 7 (NCI-H1993 model) or n = 6 (SNU-5 model) per group). Control groups are given vehicle alone, and treatment groups receive c-Met-IN-2 as indicated doses via oral administration once daily for 2 weeks in SNU-5 model and oral administration once daily for 3 weeks in NCI-H1993 model, respectively. The sizes of the tumors are measured twice per week using a caliper, and the tumor volume is calculated in cubic millimeter using the formula: V = (A × B2)/2, where A and B is the long and short diameters of the tumor, respectively. Body weights are monitored throughout the study as a gross measure of toxicity/morbidity. Tumor growth inhibition (TGI), expressed in percent (%), is calculated using the formula: 100% × (1-((treatedfinal day-treatedday 0)/(controlfinal day-controlday 0))). Percent tumor regression (PTR), expressed in percent (%), is calculated using the formula: 100% × (treatedday 0-treatedfinal day)/treatedday 0[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
c-Met-IN-2 Related Classifications
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