KRC-00715
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models.
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- CAS No.: 2079853-72-6
- Formule: C25H25F3N8O3
- Masse moléculaire:542.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
In Vitro
KRC-00715 exhibits a cytotoxic IC50 of 39 nM, demonstrating its efficacy as a potent c-Met inhibitor[1].
KRC-00715 (8, 40, 200, 1000 nM; 3 h; Hs746T, AGS) inhibits the autophosphorylation of c-Met, indicating that the suppression of c-Met activity significantly contributes to the inhibition of Hs746T cell proliferation[1].
KRC-00715 plays a role in c-Met high-expression cell lines and has an IC50 value of 39 nM in HS746T cells, and inhibits c-Met autophosphorylation in high-expression cell lines; phosphorylation of AKT and ERK[1].
KRC-00715 (30 nM and 300 nM) blocked SNU-5 G1/S more than SNU-1, with numerical values of 72.53 and 64.54 at 30 nM, respectively, at 300 nM, the values are 73.62 and 83.64 respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hs746T
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Concentration:
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Incubation Time:3 days
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Result:Showed the cytotoxic IC50 of HS746 cell line was 39 nm.
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Cell Line:SNU-1, SNU-5, SNU-16, SNU-216, SNU-484, SNU-601, SNU-620, SNU-638, SNU-668, MKN-1, MKN-28, MKN-74, NCI-N87, KATOⅢ, AGS, SNU-719, MKN-45, Hs746T
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Concentration:0.0001-1 μM
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Incubation Time:72 h
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Result:Showed the IC50 value was less than or equal to 10 nM in c-Met overexpressing cell lines and no toxic effect in low-expression cell lines.
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Cell Line:Hs746T, SNU-638, SNU-620, AGS, SNU -1, MKN-1
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Concentration:8, 40, 200, 1000 nM
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Incubation Time:3 h
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Result:Inhibited c-Met autophosphorylation by 70%, inhibited the proliferation of HS746T cells, and inhibited the phosphorylation of Akt and ERK in overexpressed cell lines, with low expression unaffected.
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Cell Line:SNU1, SNU5
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Concentration:30nM, 300nM
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Incubation Time:24 h
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Result:Induced SNU5 arrest in G1/S phase and no cell cycle arrest was found in SNU1. Induced G1/S arrest of c-met overexpressing cells to inhibit cell proliferation.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mouse Hs746T xenograft model[1].
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Dosage:50 mg/kg
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Administration:oral gavage (p.o.)；once daily; 10 days
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Result:Reduced the tumor volume, and the weight of mice did not reduce.
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Flow cytometric DNA-content cell-cycle staining
- BrdU Incorporation Assay
- Patient-Derived Xenograft (PDX)
- Protocol for Cell Cycle
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 2079853-72-6
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Masse moléculaire 542.51
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Formule C25H25F3N8O3
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SMILES
FC(F)(F)C1=C(OCCN2CCOCC2)C=CC(C3=NC(N(CC4OC(C=CC=N5)=C5NC4)N=N6)=C6N=C3)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRC-00715 Related Classifications
HY-164411 Related Classifications
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