1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. 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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KRC-00715 Chemical Structure

KRC-00715 Chemical Structure

CAS No. : 2079853-72-6

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Description

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[1].

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.

Cell Cytotoxicity Assay[1]

Cell Line: Hs746T
Concentration:
Incubation Time: 3 days
Result: Showed the cytotoxic IC50 of HS746 cell line was 39 nm.

Cell Cytotoxicity Assay[1]

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
Concentration: 0.0001-1 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: Hs746T, SNU-638, SNU-620, AGS, SNU -1, MKN-1
Concentration: 8, 40, 200, 1000 nM
Incubation Time: 3 h
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.

Cell Cycle Analysis[1]

Cell Line: SNU1, SNU5
Concentration: 30nM, 300nM
Incubation Time: 24 h
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

KRC-00715 (50 mg/kg; p.o.; once daily; 10 days) inhibited tumor volume increased in a nude mouse xenograft HS746T model[1].

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

Animal Model: Nude mouse Hs746T xenograft model[1].
Dosage: 50 mg/kg
Administration: oral gavage (p.o.);once daily; 10 days
Result: Reduced the tumor volume, and the weight of mice did not reduce.
Molecular Weight

542.51

Formula

C25H25F3N8O3

CAS No.
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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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KRC-00715
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