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KRC-00715

KRC-00715
KRC-00715 is an orally effective inhibitor of c-Met, exhibiting high selectivity with an IC50 of 9.0 nM. This compound specifically inhibits the growth of gastric cancer cell lines with high c-Met expression by inducing G1/S phase block, and reduces the activity of downstream signals, including Akt, Erk, and c-Met itself. In the gastric cancer cell line Hs746T, KRC-00715 demonstrates cytotoxicity with an IC50 of 39 nM and selectively inhibits the proliferation of cell lines that overexpress c-Met. Additionally, KRC-00715 decreases tumor size in Hs746T xenograft mouse models.
Catalog No. T200380Cas No. 2079853-72-6

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KRC-00715

Catalog No. T200380Cas No. 2079853-72-6

KRC-00715 is an orally effective inhibitor of c-Met, exhibiting high selectivity with an IC50 of 9.0 nM. This compound specifically inhibits the growth of gastric cancer cell lines with high c-Met expression by inducing G1/S phase block, and reduces the activity of downstream signals, including Akt, Erk, and c-Met itself. In the gastric cancer cell line Hs746T, KRC-00715 demonstrates cytotoxicity with an IC50 of 39 nM and selectively inhibits the proliferation of cell lines that overexpress c-Met. Additionally, KRC-00715 decreases tumor size in Hs746T xenograft mouse models.
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10 mgInquiry10-14 weeks
50 mgInquiry10-14 weeks
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Product Introduction

Bioactivity
Description
KRC-00715 is an orally effective inhibitor of c-Met, exhibiting high selectivity with an IC50 of 9.0 nM. This compound specifically inhibits the growth of gastric cancer cell lines with high c-Met expression by inducing G1/S phase block, and reduces the activity of downstream signals, including Akt, Erk, and c-Met itself. In the gastric cancer cell line Hs746T, KRC-00715 demonstrates cytotoxicity with an IC50 of 39 nM and selectively inhibits the proliferation of cell lines that overexpress c-Met. Additionally, KRC-00715 decreases tumor size in Hs746T xenograft mouse models.
In vitro
KRC-00715, exhibiting an IC 50 of 39 nM, serves as an effective inhibitor of c-Met. This compound notably inhibits c-Met autophosphorylation, primarily contributing to the suppression of cell proliferation. KRC-00715 demonstrates activity in c-Met highly-expressed cell lines, particularly achieving an IC 50 of 39 nM in Hs746T cells where it also hinders the phosphorylation of c-Met, Akt, and Erk in high-expression cell lines. Additionally, the blocking effect of KRC-00715 on SNU-5 G1/S cell cycle progression is more pronounced than in SNU-1, with doses of 30 nM and 300 nM yielding prominent inhibitory percentages of 72.53 & 64.54 and 73.62 & 83.64, respectively.
In vivo
KRC-00715, administered at a dosage of 50mg/kg via oral gavage (p.o.) once daily for a period of 10 days, effectively inhibited the increase in tumor volume of Hs746T xenografts in nude mice.
Chemical Properties
Molecular Weight542.51
FormulaC25H25F3N8O3
Cas No.2079853-72-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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