2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. KRC-00715

KRC-00715 是口服有效的 c-Met 的抑制剂 (IC50为 9.0 nM)，具有高度选择性。KRC-00715 在胃癌细胞中通过诱导 G1/S 阻滞来特异性抑制 c-Met 高表达细胞系的生长，降低了下游信号包括 Akt 和 Erk 以及 c-Met 活性。KRC-00715 在胃癌细胞系 Hs746 中的细胞毒性 IC50 为 39 nM，且只抑制高表达 c-Met 细胞系的增殖。KRC-00715 减小 Hs746T 异种移植小鼠模型的肿瘤大小。

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KRC-00715 Chemical Structure

KRC-00715 Chemical Structure

CAS No. : 2079853-72-6

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KRC-00715 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

KRC-00715 具有细胞毒性 IC50 为 39 nM，是优良的 c-Met 抑制剂[1]。
KRC-00715 (8，40，200，1000 nM; 3 h; Hs746T，AGS) 抑制 c-Met 自磷酸化，c-Met 活性的抑制主要有助于抑制细胞的增殖[1]。
KRC-00715 在 c-Met 高表达细胞系中发挥作用且在 Hs746T 细胞中 IC50 值为 39 nM，并且抑制高表达细胞系中 c-Met 自磷酸化，Akt 和 Erk 的磷酸化[1]。
KRC-00715 (30 nM 和 300 nM) 对 SNU-5 G1/S 的阻滞效果比 SNU-1 更为明显，30 nM 条件下的数值为 72.53 和 64.54，300 nM 的条件下数值为 73.62 和 83.64[1]。

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

KRC-00715 相关抗体:

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.
体内研究
(In Vivo)

KRC-00715 (50mg/kg; Oral gavage (p.o.); 每日一次; 10 天) 抑制在裸鼠异种移植 Hs746T 肿瘤体积增加[1]。

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.
分子量

542.51

Formula

C25H25F3N8O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

KRC-00715 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

KRC-007152079853-72-6KRC00715KRC 00715c-Met/HGFRG1/SGastric cancer cellsInhibitorinhibitorinhibit

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