1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. PF-04217903 phenolsulfonate

PF-04217903 phenolsulfonate 是一种高效的 ATP 竞争性 c-Met 激酶抑制剂,Ki 为 4.8 nM。PF-04217903 phenolsulfonate 相对于 208 个激酶显示出 1000 倍以上的选择性。具有抗血管生成特性。

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PF-04217903 phenolsulfonate Chemical Structure

PF-04217903 phenolsulfonate Chemical Structure

CAS No. : 1159490-85-3

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PF-04217903 phenolsulfonate 的其他形式现货产品:

Customer Review

Other Forms of PF-04217903 phenolsulfonate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties[1][2].

IC50 & Target

Ki: 4.8 nM (human c-Met)[1]

体外研究
(In Vitro)

PF-04217903 phenolsulfonate (0.1-10000 nM; 48-72 hours) inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC50 values of 12 and 30 nM, respectively[1].
PF-04217903 phenolsulfonate (1.5-3333 nM; 48 hours) induces apoptosis of GTL-16 cells (IC50=31 nM)[1].
PF-04217903 phenolsulfonate also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC50 values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC50=7-12.5 nM)[1].
PF-04217903 phenolsulfonate displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively. PF-04217903 phenolsulfonate has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM[3].

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

Cell Viability Assay[1]

Cell Line: GTL-16, H1993 cells
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 48-72 hours
Result: Inhibited proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC50 values of 12 and 30 nM, respectively.

Apoptosis Analysis[1]

Cell Line: GTL-16 cells
Concentration: 1.5-3333 nM
Incubation Time: 48 hours
Result: Induced apoptosis of GTL-16 cells.
体内研究
(In Vivo)

PF-04217903 phenolsulfonate (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors[1].
PF-04217903 phenolsulfonate (5-50 mg/kg, p.o.; once daily for 3 days) dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels. PF-04217903 phenolsulfonate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 phenolsulfonate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors[1].

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

Animal Model: Female nu/nu mice (GTL-16 xenograft model)[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: Oral; daily for 16 days
Result: Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.
Clinical Trial
分子量

546.56

Formula

C25H22N8O5S

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

PF-04217903 phenolsulfonate 相关分类

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  • 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.

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PF-04217903 phenolsulfonate
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HY-12017B
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