2. MAPK/ERK Pathway
  3. Raf
  4. PF-04880594

PF-04880594 是一种有效的、选择性的 RAF 抑制剂。 PF-04880594 对野生型和突变型 BRAF 和 CRAF 均有抑制作用。 PF-04880594 具有抗肿瘤活性。

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PF-04880594 Chemical Structure

PF-04880594 Chemical Structure

CAS No. : 1111636-35-1

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规格 价格 是否有货
5 mg ￥2547
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PF-04880594 相关抗体

Top Publications Citing Use of Products

查看 Raf 亚型特异性产品:

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BRaf c-Raf Raf

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity[1].

IC50 & Target

Braf

 

CRAF

 

体外研究
(In Vitro)

PF-04880594 (100 nM; 48 h) causes ERK activation and stimulation of IL-8 release, both of which are blocked by PD-0325901 (HY-10254) treatment[1].

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

PF-04880594 相关抗体:

Western Blot Analysis[1]

Cell Line: HL-60
Concentration: 100 nM alone or in combination with 100 nM PD-0325901
Incubation Time: 48 h
Result: Induced ERK phosphorylation and induced IL-8 production. PD-0325901 treatment blocked the induction.
体内研究
(In Vivo)

PF-04880594 (10 mg/kg) induces ERK phosphorylation and BRAF-CRAF dimerization in multiple epithelial tissues in mice and the induction can be attenuated by PD0325901[1].
PF-04880594 (0-40 mg/kg, twice daily for 3 weeks) induces epithelial hyperplasia in mice and the induction is prevented by PD0325901[1].

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

Animal Model: Nude mice[1]
Dosage: 10 mg/kg alone or in combination with 0.5 mg/kg PD-0325901
Administration: An am and pm dose on day 1 and then an am dose on day 2 approximately 2 hours before the animals were necropsied and the tissues harvested
Result: Induced ERK phosphorylation in urinary bladder, tongue, skin, and esophagus tissues. The induction of ERK phosphorylation was attenuated by cotreatment with 0.5 mg/kg PD0325901.
Animal Model: Nude mice (6–8 weeks old)[1]
Dosage: 10, 20 and 40 mg/kg alone or in combination with 0.1, 0.3, 0.5, 1.0, or 2.5 mg/kg PD-0325901
Administration: Twice daily for 3 weeks
Result: Tissues treated with the RAF inhibitor alone display the microscopic pathology typical of unopposed BRAF inhibition. Hyperplasia in nonglandular stomach epithelium was blocked by PD-0325901.
分子量

394.38

Formula

C19H16F2N8
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-04880594 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:

PF-048805941111636-35-1PF04880594PF 04880594RafRaf kinasesHL-60antitumorERKPD-0325901epithelial hyperplasiaInhibitorinhibitorinhibit

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产品名称：
PF-04880594
目录号：
HY-13810
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