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。
| 生物活性 | PF-04880594 is a potent and selectiveRAFinhibitor. PF-04880594 inhibits both wild-type and mutantBRAFand CRAF. PF-04880594 shows antitumor activity[1]. |
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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].
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. |
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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].
| 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. |
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| 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. |
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