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编 号：F038510
分子式：C19H16F2N8
分子量：394.38
分子式：C19H16F2N8
分子量：394.38
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CAS No: 1111636-35-1
产品详情
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.
体内研究：
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.PF-04880594 (0-40 mg/kg, twice daily for 3 weeks) induces epithelial hyperplasia in mice and the induction is prevented by PD0325901.Animal Model:Nude mice
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)
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.
体外研究：
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.
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.
体内研究：
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.PF-04880594 (0-40 mg/kg, twice daily for 3 weeks) induces epithelial hyperplasia in mice and the induction is prevented by PD0325901.Animal Model:Nude mice
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)
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.
体外研究：
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.
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