PF-04880594
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.
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- CAS No.: 1111636-35-1
- 화학식: C19H16F2N8
- 분자량:394.38
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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Braf |
CRAF |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60
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Concentration:100 nM alone or in combination with 100 nM PD-0325901
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Incubation Time:48 h
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Result:Induced ERK phosphorylation and induced IL-8 production. PD-0325901 treatment blocked the induction.
In Vivo
PF-04880594 (0-40 mg/kg, twice daily for 3 weeks) induces epithelial hyperplasia in mice and the induction is prevented by PD0325901[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice[1]
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Dosage:10 mg/kg alone or in combination with 0.5 mg/kg PD-0325901
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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
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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.
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Animal Model:Nude mice (6–8 weeks old)[1]
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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
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Administration:Twice daily for 3 weeks
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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.
Chemical Information
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CAS No. 1111636-35-1
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분자량 394.38
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화학식 C19H16F2N8
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SMILES
N#CCCNC1=NC=CC(C2=CN(CC(F)F)N=C2C3=CN=C(NC=C4)C4=C3)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-04880594 Related Classifications
HY-13810 Related Classifications
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