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

PF-04880594 Chemical Structure

CAS No. : 1111636-35-1

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Based on 1 publication(s) in Google Scholar

PF-04880594 Related Antibodies

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BRaf c-Raf Raf

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Description

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

 

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.

PF-04880594 Related Antibodies

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.
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].

MedChemExpress (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.
Molecular Weight

394.38

Formula

C19H16F2N8
CAS No.
SMILES

N#CCCNC1=NC=CC(C2=CN(CC(F)F)N=C2C3=CN=C(NC=C4)C4=C3)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-04880594 Related Classifications

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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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