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.
For research use only. We do not sell to patients.
- CAS No.: 1111636-35-1
- Formula: C19H16F2N8
- Molecular Weight:394.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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. Further protocols information, click here.
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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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Molecular Weight 394.38
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-04880594 Related Classifications
HY-13810 Related Classifications
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