PF-04880594

Modify Date: 2024-01-09 19:23:35

PF-04880594 Structure
PF-04880594 structure
 Common Name PF-04880594
CAS Number 1111636-35-1 Molecular Weight 394.381
Density 1.5±0.1 g/cm3 Boiling Point 666.3±65.0 °C at 760 mmHg
Molecular Formula C19H16F2N8 Melting Point N/A
MSDS USA Flash Point 356.8±34.3 °C
Symbol GHS07
GHS07		 Signal Word Warning

 Use of 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[1].

 Names

Name 3-((4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl)amino)propanenitrile
Synonym More Synonyms

 PF-04880594 Biological Activity

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].
Related Catalog
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]. 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]. 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.
References

[1]. Torti VR, et al. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. Mol Cancer Ther. 2012 Oct;11(10):2274-83.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 666.3±65.0 °C at 760 mmHg
Molecular Formula C19H16F2N8
Molecular Weight 394.381
Flash Point 356.8±34.3 °C
Exact Mass 394.146606
PSA 108.10000
LogP 1.24
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.710
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P280-P304 + P340 + P312-P305 + P351 + P338-P337 + P313
RIDADR NONH for all modes of transport

 Synonyms

PF-04880594
3-[[4-[1-(2,2-Difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]propanenitrile
PF-04880594/PF04880594
3-({4-[1-(2,2-Difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyrimidinyl}amino)propanenitrile
Propanenitrile, 3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]-
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Chemsrc provides PF-04880594(CAS#:1111636-35-1) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of PF-04880594 are included as well.>> amp version: PF-04880594

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