1111636-35-1

1111636-35-1 structure

Name: PF-04880594
Chemical 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
CAS Number: 1111636-35-1
Molecular Formula: C₁₉H₁₆F₂N₈
Molecular Weight: 394.381
Catalog: Signaling Pathways MAPK/ERK Pathway Raf
Create Date: 2016-04-24 20:10:57
Modify Date: 2024-01-09 19:23:35
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].

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
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]-

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	Research Areas >> Cancer Signaling Pathways >> MAPK/ERK Pathway >> Raf
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.

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℃

Symbol	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

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