PF-04965842

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-04965842 (Abrocitinib, PF04965842) 是一种有效的、选择性的、口服生物可利用的 JAK1 抑制剂，IC50 为 29 nM。

PF-04965842 (Abrocitinib, PF04965842) is a potent, selective, orally bioavailable JAK1 inhibitor with IC50 of 29 nM; exhibits good selective inhibition profile for JAK1 versus other JAK family enzymes (IC50=803/>10,000/1250 nM for JAK2/JAK3/TYK2, respectively); demonstrates efficacy in a rat adjuvant-induced arthritis (rAIA) model.Dermatitis Phase 3 Clinical(In Vitro):Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively.(In Vivo):Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model.

Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively.

Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model. Animal Model:Female Lewis rats (8?10 weeks old)Dosage:5, 15, 50 mg/kg Administration:P.O. daily for 7 days Result:Obviously reduced paw swelling at all doses.

Abrocitinib | PF 04965842 | PF04965842

Angiogenesis

JAK

JAK

Inflammation/Immunology

Dermatitis

1622902-68-4

323.415

C14H21N5O2S

>98% (HPLC)

DMSO : 125 mg/mL 386.51 mM

CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3

N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years