PF 06651600

Name	1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one
Synonyms	CS-2733 EOS-61890 PF06651600 PF-06651600 PF 06651600 PF-06651600 Ritlecitinib PF06651600 PF 06651600 RITLECITINIB 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one 1-[(2S,5R)-2-methyl-5(7H-pyrrolo[2,3-d]pyrimidine-4-ylamino)-1-piperidinly]-2-propen-1-one malonate,PF06651600
CAS	1792180-81-4

Molecular Formula	C15H19N5O
Molar Mass	285.34
Density	1.272±0.06 g/cm3(Predicted)
Appearance	powder
Color	white to beige
pKa	13.03±0.50(Predicted)
Storage Condition	room temp
In vitro study	PF-06651600 is a new potent and selective inhibitor of JAK3, which is very effective in inhibiting γc factor signaling. In Vitro, PF-06651600 inhibits Th1 and Th17 cell differentiation and function. In total lymphocytes of human whole blood, PF-06651600 inhibiting STAT5 phosphorylation by IL-2, IL-4, IL-7, and IL-15, The IC50 was 244, 340, 407 and 266 nM, respectively. It also inhibits STAT3 phosphorylation by IL-21 with an IC50 of 355 nM.
In vivo study	In the murine model of experimental autoimmune encephalomyelitis and in the rat adjuvant arthritis, PF-06651600 reduces the pathological features of the disease. PF-06651600 have suitable pharmacokinetic and pharmacodynamic properties in preclinical and clinical evaluations. The pharmacokinetic prediction of PF-06651600 in humans indicates that the blood clearance is about 5.6 mL/min/kg, the volume of distribution is 1.3 L/kg, and the oral bioavailability is 90%, the systemic Half-Life is 2 hours.

biological activity	Ritlecitinib (PF-06651600) was a JAK3 selective inhibitor with an IC50 of 33.1 nM. There was no activity against JAK1, JAK2 and TYK2 (IC50 > 10 000 nM).
Target	Value
JAK3 (Cell-free assay)	33.1 nM

Last Update：2024-04-09 21:04:16

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CAS: 1792180-81-4
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Spot supply

Product Name: Ritlecitinib Visit Supplier Webpage Request for quotation
CAS: 1792180-81-4
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052

Wechat: 15671228036

Wechat: 18301782025

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PF 06651600

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