Abrocitinib-PF-04965842-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAbrocitinibCat. No.: HY-107429CAS No.: 1622902-68-4Synonyms: PF-04965842分式: CHNOS分量: 323.41作靶点: JAK作通路: Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实

2、验 DMSO : 125 mg/mL (386.51 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0921 mL 15.4603 mL 30.9205 mL5 mM 0.6184 mL 3.0921 mL 6.1841 mL10 mM 0.3092 mL 1.5460 mL 3.0921 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可

3、靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.43 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (6.43 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% cor

4、n oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (6.43 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Abrocitinib (PF-04965842)种有效、可服、选择性的 JAK1 抑制剂，对 JAK1 和 JAK2 的 IC50 值分别为29 和 803 nM。Abrocitinib (PF-04965842) 可抑制 TYK2 的活性(IC50，1.253 M) 和刺激后 STAT1，STAT3和 STAT5 的磷酸化平。可于免疫症的研究

5、1。IC50 & Target JAK1 JAK2 Tyk229 nM (IC50) 803 nM (IC50) 1253 nM (IC50)体外研究 Abrocitinib (Compound 25) inhibits IFN-stimulated phosphorylation of STAT3, IFN-stimulatedphosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB(JAK2), with IC50s of 189, 163 nM, 7.17

6、8 M, respectively 1.体内研究 Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in ratadjuvant-induced arthritis model 1.Animal Model: Female Lewis rats (810 weeks old) 1Dosage: 5, 15, 50 mg/kgAdministration: P.O. daily for 7 daysResult: Obviously reduc

7、ed paw swelling at all doses.REFERENCES1. Vazquez ML, et al. Identification of N-cis-3-Methyl(7H-pyrrolo2,3-dpyrimidin-4-yl)aminocyclobutylpropane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. J Med Chem. 2018 Feb 8;61(3):1130-1152.McePdfHeightCaution: Product has not been fully validated for medical applications.For research u