UPADacitinib 是高效选择性的,具有口服活性的JAK1抑制剂,IC50为43 nM,可用于多种自身免疫性疾病的研究。它对 JAK1 的选择性约为 JAK2 的 74 倍。
产品描述
Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.
体外活性
Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2, which is involved in erythropoiesis. And Upadacitinib is 58-fold more selective for JAK-1 than for JAK-3, which is involved in immunosurveillance. The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit-risk profile in patients with RA range.
体内活性
Upadacitinib, a second JAK inhibitor, has been developed by AbbVie.Upadacitinib finished multiple-dose Phase I studies in 2013. Upadacitinib show to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation in phase I trials. Upadacitinib exposure is dose proportional to the evaluated multiple dose.
Cas No.
1310726-60-3
分子式
C17H19F3N6O
分子量
380.375
别名
乌帕替尼;ABT-494
储存和溶解度
DMSO:22 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years