Syk-IN-4 是一种有效的，具有口服活性的选择性 SYK 抑制剂，IC50 为 0.31 nM。SYK 已成为自身免疫和血液肿瘤等多个研究领域的潜在靶标。
货号:ajcx34028
CAS:N/A
分子式:C21H25N9O
分子量：419.48
溶解度:DMSO : 62.5 mg/mL (148.99 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers[1].

Syk-IN-4 is a potent inhibitor of hERG with an IC50 of 3.0 μM[1].Syk-IN-4 inhibits SUDHL-4 and T cell proliferation with GI50s of 0.24 and 2.6 µM, respectively[1].

Syk-IN-4 exhibits moderate oral bioavailability (60%) following oral administration (1 mg/kg) in male Hans Wistar rats[1]. Syk-IN-4 exhibits high plasma clearance (151 mL/min/kg) combined with large volumes of distribution (1.0 L/kg respectively) following i.v. administration (0.5 mg/kg) in male Hans Wistar rats[1].

[1]. Neil P Grimster, et al. Optimization of a Series of Potent, Selective and Orally Bioavailable SYK Inhibitors. Bioorg Med Chem Lett. 2020 Jul 24;127433.