MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PF-06650833

CAS No. : 1817626-54-2

MCE 站：PF-06650833

产品活性：PF-06650833 是一种有效的，选择性的和口服可生物利用的白介素-1 受体相关激酶 4 (IRAK4) 的抑制剂，其 IC₅₀ 值为 0.2 nM，在 PBMC 分析中，IC₅₀ 值为 2.4 nM。 PF-06650833 有潜力用于类风湿性关节炎，狼疮和淋巴瘤等疾病的研究。

研究领域：Immunology/Inflammation

作用靶点：IRAK

In Vitro: The kinome selectivity profile of PF-06650833 (Compound 40) is assessed in a panel of 278 kinases (Invitrogen) at 200 nM inhibitor concentration using the ATP K_m for each kinase. Approximately 100% inhibition is observed for IRAK4.
Lactam PF-06650833 (Compound 40) is assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to ａnd including 30 μM. In a voltage clamp assay, PF-06650833 inhibits hERG current by 25% at 100 μM.
The ability of PF-06650833 (Compound 40) to inhibit five major CYP450 enzymes is assessed using pooled human liver microsomes ａnd probe substrates for the CYP450 enzymes. At a concentration of 3 μM of PF-06650833, less than 5% inhibition of CYPs 1A2, 2C8, 2C9, 2D6, ａnd 3A4 is observed. Lactam PF-06650833 is examined for time dependent inhibition effects on six major CYP450 enzymes (CYP1A2, 2B6, 2C8, 2C9, 2C19, ａnd 2D6) using pooled human liver microsomes ａnd probe substrates. At 100 μM of PF-06650833, no time dependent CYP inhibition is observed. The potential induction of CYP3A by PF-06650833 is assessed using cryopreserved human hepatocytes ａnd afforded a 4.4-fold increase in mRNA at 10 μM.

In Vivo: PF-06650833 (Compound 40; 0.3-30 mg/kg; oral administration; for 2.5 hours; male Sprague-Dawley rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of PF-06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM ａnd 150 nM free, respectively, at 2.5 hours after oral administration of PF-06650833 at 0.3, 1, 3, ａnd 30 mg/kg. The fraction unbound in rat plasma of PF-06650833 is 0.3.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Ginsenoside Rb1  |  CA-4948  |  IRAK-1-4 Inhibitor I  |  JH-X-119-01 hydrochloride  |  IRAK4-IN-7  |  AZ1495  |  IRAK4-IN-4  |  IRAK inhibitor 1  |  IRAK4-IN-1  |  IRAK inhibitor 2  |  PF-06426779  |  IRAK inhibitor 6  |  IRAK inhibitor 3  |  IRAK-4 protein kinase inhibitor 2  |  IRAK inhibitor 4  |  IRAK4-IN-6  |  PROTAC IRAK4 degrader-1  |  AS2444697  |  HG-12-6  |  HS271  |  PROTAC IRAK4 degrader-3  |  PROTAC IRAK4 degrader-4  |  PROTAC IRAK4 degrader-5  |  PROTAC IRAK4 degrader-6

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。