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CAS No. : 1817626-54-2
MCE 国际站:Zimlovisertib
产品活性:Zimlovisertib (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。Zimlovisertib 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 Zimlovisertib (Compound 40) is assessed in a panel of 278 kinases (Invitrogen) at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4.
Lactam Zimlovisertib 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, Zimlovisertib inhibits hERG current by 25% at 100 μM.
The ability of Zimlovisertib 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 Zimlovisertib, less than 5% inhibition of CYPs 1A2, 2C8, 2C9, 2D6, and 3A4 is observed. Lactam Zimlovisertib 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 Zimlovisertib, no time dependent CYP inhibition is observed. The potential induction of CYP3A by Zimlovisertib is assessed using cryopreserved human hepatocytes and afforded a 4.4-fold increase in mRNA at 10 μM.
In Vivo: Zimlovisertib (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 Zimlovisertib in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of Zimlovisertib at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of Zimlovisertib 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 | Rare Diseases Drug Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | IRAK4-IN-4 | HS-276 | HS-243 | IRAK inhibitor 2 | IRAK4-IN-14 | HG-12-6 | IRAK4-IN-13 | Zabedosertib | KTX-612 | IRAK inhibitor 6 | KTX-582 | IRAK4-IN-19 | AZ1495 | IRAK4-IN-1 | IRAK4-IN-21 | PROTAC IRAK4 degrader-5 | IRAK4-IN-17 | IRAK4-IN-12 | PROTAC IRAK4 degrader-6 | KTX-951 | IRAK4-IN-22 | IRAK4-IN-11 | JH-X-119-01 hydrochloride | PF-06426779 | JNJ-1013 | IRAK4-IN-16 | Ginsenoside Rb1 | KTX-497 | IRAK-1-4 Inhibitor I
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