13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費(fèi)訂購熱線：021-59541103 021-60443211
標(biāo)簽:PF06650833
聯(lián)系人:高小姐
電話:021-59541103 021-60443211
手機(jī):13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細(xì)地址：上海嘉定區(qū)嘉羅公路1661
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化學(xué)性質(zhì)：
| 規(guī)格 | 5mg 10mg 50mg 100mg |
| CAS | 1817626-54-2 |
| 別名 | N/A |
| 化學(xué)名 | N/A |
| 分子式 | C18H20FN3O4 |
| 分子量 | 361.37 |
| 溶解度 | DMSO : ≥ 33 mg/mL (91.32 mM) |
| 儲(chǔ)存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述：
PF06650833 is a potent, selective and orally active inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4) with IC50s of 0.2 and 2.4 nM in the cell and PBMC assay, respectively. PF06650833 is used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas[1][2].
The kinome selectivity profile of PF06650833 (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[1]. Lactam PF06650833 (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, PF06650833 inhibits hERG current by 25% at 100 μM[1]. The ability of PF06650833 (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 PF06650833, less than 5% inhibition of CYPs 1A2, 2C8, 2C9, 2D6, and 3A4 is observed. Lactam PF06650833 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 PF06650833, no time dependent CYP inhibition is observed. The potential induction of CYP3A by PF06650833 is assessed using cryopreserved human hepatocytes and afforded a 4.4-fold increase in mRNA at 10 μM[1].
PF06650833 (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 PF06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF06650833 at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of PF06650833 is 0.3[1].
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原創(chuàng)作者：上海莼試生物技術(shù)有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業(yè)部
賬 號：2169 2341 6278
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