CAS NO: | 1436383-95-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with anIC50of 5.7 nM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | BF738735 (Compound 1) strongly inhibits PI4KIIIβ activity in vitro, with an IC50of 5.7 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC50of 1.7 μM). In addition, the activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. BF738735 exhibits a broad spectrum of antiviral activity, as it inhibits all tested species of enteroviruses and rhinoviruses, with 50% effective concentrations ranging between 4 and 71 nM. BF738735 potently inhibits all viruses tested, with EC50s ranging between 4 and 71 nM. The cytotoxicity of BF738735, determined in parallel with the EC50and using the same culture conditions for 3 to 4 days, is low, with CC50values ranging from 11 to 65 μM, resulting in high selectivity indices. Low concentrations of BF738735 reduce the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC50of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3)[1]. | ||||||||||||||||
体内研究 (In Vivo) | BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed[2]. | ||||||||||||||||
分子量 | 426.46 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H19FN4O3S | ||||||||||||||||
CAS 号 | 1436383-95-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(293.11 mM;Need ultrasonic) 配制储备液
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