CAS NO: | 1268454-23-4 |
生物活性 | Serabelisib (MLN1117) is a selectivep110αinhibitor with anIC50of 15 nM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Serabelisib (MLN1117) inhibits Akt phosphorylation and growth inPIK3CAmutant breast cancer cells with IC50s around 2 μM, yet has no effect on cells lackingPTEN. BCR-stimulated B cells treated with 1 μM Serabelisib (MLN1117) displays a significant reduction (up to 50%) in the magnitude of the phosphorylated Akt (p-Akt) signal measured by intracellular flow cytometry. The effect of Serabelisib is dose-dependent[1]. | ||||||||||||||||
体内研究 (In Vivo) | Treatment with Serabelisib (MLN1117) at 30 and 60 mg/kg causes little reduction of TNP-specific IgG3. Notably, reduction of TNP-specific IgG3 at higher doses of Serabelisib (MLN1117) (120 mg/kg) is observed, consistent with the partial reduction in cell division in B cells treated with Serabelisib before anti-IgM stimulation. However, 120 mg/kg is above the effective dose of Serabelisib (MLN1117) for tumor growth inhibition (30-60 mg/kg)[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 363.37 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H17N5O3 | ||||||||||||||||
CAS 号 | 1268454-23-4 | ||||||||||||||||
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 : 6.4 mg/mL(17.61 mM;Need ultrasonic and warming) 配制储备液
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