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Serabelisib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Serabelisib图片
CAS NO:1268454-23-4

MLN1117
INK1117
TAK-117
Serabelisib (MLN1117) 是一种选择性的p110α抑制剂,IC50值为 15 nM。
生物活性

Serabelisib (MLN1117) is a selectivep110αinhibitor with anIC50of 15 nM.

IC50& Target

p110α

15 nM (IC50)

p110β

4500 nM (IC50)

p110δ

13900 nM (IC50)

p110γ

1900 nM (IC50)

mTOR

1670 nM (IC50)

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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 6.4 mg/mL(17.61 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7520 mL13.7601 mL27.5202 mL
5 mM0.5504 mL2.7520 mL5.5040 mL
10 mM0.2752 mL1.3760 mL2.7520 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

 
 
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