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APS-2-79

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Chemical Structure| 2002381-25-9 同义名 : -
CAS号 : 2002381-25-9
货号 : A492049
分子式 : C23H21N3O3
纯度 : 99%+
分子量 : 387.431
MDL号 : MFCD30489745
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(46.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 APS-2-79 functions as a KSR-dependent antagonist of MEK. It effectively blocks ATP-biotin from binding to KSR2 in the KSR2-MEK1 complex, with an IC50 value of 120 nM. APS-2-79 stabilizes the inactive state of KSR, thereby counteracting oncogenic Ras-MAPK signaling. At a concentration of 5 μM, APS-2-79 inhibits the phosphorylation of MEK and ERK induced by KSR in 293H cells. Furthermore, at 1 μM, APS-2-79 boosts the effectiveness of the MEK inhibitor trametinib used in clinical settings against cancer cell lines that harbor K-Ras mutations[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.58mL

0.52mL

0.26mL

12.91mL

2.58mL

1.29mL

25.81mL

5.16mL

2.58mL
参考文献

[1]Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116.