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Chemical Structure| 1818393-16-6 同义名 : Apg-115;AA-115
CAS号 : 1818393-16-6
货号 : A236509
分子式 : C34H38Cl2FN3O4
纯度 : 98%
分子量 : 642.588
MDL号 : MFCD32197175
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(163.4 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 APG-115 is a compound with a very high affinity to MDM2 (Ki < 1 nM), potent cellular activity, and an excellent oral pharmacokinetic profile.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.56mL

0.31mL

0.16mL

7.78mL

1.56mL

0.78mL

15.56mL

3.11mL

1.56mL

参考文献

[1]Aguilar A, Lu J, et al. Discovery of 4-((3'R,4'S,5'R)-6″-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2″-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3″-indoline] -5'-carboxamido)bicyclo[2.2.2] octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development. J Med Chem. 2017 Apr 13;60(7):2819-2839.