Siremadlin

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Chemical Structure| 1448867-41-1 同义名 : HDM201;NVP-HDM 201;NVP-HDM201
CAS号 : 1448867-41-1
货号 : A468171
分子式 : C26H24Cl2N6O4
纯度 : 99%+
分子量 : 555.413
MDL号 : MFCD30502893
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 55 mg/mL(99.03 mM),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 Siremadlin (NVP-HDM201) interrupts the interaction between TP53 and MDM2 in both human and mouse cells, exhibiting nanomolar IC50 values and effectively preventing TP53 degradation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

18.00mL

3.60mL

1.80mL

参考文献

[1]Chapeau EA, et al. Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf-/- mouse model. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3151-3156.

[2]Furet P, et al. Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-41.

[3]Stéphane F, et al. Abstract 1224: Insights into the mechanism of action of NVP-HDM201, a differentiated and versatile Next-Generation small-molecule inhibitor of Mdm2, under evaluation in phase I clinical trials. Insights into the mechanism of action of N