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HDM201 R Enantiomer
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。
HDM201 R Enantiomer图片
CAS NO:1448867-42-2
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
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产品介绍
理化性质和储存条件
Molecular Weight (MW) 555.41
Formula C26H24Cl2N6O4
CAS No.1448867-42-2 (R-isomer);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ~100 mg/mL (180.0 mM)
Water: < 1 mg/mL
Ethanol: 3 mg/mL (5.4 mM)
Exact Mass 554.1236
Synonyms HDM-201; HDM 201; HDM201; NVP-HDM 201; NVP-HDM201; NVP-HDM-201
SMILES Code O=C1N(C2=CC(Cl)=CN(C)C2=O)[C@@H](C3=CC=C(Cl)C=C3)C4=C1N=C(C5=CN=C(OC)N=C5OC)N4C (C)C
实验参考方法
In Vitro

In vitro activity: HDM201 acts by binding to the p53 binding-site of the Mdm2 protein, thereby disrupting the interaction of the two proteins (p53 and Mdm2) and leading to the activation of the p53 pathway. It induces robust p53-dependent cell cycle arrest and apoptosis in human p53 wild-type tumor cells. HDM201 exhibits highly selectivity across a panel of cancer cell lines


Kinase Assay:


Cell Assay: The in vitro combination screen was performed at Horizon Discovery (Cambridge, MA) on cancer cell lines, and data analysis was performed as described previously. Here we focused the data analysis on combinations with CGM097, a previous class of selective TP53-MDM2 inhibitors. A total of 485 cancer cell lines were treated with varying concentrations of CGM097 and for 25 other compounds. We integrated the information on TP53 mutation status and differentiated cell lines with no TP53 mutation from cell lines with TP53 alteration. We assessed the synergistic effect of combinations of HDM201and A-1155463 as described previously.

In VivoTreatment was initiated when the tumors engrafted in the flank were at least 150 mm3. Random enrollment was applied. Efficacy studies, tumor response, and relapse were reported with the measures of tumor volumes at the start of treatment. HDM201 was administered at 100 mg/kg in 0.5% methylcellulose and 0.1% Tween 80 orally twice a week, with alternating intervals of 3 d and 4 d. Vehicle was generated according to the formulation. Treatments were administered in the morning.
Animal model Mouse
Formulation & Dosage HDM201 was administered at 100 mg/kg in 0.5% methylcellulose and 0.1% Tween 80 orally twice a week
References Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3151-3156.