MD-222 是一种首创的高效的基于 PROTAC 的MDM2降解剂。MD-222 由Cereblon和MDM2配体组成。MD-222 诱导MDM2蛋白快速降解并激活细胞中的野生型 p53。MD-222 具有抗癌作用。
生物活性 | MD-222 is the first-in-class highly potentPROTACdegrader ofMDM2. MD-222 consists of ligands forCereblonandMDM2. MD-222 induces rapid degradation of theMDM2protein and activation of wild-type p53 in cells. MD-222 has anticancer effects[1][2]. |
IC50& Target[1][2] | |
体外研究 (In Vitro) | MD-222 (1-30 nM; 1-2 hours) treatment shows very effective in reducing the levels of MDM2 protein and increasing the levels of p53 in a time- and dose-dependent manner in RS4;11 and RS4;11/IRMI-2 cells[1]. MD-222 (30-100 nM; 6 hours) is effective in increasing the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA in RS4;11 cells, indicating strong activation of p53[2]. MD-222 (4 days) shows cell growth inhibitory activity in RS4;11 cells with an IC50 of 5.5 nM, and has no effect on RS4;11/IRMI-2, MDA-MB-231 and MDA-MB-468 cells[1].
Western Blot Analysis[1] Cell Line: | RS4;11 and RS4;11/IRMI-2 cells | Concentration: | 1 nM, 3 nM, 10 nM, 30 nM | Incubation Time: | 1 hour, 2 hours | Result: | Reduced the level of MDM2 and increased the level of p53. |
RT-PCR[2] Cell Line: | RS4;11 cells | Concentration: | 30 nM, 100 nM | Incubation Time: | 6 hours | Result: | Increasd the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 200 mg/mL(223.76 mM;Need ultrasonic) 配制储备液 1 mM | 1.1188 mL | 5.5939 mL | 11.1878 mL | 5 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL | 10 mM | 0.1119 mL | 0.5594 mL | 1.1188 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 (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 5 mg/mL (5.59 mM); Suspended solution; Need ultrasonic
此方案可获得 5 mg/mL (5.59 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (5.59 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (5.59 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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