MS1943CAS号： 2225938-17-8分子式： C42H54N8O3分子量： 718.93描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 可溶性/溶解性 |
DMSO:120mg/mL (166.91mM)
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| 生物活性 | |
| 靶点 |
EZH2:120 nM
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| In vitro(体外研究) |
MS1943 inhibits cell growth (GI50 of 2.2 μM). MS1943 induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1].
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| In vivo(体内研究) |
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 μM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 μM, but plasma concentrations were below the cellular IC50 value.MS1943 suppresses tumor growth[1].
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