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- 详细信息
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
MI463
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1628317-18-9
- 规格：
50mg/25mg/5mg/1mg/10mg
| 规格： | 50mg | 产品价格： | ￥2903.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2028.0 |
| 规格： | 5mg | 产品价格： | ￥735.0 |
| 规格： | 1mg | 产品价格： | ￥363.0 |
| 规格： | 10mg | 产品价格： | ￥1168.0 |
| 基本信息 | |
| CAS | No.1628317-18-9 |
| 英文名称 | MI463 |
| 别名 | ;MI-463;MI463; |
| 分子式 | C24H23F3N6S |
| 分子量 | 484.54 |
| 溶解性 | Soluble in DMSO ≥10mg/mL;Soluble in Water ＜ 1mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28506301 |
| SMILES | FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4C)CC3 |
| 靶点 | Menin-MLL interaction |
| 通路 | Epigenetics |
| 背景说明 | MI-463是Menin-mLL interaction的有效抑制剂。 |
| 生物活性 | MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.[1] |
| In Vitro | MI-463 can reach the target protein in mammalian cells and effectively inhibit the menin-mLL-AF9 interaction at sub-micromolar concentrations. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition， with GI50 of 0.23 μM[1]. |
| 细胞实验 | MI-463 achieves high level in peripheral blood following a single intravenous or oral dose， while also showing high oral bioavailability (45%). Pharmacologic inhibition of the menin-mLL interaction substantially delays progression of mLL leukemia in murine models through on-target activity without causing toxicity. MI-463 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes， HOXA9 and MEIS1， are significant reduced upon treatment with MI-463. 20 days treatment of MV4;11 xenograft recipient mice with MI-463 also results in a substantial delay in leukemia progression as manifested by a marked decrease in the bioluminescence level which is associated with a significant decrease in the population of leukemic cells in the peripheral blood， spleen and bone marrow samples[1]. |
| 细胞实验 | Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed at day 4， viable cell numbers are restored to the original concentration and MI-463 are re-supplied. MTT cell proliferation assay kit is then employed， and plates are read for absorbance at 570 nm using a microplate reader[1]. |
| 动物实验 | Mice: For efficacy studies in MV4;11 subcutaneous xenograft mice model， 5×106 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm3. Vehicle (25% DMSO， 25% PEG400， 50% PBS) or compounds (MI-463 or MI-503) are administrated once daily at designated doses using i.p. injections[1]. |
| 数据来源文献 | [1]. Borkin D， et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602. |
| 单位 | 瓶 |
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IM2390 MI463 表观遗传学 索莱宝
￥363 - 2903
