|4-甲基-5-((4-((6-(2,2,2-三氟乙基)噻吩并[2,3-d]嘧啶-4-基)氨基)哌啶-1-基)甲基)-1H-吲哚-2-甲腈|CsnPharm

CAS No.: 1628317-18-9

MI-463 Catalog No. CSN17202

Synonyms: MI-463

MI-463 is an effective inhibitor of themenin-MLL interaction.

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400-920-2911

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tech@csnpharm.cn

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MI-463 is a highly potent inhibitor of the menin-MLL interaction with Kd value of 9.9nM and IC50 value of 15.3nM. MI-463 at concentration of 0.3, 1 and 3μM disrupted menin-MLLAF9 interaction in HEK293 cells transfected with MLL-AF9. Also, MI-463 potently inhibited proliferation of MLL-AF9 and Hoxa9/Meis1 (HM-2) transformed murine BMCs after 7-day treatment with GI50 of 0.23μM accompanied with increased level of apoptosis, as well as inhibited the transcription of Hoxa9 and Meis1 post 6 days. Daily administration of 35mg/kg MI-463, i.p., for 28 days, inhibited tumor growth of BALB/c nude mice subcutaneously injected of 0.53 107 MV4;11 cells. Significant decrease of hCD45⁺ can be observed in blood, spleen, and bone marrow samples harvested from NSG mice transplanted with MV4;11 cells after 20-day treatment with MI-463, with decreased transcription of HOXA9, MIES1, MEF2C, and increased transcription of ITGAM in spleen samples. Oral administration of 40mg/kg twice daily blocked progression of MLL Leukemia in C57BL/6 mice transplanted with syngeneic MLL-AF9 leukemic cells isolated from primary recipient mice.
动物研究
剂量
Mice: 35 mg/kg^[1] (i.p.); 50 mg/kg^[1] (p.o., BID)

给药途径
i.p., p.o.

动物研究
剂量	Mice: 35 mg/kg^[1] (i.p.); 50 mg/kg^[1] (p.o., BID)
给药途径	i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0638 mL
- 10.3191 mL
- 20.6381 mL
- 5 mM
- 0.4128 mL
- 2.0638 mL
- 4.1276 mL
- 10 mM
- 0.2064 mL
- 1.0319 mL
- 2.0638 mL

技术信息

CAS号

1628317-18-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H23F3N6S

运输

蓝冰

分子量

484.54

别名

MI-463

溶解度

DMSO	230.0 mg/mL (474.7 mM)
Water	insoluble

动物实验配方

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