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MI-463 Sale

目录号 : GC19246

An inhibitor of menin-MLL fusion protein interactions

MI-463 Chemical Structure

Cas No.:1628317-18-9

规格 价格 库存 购买数量
1mg
¥483.00
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5mg
¥1,166.00
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10mg
¥1,848.00
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50mg
¥6,762.00
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100mg
¥10,784.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment:

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].

Animal experiment:

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].

References:

[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.

产品描述

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

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 uM[1].

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].

References:
[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.

Chemical Properties

Cas No. 1628317-18-9 SDF
Canonical SMILES FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4C)CC3
分子式 C24H23F3N6S 分子量 484.54
溶解度 DMSO : 125 mg/mL (257.98 mM);Water : < 0.1 mg/mL (insoluble) 储存条件 Store at -20°C
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溶解性数据

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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
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