上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
MI-463 纯度: 99.82%
MI-463是高效,有口服活性的menin-mLL相互作用的小分子抑制剂。
MI-463 Chemical Structure
CAS No. : 1628317-18-9
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥1812 | In-stock | |
1 mg | ¥700 | In-stock | |
5 mg | ¥1700 | In-stock | |
10 mg | ¥2700 | In-stock | |
50 mg | ¥9900 | In-stock | |
100 mg | ¥15800 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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MI-463 相关产品
•相关化合物库:
- Covalent Screening Library Plus
- Bioactive Compound Library Plus
- Epigenetics Compound Library
- Histone Modification Research Compound Library
- Anti-Cancer Compound Library
- Covalent Screening Library
- Reprogramming Compound Library
- Orally Active Compound Library
- Anti-Blood Cancer Compound Library
生物活性 |
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. |
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体外研究 (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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
484.54 |
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Formula |
C24H23F3N6S |
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CAS 号 |
1628317-18-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 125 mg/mL (257.98 mM; Need ultrasonic) 配制储备液
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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。 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
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参考文献 |
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Cell Assay [1] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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