貨號	規格	價格	上海	北京	武漢	南京
S81383-5mg	99.2%	￥590.00 S81383-5mg ￥590.00 現貨	6 6	-	-	-
S81383-10mg	99.2%	￥940.00 S81383-10mg ￥940.00 現貨	5 5	-	-	-
S81383-25mg	99.2%	￥1630.00 S81383-25mg ￥1630.00 現貨	4 4	-	-	-
S81383-100mg	≥99%	￥3210.00 S81383-100mg ￥3210.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).

產品描述：

MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).

靶點：

Epigenetic Reader Domain;Histone Methyltransferase;EpigeneticReaderDomain;?HistoneMethyltransferase

體外研究：

Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition (GI50: 0.23 μM). MI-463 is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of MI-463 also leads to markedly reduced expression of Hoxa9 and Meis1.

體內研究：

MI-463 shows substantial survival benefit in mouse models of MLL leukemia. It has very favorable druglike properties, including metabolic stability and PK profile in mice. MI-463 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). 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, is significantly reduced upon treatment with MI-463.

細胞實驗：

Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed on day 4, viable cell numbers are restored to the original concentration and MI-463 is re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader.

動物實驗：

For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×10^6 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm^3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or MI-463 are administrated once daily at designated doses using i.p. injections.

參考文獻：

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.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.064 ml	10.319 ml	20.638 ml
5 mM	0.413 ml	2.064 ml	4.128 ml
10 mM	0.206 ml	1.032 ml	2.064 ml
50 mM	0.041 ml	0.206 ml	0.413 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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MI-463

4-methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile