貨號	規(guī)格	價格	上海	北京	武漢	南京
S81409-5mg	99.7%	￥400.00 S81409-5mg ￥400.00 現(xiàn)貨	5 5	-	-	-
S81409-10mg	99.7%	￥550.00 S81409-10mg ￥550.00 現(xiàn)貨	5 5	-	-	-
S81409-25mg	99.7%	￥800.00 S81409-25mg ￥800.00 現(xiàn)貨	5 5	-	-	-
S81409-100mg	≥98%	￥2360.00 S81409-100mg ￥2360.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.

產(chǎn)品描述：

MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.

靶點：

Epigenetic Reader Domain;Histone Methyltransferase;EpigeneticReaderDomain;?HistoneMethyltransferase

體外研究：

MI-503 occupies the F9 and P13 pockets on menin, forming a hydrogen bond with Tyr276, and also extends beyond the P13 pocket to form hydrogen bonds with Trp341 and Glu366. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-503 results in substantial growth inhibition, with GI50 of 0.22 μM. The cell growth inhibitory effect of MI-503 is time-dependent, with a pronounced effect achieved after 7-10 days of treatment.

體內(nèi)研究：

MI-503 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (75%). MI-503 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. Treatment with MI-503 results in an over 80% reduction in MV4;11 tumor volume and complete tumor regression in two mice. Ten consecutive days of treatment with MI-503 results in a marked delay in progression of mLL leukemia in mice and significantly reduces leukemia tumor burden. Treatment with MI-503 and MI-463 leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of mLL fusion proteins substantially upregulated in mLL leukemias.

細胞實驗：

Leukemia cells are treated with MI-503 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-503 are 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 compounds (MI-463 or MI-503) 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	1.771 ml	8.855 ml	17.711 ml
5 mM	0.354 ml	1.771 ml	3.542 ml
10 mM	0.177 ml	0.886 ml	1.771 ml
50 mM	0.035 ml	0.177 ml	0.354 ml

注意：

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

參考文獻

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MI-503

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