货号	规格	价格	上海	北京	珠海	重庆	武汉
S81382-5mg促销	≥98%	￥990.00 ￥630.00 S81382-5mg ￥630.00 现货	10 10	-	-	-	-
S81382-10mg促销	≥98%	￥1700.00 ￥1030.00 S81382-10mg ￥1030.00 现货	10 10	-	-	-	-
S81382-25mg促销	≥98%	￥3390.00 ￥1830.00 S81382-25mg ￥1830.00 现货	8 8	-	-	-	-
S81382-50mg促销	≥98%	￥5350.00 ￥3190.00 S81382-50mg ￥3190.00 现货	4 4	-	-	-	-
S81382-100mg促销	≥98%	￥9680.00 ￥4470.00 S81382-100mg ￥4470.00 现货	4 4	-	-	-	-

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产品描述：

MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced

靶点：

Androgen Receptor;Apoptosis;Epigenetic Reader Domain;Apoptosis; EpigeneticReaderDomain; AndrogenReceptor

体外研究：

MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage and blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer.

体内研究：

Treatment of VCaP tumor-bearing mice with MI-136 (40 mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight.

细胞实验：

To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM MI-136 for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and MI-136 for 48 hrs. Cells are then stimulated with 10nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays. (Only for Reference)

参考文献：

1. Malik R, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015, 21(4):344-352.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.125 ml	10.627 ml	21.253 ml
5 mM	0.425 ml	2.125 ml	4.251 ml
10 mM	0.213 ml	1.063 ml	2.125 ml
50 mM	0.043 ml	0.213 ml	0.425 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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MI-136

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

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)