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CAS No.: 1628316-74-4

MI-136 Catalog No. CSN17201

MI-136 can selectively inhibit the interaction of menin and MLL. It also suppresses DHT-induced expression of androgen receptor (AR) target genes.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MI-136 can disrupt menin-MLL interaction. MI-136 inhibits AR-mediated transcription by blocking MLL recruitment predominantly at the level of the menin-MLL interaction. In the presence of MI-136, the recruitment of ASH2L (but not AR) to TMPRSS2 and PSA promoters was significantly decreased, thus inhibiting the expression of genes that were bound to ASH2L after AR stimulation. AR positive cell lines such as VCaP, LNCaP and 22RV1 were sensitive to MI-136. It blocked DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP) and induced apoptosis of VCaP cells as evidenced by PARP cleavage. Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) led to a modest but significant reduction in tumor volume^[2].
动物研究
剂量
Mice: 40 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 40 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Malik R, Khan AP, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52.
[2] Malik R, Khan AP, Asangani IA, Cieślik M, Prensner JR, Wang X, Iyer MK, Jiang X, Borkin D, Escara-Wilke J, Stender R, Wu YM, Niknafs YS, Jing X, Qiao Y, Palanisamy N, Kunju LP, Krishnamurthy PM, Yocum AK, Mellacheruvu D, Nesvizhskii AI, Cao X, Dhanasekaran SM, Feng FY, Grembecka J, Cierpicki T, Chinnaiyan AM. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52. doi: 10.1038/nm.3830. Epub 2015 Mar 30. PMID: 25822367; PMCID: PMC4390530.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1253 mL
- 10.6267 mL
- 21.2534 mL
- 5 mM
- 0.4251 mL
- 2.1253 mL
- 4.2507 mL
- 10 mM
- 0.2125 mL
- 1.0627 mL
- 2.1253 mL

技术信息

CAS号

1628316-74-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H21F3N6S

运输

蓝冰

分子量

470.51

别名

溶解度

DMSO	480.0 mg/mL (1020.2 mM)
Water	insoluble

动物实验配方

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