MI-136CAS号： 1628316-74-4分子式： C23H21F3N6S 分子量： 470.51描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
|
| 纯度 |
＞98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 可溶性/溶解性 |
体外:
DMSO 94mg/mL(199.78mM) Ethanol 94mg/mL(199.78mM) Water <1mg> |
| 生物活性 | |
| 靶点 |
Menin-MLL interaction
|
| In vitro(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.
|
| In vivo(体内研究) |
Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight.
|
分子结构图
