规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | MELK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
OTSSP167 |
+++
MELK, IC50: 0.41 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1]. OTSSP167 effectively interferes with the mitotic checkpoint and disrupts MCC and MCC-APC/C interactions in MCF7 cells, also causing GFP-MELK localization to the cell cortex in prometaphase cells[2]. As a selective MELK inhibitor, OTSSP167 exhibits a strong in vitro activity with an IC50 of 0.41 nM[3]. |
体内研究 | In vivo, OTSSP167 at 20 mg/kg (i.v.) achieves a tumor growth inhibition (TGI) of 73% in a xenograft mouse model; oral administrations at 1, 5, and 10 mg/kg result in TGI of 51, 91, and 108%, respectively, though a 20 mg/kg oral dose does not suppress tumor growth in PC-14 xenografts[1]. |
体外研究 | OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1]. OTSSP167 effectively interferes with the mitotic checkpoint and disrupts MCC and MCC-APC/C interactions in MCF7 cells, also causing GFP-MELK localization to the cell cortex in prometaphase cells[2]. As a selective MELK inhibitor, OTSSP167 exhibits a strong in vitro activity with an IC50 of 0.41 nM[3]. |
作用机制 | OTSSP167 optimally occupies the active site of MELK, especially the hydrophobic back pocket, mainly through van der Waals interactions.[2] |
Dose | Mice: 1 mg/kg - 20 mg/kg[1] (i.v.); 5 mg/kg, 10mg/kg[1] (p.o.) |
Administration | i.v., p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.05mL 0.41mL 0.21mL |
10.26mL 2.05mL 1.03mL |
20.52mL 4.10mL 2.05mL |
CAS号 | 1431697-89-0 |
分子式 | C25H28Cl2N4O2 |
分子量 | 487.421 |
别名 | OTS167 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 2 mg/mL(4.1 mM),配合低频超声,水浴加热至45℃,并调节pH至4,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+water 0.04 mg/mL clear PO 0.5% CMC-Na 31 mg/mL suspension |