货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T93543-1ml促销	10mM in DMSO	￥878.00 ￥790.00 T93543-1ml ￥790.00 现货	10 10	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T93543-1ml促销

10mM in DMSO

￥878.00 ￥790.00

产品描述：

BMI-1 抑制剂;BMI-1 Inhibitors;产品介绍：PTC-028是一种具有生物口服活性的化合物，能够通过翻译后修饰减少BMI-1水平。;InformationPTC-028 PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.TargetsBMI-1In vitroPTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification. PTC-028 treatment selectively inhibits cancer cells in clonal growth and viability assays, whereas normal cells remain unaffected. Hyperphosphorylation-mediated depletion of cellular BMI-1 by PTC-028 coupled with a concurrent temporal decrease in ATP and a compromised mitochondrial redox balance potentiates caspase-dependent apoptosis.In vivoorally administered PTC-028, as a single agent, exhibits significant antitumor activity comparable with the standard cisplatin/paclitaxel therapy in an orthotopic mouse model of ovarian cancer. After administration of single oral doses to the CD-1 mice, total plasma AUC0-24h are 10.9 and 26.1 mg/h/mL at doses of 10 and 20 mg/kg, showing dose proportional pharmacokinetics. The Cmax for PTC-028 at 10 and 20 mg/kg is 0.79 and 1.49 mg/mL, respectively. The Cmax is reached at both dose levels 1-hour postdose after which plasma concentrations slowly reduce.Cell Research(from reference)Cell lines：Immortalized ovarian surface epithelium (OSE) or the fallopian tube epithelium(FTE) cells and ovarian cancer cells Concentrations：0-500 nmol/L Incubation Time：48 h

靶点：

BMI-1

体内研究：

PTC-028 (15 mg/kg；每周口服给药两次) 与对照组 (平均肿瘤重量，~3g) 相比，导致肿瘤重量减少约 94% (0.169 g)。
根据平均体重评估，动物在处理实验期间未发现明显毒性。
PTC-028 (10 mg/kg 或 20mg/kg；单次口服剂量) 施用于 CD-1 小鼠。两种剂量水平的 Cmax 均在给药后 1 小时达到，之后血浆浓度缓慢降低。

参考文献：

1. Dey A, et al. Evaluating the Mechanism and Therapeutic Potential of PTC-028, a Novel Inhibitor of BMI-1 Function in Ovarian Cancer. Mol Cancer Ther. 2018 Jan;17(1):39-49.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.467 ml	12.336 ml	24.672 ml
5 mM	0.493 ml	2.467 ml	4.934 ml
10 mM	0.247 ml	1.234 ml	2.467 ml
50 mM	0.049 ml	0.247 ml	0.493 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。

参考文献

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