PTC-209是特异的BMI-1抑制剂,IC50为0.5 uM。并能不可逆的减少癌起始细胞(CICs).
PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
~10 μM
~60mg/kg/天s.c.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Kreso A, et al. Nat Med. 2014, 20(1), 29-36.
[2] Christian Mayr,et al. The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells. Oncotarget. 2016 Jan 5; 7(1): 745–758. Published online 2015 Nov 24. doi: 10.18632/oncotarget.6378.
[3] Arnold Bolomsky,et al. Targeting of BMI-1 with PTC-209 shows potent anti-myeloma activity and impairs the tumour microenvironment. J Hematol Oncol. 2016; 9: 17. Published online 2016 Mar 2. doi: 10.1186/s13045-016-0247-4.
分子式 C17H13Br2N5OS |
分子量 495.19 |
CAS号 315704-66-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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