生物活性
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α[1][2].
体外研究
PI-1840 (5-60 µM; 24 and 48 h) inhibits the proliferation of MG-63 and U2-OS cells[1].
PI-1840 (40 µM (U2-OS cells) and 60 µM (MG-63 cells); 24 and 48 h) induces cell cycle arrest at the G2/M phase[1].
PI-1840 (15-60 µM (MG-63 cells), 10-40 µM (U2-OS cells); 48 h) induces apoptosis through NF-κB pathway in MG-63 and U2-OS cells. PI-1840 induces autophagy in MG-63 and U2-OS cells[1].
Cell Viability Assay[1]
Cell Line: MG-63 and U2-OS cells
Concentration: 5, 10, 20, 40, 80, and 160 µM
Incubation Time: 24 and 48 hours
Result: Inhibited cell growth in a dose-dependent manner with IC50 values of 108.40 µM (MG-63, 24 h), 59.58 µM (MG-63, 48 h), 86.43 µM (U2-OS, 24 h), and 38.83 µM (U2-OS, 48 h), respectively.
体内研究
PI-1840 (150 mg/kg; i.p.; daily, for 14 d) inhibits the growth of human breast tumor xenografts in nude mice[2].
Animal Model: Female nude mice with MDA-MB-231 xenografts[2]
Dosage: 150 mg/kg
Administration: Intraperitoneal injection; daily, for 14 days
Result: Inhibited the growth of MDA-MB-231 tumor xenografts by 76%.
分子量
394.47
性状
Solid
Formula
C22H26N4O3
CAS 号
1401223-22-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : 100 mg/mL (253.50 mM; Need ultrasonic)
H2O : 0.1 mg/mL (0.25 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: