| 产品描述: | Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia. |
| 靶点: |
HDAC1:0.81 nM (IC50); HDAC10:1.1 nM (IC50); HDAC2:1.4 nM (IC50); HDAC3:1.7 nM (IC50); HDAC8:3.8 nM (IC50); HDAC6:11.5 nM (IC50) |
| 体外研究: |
Purinostat mesylate (5-10 mg/kg; i.p. three times a week for 5 weeks) effectively suppresses leukemia progression in vivo[1]. Purinostat mesylate (5-10 mg/kg; i.v. three times a week for 8 weeks) shows potently anti-leukemia effects in BCR-ABL(T315I)-induced primary B-ALL mice[1]. |
| 体内研究: |
Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3 and 8 with IC50s of 0.81, 1.4, 1.7 and 3.8 nM, inhibits HDAC6 and 10 with IC50s of 11.5 and 1.1 nM, and inhibits HDAC4, 5, 7, 9 and 11 with IC50s of 1072, 426, 690, 622 and 3348 nM, respectively. Purinostat mesylate (0-60 nM; 24 h) induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells. |
| 参考文献: |
1. Yang L, et al. Purinostat Mesylate Is a Uniquely Potent and Selective Inhibitor of HDACs for the Treatment of BCR-ABL-Induced B-Cell Acute Lymphoblastic Leukemia. Clin Cancer Res. 2019 Dec 15;25(24):7527-7539. |
| 保存条件: |
-80°C 6个月; -20°C 1个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.705 ml |
8.523 ml |
17.047 ml |
| 5 mM |
0.341 ml |
1.705 ml |
3.409 ml |
| 10 mM |
0.17 ml |
0.852 ml |
1.705 ml |
| 50 mM |
0.034 ml |
0.17 ml |
0.341 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。 |