| Identification | Back Directory | [Name]
5-Pyrimidinecarboxamide, 2-[[[2-(4-aminophenyl)-9-methyl-6-(4-morpholinyl)-9H-purin-8-yl]methyl]methylamino]-N-hydroxy-, methanesulfonate (1:1) | [CAS]
2650188-32-0 | [Synonyms]
Purinostat mesylate
5-Pyrimidinecarboxamide, 2-[[[2-(4-aminophenyl)-9-methyl-6-(4-morpholinyl)-9H-purin-8-yl]methyl]methylamino]-N-hydroxy-, methanesulfonate (1:1) | [Molecular Formula]
C24H30N10O6S | [MOL File]
2650188-32-0.mol | [Molecular Weight]
586.63 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
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]. | Animal Model: | Non-irradiated C57BL/6 recipient mice with BL-2 cells injection[1] | | Dosage: | 5 and 10 mg/kg | | Administration: | Intraperitoneal injection; 5-10 mg/kg three times a week; for five weeks | | Result: | Significantly prolonged the overall survival rate and suppressed leukemia progression of mice, and no tumor cell was detected after stopped treatment. |
| Animal Model: | Non-irradiated C57BL/6 recipient mice with BL-2 secondary transplantation[1] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection; 10 mg/kg three times a week | | Result: | Completely eliminated GFP+B220+ cells in spleens on day 3 with two times treatment and this complete inhibition was maintained for 26 days duration of treatment. |
| Animal Model: | B-ALL mouse with BCR-ABL(T315I)-induced leukemia[1] | | Dosage: | 5 and 10 mg/kg | | Administration: | Intravenous injection; 5 and 10 mg/kg three times a week; for 8 weeks | | Result: | Significantly prolonged survival rate of BCR-ABL(T315I)-induced B-ALL mice. Survived all mice after treatment for 42 days. |
| [IC 50]
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); HDAC5: 426 nM (IC50); HDAC7: 590 nM (IC50); HDAC9: 622 nM (IC50); HDAC4: 1072 nM (IC50); HDAC11: 3349 nM (IC50) | [References]
[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. DOI:10.1158/1078-0432.CCR-19-0516 |
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