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编 号：F754396
分子式：C24H30N10O6S
分子量：586.62
分子式：C24H30N10O6S
分子量：586.62
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CAS No: 2650188-32-0
产品详情
生物活性：
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.
体内研究：
Purinostat mesylate (5-10 mg/kg; i.p. three times a week for 5 weeks) effectively suppresses leukemia progression in vivo.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.Animal Model:Non-irradiated C57BL/6 recipient mice with BL-2 cells injection
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
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
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.
体外研究：
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.
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.
体内研究：
Purinostat mesylate (5-10 mg/kg; i.p. three times a week for 5 weeks) effectively suppresses leukemia progression in vivo.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.Animal Model:Non-irradiated C57BL/6 recipient mice with BL-2 cells injection
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
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
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.
体外研究：
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.
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