Purinostat mesylate

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Purinostat mesylate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	2650188-32-0
规格:	≥98%

包装与价格：

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议

产品介绍

理化性质和储存条件

Molecular Formula: C24H30N10O6S;

Molecular Weight: 586.62

In Vitro	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[1]. Purinostat mesylate (0-60 nM; 24 h) induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells[1]. Cell Proliferation Assay[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-80 nM Incubation Time: 24, 48 and 72 hours Result: Significantly inhibited cell proliferation of LAMA84 and 188 BL-2 cells. Apoptosis Analysis[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-60 nM Incubation Time: 24 hours Result: Induced apoptosis of LAMA84 and 188 BL-2 cells. Cell Cycle Analysis[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-40 nM Incubation Time: 24 hours Result: Dose-dependently blocked cell cycle progression at G0/G1 phase. Western Blot Analysis[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-40 nM Incubation Time: 24 hours Result: Dose-dependently increased the 191 levels of Ac-H3 and Ac-H4, and decreased HSP90.
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.

In Vitro

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[1]. Purinostat mesylate (0-60 nM; 24 h) induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells[1]. Cell Proliferation Assay[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-80 nM Incubation Time: 24, 48 and 72 hours Result: Significantly inhibited cell proliferation of LAMA84 and 188 BL-2 cells. Apoptosis Analysis[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-60 nM Incubation Time: 24 hours Result: Induced apoptosis of LAMA84 and 188 BL-2 cells. Cell Cycle Analysis[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-40 nM Incubation Time: 24 hours Result: Dose-dependently blocked cell cycle progression at G0/G1 phase. Western Blot Analysis[1] Cell Line: LAMA84 and 188 BL-2 cell lines Concentration: 0-40 nM Incubation Time: 24 hours Result: Dose-dependently increased the 191 levels of Ac-H3 and Ac-H4, and decreased HSP90.

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.