产品
编 号：F763005
分子式：C22H24FN3O5
分子量：429.44
分子式：C22H24FN3O5
分子量：429.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 3031349-25-1
产品详情
生物活性：
TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity.
体内研究：
TH-6 (10, 20 mg/kg; i.v.; daily for 21 days) shows anti-tumor activity in mouse.TH-6 (20 mg/kg) shows antivascular activity and a good cardiovascular safety profile in mouse.Animal Model:4-5 weeks, 18-22 g female ICR mice (H22 allograft mouse model)
Dosage:10, 20 mg/kg
Administration:I.v.; daily for 21 days
Result:Reduced tumor weights at day 21 by 82% and did not affect body weight during treatment, indicating the low toxicity.
体外研究：
TH-6 (0-2 μM) shows antiproliferative activities in cancer cell lines and normal human lung cells.TH-6 (0-10 μM) inhibits tubulin polymerization with an IC50 value of 4.06 μM.TH-6 (0.03, 0.1, 0.3 1 μM; 24 h) increases the expression of Ac-α-Tubulin and AC-Histone H3 in HepG2 cells.TH-6 (7.5, 15, 30 nM) induces apoptosis and cell cycle arrest at G2/M phase.TH-6 (0-30 nM) decreases the MMP and increase ROS levels of HepG2 cells in a dose-dependent manner.TH-6 (7.5, 15, 30 nM; 48 h) inhibits cell migration and invasion in MDA-MB-231 cells and suppress the migration of HUVECs in a concentration-dependent manner.TH-6 shows favorable liver microsomal stability in vitro with t1/2 of 50.3 min.
TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity.
体内研究：
TH-6 (10, 20 mg/kg; i.v.; daily for 21 days) shows anti-tumor activity in mouse.TH-6 (20 mg/kg) shows antivascular activity and a good cardiovascular safety profile in mouse.Animal Model:4-5 weeks, 18-22 g female ICR mice (H22 allograft mouse model)
Dosage:10, 20 mg/kg
Administration:I.v.; daily for 21 days
Result:Reduced tumor weights at day 21 by 82% and did not affect body weight during treatment, indicating the low toxicity.
体外研究：
TH-6 (0-2 μM) shows antiproliferative activities in cancer cell lines and normal human lung cells.TH-6 (0-10 μM) inhibits tubulin polymerization with an IC50 value of 4.06 μM.TH-6 (0.03, 0.1, 0.3 1 μM; 24 h) increases the expression of Ac-α-Tubulin and AC-Histone H3 in HepG2 cells.TH-6 (7.5, 15, 30 nM) induces apoptosis and cell cycle arrest at G2/M phase.TH-6 (0-30 nM) decreases the MMP and increase ROS levels of HepG2 cells in a dose-dependent manner.TH-6 (7.5, 15, 30 nM; 48 h) inhibits cell migration and invasion in MDA-MB-231 cells and suppress the migration of HUVECs in a concentration-dependent manner.TH-6 shows favorable liver microsomal stability in vitro with t1/2 of 50.3 min.
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