产品
编 号：F286634
分子式：C33H29F6N3O5S
分子量：693.66
分子式：C33H29F6N3O5S
分子量：693.66
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规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2361659-61-0
产品详情
生物活性：
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM.
体内研究：
AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells.NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching Cmax 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h.Animal Model:C57Bl/6 mice injected with KPC2 cells
Dosage:50 mg/kg
Administration:Intraperitoneal injection; 5 days a week; for 1 month
Result:Significantly increased survival of mice.
体外研究：
AES-135 inhibits cancer cells growth with IC50 values of 2.3 μM, 1.4 μM, 0.27 μM, 0.94 μM, 1.9 μM, 2.72 μM, 2.1 μM, 15.0 μM, 1.6 μM and 19.2 μM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively.
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM.
体内研究：
AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells.NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching Cmax 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h.Animal Model:C57Bl/6 mice injected with KPC2 cells
Dosage:50 mg/kg
Administration:Intraperitoneal injection; 5 days a week; for 1 month
Result:Significantly increased survival of mice.
体外研究：
AES-135 inhibits cancer cells growth with IC50 values of 2.3 μM, 1.4 μM, 0.27 μM, 0.94 μM, 1.9 μM, 2.72 μM, 2.1 μM, 15.0 μM, 1.6 μM and 19.2 μM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively.
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