产品
编 号：F756883
分子式：C23H20ClN7O2
分子量：461.9
分子式：C23H20ClN7O2
分子量：461.9
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CAS No: 2921948-27-6
产品详情
生物活性：
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer.
体内研究：
HDAC-IN-53 (60 或 120 mg/kg; 灌胃给药; 每日一次; 持续 15 天) 通过直接肿瘤生长抑制和间接免疫细胞介导的抗肿瘤作用发挥抗肿瘤活性。 Pharmacokinetic Parameters of HDAC-IN-53 in Mice.IV (5 mg/kg) PO (20 mg/kg)
Tmax (h)0.42
Cmax (ng/mL)81299558
AUC0-t (ng/mL?h)586415278
t1/2 (h)0.852.49
F (%)65.1%
Animal Model:C57BL/6 Mice or athymic nude mice (female, 6-8 weeks old) with MC38 cells
Dosage:60 or 120 mg/kg
Administration:PO; daily for 15 days
Result:Yielded TGI values of 60.3 and 87.6%, respectively. Increased the percentage of CD4+ T cells.
体外研究：
HDAC-IN-53 (化合物 19h) 对一组癌细胞系具有良好的抗增殖活性，例如 MC38 (IC50=0.66 μM)、HCT116 细胞 (IC50=0.56 μM)。 HDAC-IN-53 (0.1-1 μM; 24 小时) 在 MC38 细胞中引起 G0/G1 细胞周期停滞，在 HCT116 细胞中诱导 G2/M 细胞周期停滞。 HDAC-IN-53 (0.1-1 μM; 24 小时) 以剂量依赖的方式上调 cleaved caspase-3 和 cleaved PARP 的表达。
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer.
体内研究：
HDAC-IN-53 (60 或 120 mg/kg; 灌胃给药; 每日一次; 持续 15 天) 通过直接肿瘤生长抑制和间接免疫细胞介导的抗肿瘤作用发挥抗肿瘤活性。 Pharmacokinetic Parameters of HDAC-IN-53 in Mice.IV (5 mg/kg) PO (20 mg/kg)
Tmax (h)0.42
Cmax (ng/mL)81299558
AUC0-t (ng/mL?h)586415278
t1/2 (h)0.852.49
F (%)65.1%
Animal Model:C57BL/6 Mice or athymic nude mice (female, 6-8 weeks old) with MC38 cells
Dosage:60 or 120 mg/kg
Administration:PO; daily for 15 days
Result:Yielded TGI values of 60.3 and 87.6%, respectively. Increased the percentage of CD4+ T cells.
体外研究：
HDAC-IN-53 (化合物 19h) 对一组癌细胞系具有良好的抗增殖活性，例如 MC38 (IC50=0.66 μM)、HCT116 细胞 (IC50=0.56 μM)。 HDAC-IN-53 (0.1-1 μM; 24 小时) 在 MC38 细胞中引起 G0/G1 细胞周期停滞，在 HCT116 细胞中诱导 G2/M 细胞周期停滞。 HDAC-IN-53 (0.1-1 μM; 24 小时) 以剂量依赖的方式上调 cleaved caspase-3 和 cleaved PARP 的表达。
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