产品
编 号：F624518
分子式：C23H24N2O2S
分子量：392.51
分子式：C23H24N2O2S
分子量：392.51
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CAS No: 1338542-14-5
产品详情
生物活性：
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
体内研究：
OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression. OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression.Animal Model:Nude mice bearing LU-99 lung cancer cells
Dosage:40 mg/kg
Administration:Intravenously; on days 1, 4, 8, 11, 15, and 18
Result:The tumors continued shrinking even after the treatment and finally revealed complete regression.
Animal Model:Nude mice bearing LU-99 lung cancer cells
Dosage:50 or 100 mg/kg
Administration:Oral administration; once every day for 2 weeks
Result:Achieved complete tumor regression.
体外研究：
OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation. OTS964 (10 nM; 48 hours) increases cancer cell death. OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner.
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
体内研究：
OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression. OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression.Animal Model:Nude mice bearing LU-99 lung cancer cells
Dosage:40 mg/kg
Administration:Intravenously; on days 1, 4, 8, 11, 15, and 18
Result:The tumors continued shrinking even after the treatment and finally revealed complete regression.
Animal Model:Nude mice bearing LU-99 lung cancer cells
Dosage:50 or 100 mg/kg
Administration:Oral administration; once every day for 2 weeks
Result:Achieved complete tumor regression.
体外研究：
OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation. OTS964 (10 nM; 48 hours) increases cancer cell death. OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner.
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