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OTS964
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。
OTS964图片
CAS NO:1338542-14-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
OTS964 是一种口服有效的,高亲和力和选择性的TOPK抑制剂,IC50为 28 nM。OTS964 也是一种有效的细胞周期蛋白依赖激酶CDK11抑制剂,结合 CDK11B 的Kd值为 40 nM。
生物活性

OTS964 is an orally active, high affinity and selectiveTOPKinhibitor with anIC50of 28 nM[1]. OTS964 is also a potent inhibitor of thecyclin-dependent kinaseCDK11, which binds to CDK11B with aKdof 40 nM[2].

IC50& Target[1][2]

CDK11B

40 nM (Kd)

TOPK

28 nM (IC50)

体外研究
(In Vitro)

OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation[1].
OTS964 (10 nM; 48 hours) increases cancer cell death[1].
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[3].

Cell Proliferation Assay[1]

Cell Line:LU-99 cells
Concentration:10 nM
Incubation Time:48 hours
Result:Suppressed cancer cell proliferation.

Apoptosis Analysis[1]

Cell Line:LU-99 cells
Concentration:10 nM
Incubation Time:48 hours
Result:Increased cancer cell death.

Western Blot Analysis[3]

Cell Line:Hs683 cells, H4 cells
Concentration:0.1, 1, 2 μM
Incubation Time:24 and 48 hours
Result:Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner.
体内研究
(In Vivo)

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[1].
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression[1].

Animal Model:Nude mice bearing LU-99 lung cancer cells[1]
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[1]
Dosage:50 or 100 mg/kg
Administration:Oral administration; once every day for 2 weeks
Result:Achieved complete tumor regression.
分子量

392.51

Formula

C23H24N2O2S

CAS 号

1338542-14-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.