生物活性
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM[1]. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2].
体外研究(In Vitro)
OTS964 hydrochloride (10 nM; 48 hours) suppresses cancer cell proliferation[1].
OTS964 hydrochloride (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].
体内研究(In Vivo)
OTS964 hydrochloride (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 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately 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.
分子量
428.97
性状
Solid
Formula
C23H25ClN2O2S
CAS 号
1338545-07-5
运输条件
Room temperature in continental US; may vary elsewhere.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.3312 mL 11.6558 mL 23.3117 mL
5 mM 0.4662 mL 2.3312 mL 4.6623 mL
10 mM 0.2331 mL 1.1656 mL 2.3312 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: