OTS964 hydrochloride 是一种口服有效的，高亲和力和选择性的TOPK(T 淋巴因子激活的杀伤细胞起源的蛋白激酶) 抑制剂，IC50为 28 nM。OTS964 hydrochloride 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 hydrochloride is an orally active, high affinity and selectiveTOPK(T-lymphokine-activated killer cell-originated protein kinase) inhibitor with anIC50of 28 nM[1]. OTS964 hydrochloride is also a potent inhibitor of thecyclin-dependent kinaseCDK11, which binds to CDK11B with aKdof 40 nM[2]. |
| IC50& Target[1][2] | TOPK 28 nM (IC50) | CDK11B 40 nM (Kd) |
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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].
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. |
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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. |
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 83.33 mg/mL(194.26 mM) H2O : 1.43 mg/mL(3.33 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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