OTS964 hydrochloride|cas:1338545-07-5|西域试剂

OTS964 hydrochloride,99.32%

产品编号：Bellancom-12467| CAS NO：1338545-07-5| 分子式：C₂₃H₂₅ClN₂O₂S| 分子量：428.97

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货号	价格	库存与货期
Bellancom-12467	￥1100.00	杭州北京（现货）
Bellancom-12467	￥1600.00	杭州北京（现货）
Bellancom-12467	￥2600.00	杭州北京（现货）
Bellancom-12467	￥4800.00	杭州北京（现货）
Bellancom-12467	￥8800.00	杭州北京（现货）

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OTS964 hydrochloride

产品介绍

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 K_d 值为 40 nM。

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. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K_d of 40 nM.

体外研究

OTS964 hydrochloride (10 nM; 48 hours) suppresses cancer cell proliferation.
OTS964 hydrochloride (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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

Apoptosis Analysis

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

Western Blot Analysis

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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

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：

——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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。