OTS964 hydrochloride
目录号 : KM3019 CAS No. : 1338545-07-5 纯度 : 98%

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。

规格 价格 是否有货 数量
2mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg 询价 In-stock

Other Forms of Rapamycin:

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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 Kd 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.

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

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.

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.
分子式
C23H26Cl2N2O2S
分子量
428.97
CAS号
1338545-07-5
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。-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。

  • 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。

  • 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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