CDK12-IN-E9 - CAS:2020052-55-3

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CDK12-IN-E9

目录号 : KM6104 CAS No. : 2020052-55-3 纯度 : 98%

Data Sheet 产品使用指南

CDK12-IN-E9 是一种有效的选择性共价 CDK12 抑制剂和非共价 CDK9 抑制剂，同时避免了 ABC 转运蛋白介导的外排。CDK12-IN-E9 对 CDK7/CyclinH 复合物的结合能力较弱，IC₅₀ > 1 μM。

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500mg	询价	In-stock

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生物活性

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC₅₀> 1 μM.

体外研究

CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1 NB and lung cancer cells, with IC₅₀ values ranging from 8 to 40 nM.
CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1 NB and lung cancer models, accompanied by decreased MYC and MCL1 expression.
CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1 lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9.

Cell Proliferation Assay

Cell Line:	Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells
Concentration:	10 nM-10 μM
Incubation Time:	72 hours
Result:	Showed potent antiproliferative activity in THZ1 NB and lung cancer cells, with IC₅₀ values ranging from 8 to 40 nM.

Western Blot Analysis

Cell Line:	Kelly, PC-9, and NCI-H82 cells
Concentration:	0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM
Incubation Time:	6 hours
Result:	Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1 NB and lung cancer models.

分子式

C₂₄H₃₀N₆O₂

分子量

434.53

CAS号

2020052-55-3

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 : 125 mg/mL (287.67 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3013 mL	11.5067 mL	23.0134 mL
5 mM	0.4603 mL	2.3013 mL	4.6027 mL
10 mM	0.2301 mL	1.1507 mL	2.3013 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 90% corn oil
Solubility: ≥ 20.83 mg/mL (47.94 mM); Clear solution

此方案可获得 ≥ 20.83 mg/mL (47.94 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 208.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.79 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。

纯度： 98%

Data Sheet

产品使用指南

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