CCT241533 hydrochloride

目录号: HY-14715B 纯度: 99.51%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

CCT241533 hydrochloride是有效，选择性的 CHK2 抑制剂，IC₅₀ 和 K_i 分别为 3 nM 和 1.16 nM。

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CCT241533 hydrochloride Chemical Structure

CAS No. : 1431697-96-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1470	In-stock
2 mg	￥930	In-stock
5 mg	￥1395	In-stock
10 mg	￥2660	In-stock
50 mg	现货	询价
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of CCT241533 hydrochloride:

CCT241533 dihydrochloride 询价
CCT241533 询价

MCE 顾客使用本产品发表的 4 篇科研文献

CCT241533 hydrochloride 相关产品

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Chk1 Chk2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC₅₀ of 3 nM and a K_i of 1.16 nM^[1].

IC₅₀ & Target^[1]

Chk2

3 nM (IC₅₀)

Chk1

245 nM (IC₅₀)

Chk2

1.16 nM (Ki)

体外研究
(In Vitro)

CCT241533 hydrochloride inhibits CHK2 with an IC₅₀ of 3 nM and shows minimal cross reactivity against a panel of kinases at 1 μM. X-ray crystallography confirms that CCT241533 binds to CHK2 in the ATP pocket. CCT241533 blocks CHK2 activity in human tumor cell lines in response to DNA damage, as demonstrated by inhibition of CHK2 autophosphorylation at S516, band-shift mobility changes and HDMX degradation. CCT241533 does not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. However, CCT241533 significantly potentiates the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of the pS516 CHK2 signal is seen with a PARP inhibitor alone and this activation is abolished by CCT241533. The cytotoxicity of CCT241533 in HT-29, HeLa and MCF-7, measured as the growth inhibitory IC₅₀(GI₅₀) by SRB assay, is 1.7, 2.2 and 5.1 μM, respectively^[1]. CCT241533 hydrochloride is a potent CHK2 inhibitor (IC₅₀=3 nM), with selectivity (63-fold) over CHK1(IC₅₀=190 nM) and low hERG inhibition (IC₅₀=22 μM)^[2].

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

分子量

478.94

Formula

C₂₃H₂₈ClFN₄O₄

CAS 号

1431697-96-9

性状

固体

颜色

White to light yellow

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

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (208.79 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 33.33 mg/mL (69.59 mM; 超声助溶)

* "≥" 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	2.0879 mL	10.4396 mL	20.8793 mL
5 mM	0.4176 mL	2.0879 mL	4.1759 mL
10 mM	0.2088 mL	1.0440 mL	2.0879 mL

查看完整储备液配制表

* 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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.22 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.22 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.22 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。
方案四

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.22 mM); 澄清溶液
方案五

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.22 mM); 澄清溶液

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.51%

选择批次：

Data Sheet (628 KB) SDS (252 KB)

COA (200 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Anderson VE, et al. CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72. [Content Brief]

[2]. Caldwell JJ, et al. Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J Med Chem. 2011 Jan 27;54(2):580-90. [Content Brief]

Cell Assay ^[1]	HT-29, HeLa and MCF-7 cells are exposed to a fixed concentration (GI₅₀) of CCT241533 in combination with increasing concentrations of either PARP inhibitor or cytotoxic drug in a 96 hour SRB assay or 7-10 day colony forming assay. The ability of CCT241533 to enhance cell killing is expressed as a potentiation index (PI) which is the ratio of GI₅₀ for the genotoxic or PARP inhibitor alone: GI₅₀ for the genotoxic or PARP inhibitor in combination with a CHK2 inhibitor. Thus PI>1 indicates potentiation and PI<1 indicates protection^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Anderson VE, et al. CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72. [Content Brief] [2]. Caldwell JJ, et al. Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J Med Chem. 2011 Jan 27;54(2):580-90. [Content Brief]

Cell Assay
^[1]

HT-29, HeLa and MCF-7 cells are exposed to a fixed concentration (GI₅₀) of CCT241533 in combination with increasing concentrations of either PARP inhibitor or cytotoxic drug in a 96 hour SRB assay or 7-10 day colony forming assay. The ability of CCT241533 to enhance cell killing is expressed as a potentiation index (PI) which is the ratio of GI₅₀ for the genotoxic or PARP inhibitor alone: GI₅₀ for the genotoxic or PARP inhibitor in combination with a CHK2 inhibitor. Thus PI>1 indicates potentiation and PI<1 indicates protection^[1].

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

参考文献

[1]. Anderson VE, et al. CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72. [Content Brief]

[2]. Caldwell JJ, et al. Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J Med Chem. 2011 Jan 27;54(2):580-90. [Content Brief]

CCT241533 hydrochloride 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.0879 mL	10.4396 mL	20.8793 mL	52.1981 mL
	5 mM	0.4176 mL	2.0879 mL	4.1759 mL	10.4396 mL
	10 mM	0.2088 mL	1.0440 mL	2.0879 mL	5.2198 mL
	15 mM	0.1392 mL	0.6960 mL	1.3920 mL	3.4799 mL
	20 mM	0.1044 mL	0.5220 mL	1.0440 mL	2.6099 mL
	25 mM	0.0835 mL	0.4176 mL	0.8352 mL	2.0879 mL
	30 mM	0.0696 mL	0.3480 mL	0.6960 mL	1.7399 mL
	40 mM	0.0522 mL	0.2610 mL	0.5220 mL	1.3050 mL
	50 mM	0.0418 mL	0.2088 mL	0.4176 mL	1.0440 mL
	60 mM	0.0348 mL	0.1740 mL	0.3480 mL	0.8700 mL
DMSO	80 mM	0.0261 mL	0.1305 mL	0.2610 mL	0.6525 mL
DMSO	100 mM	0.0209 mL	0.1044 mL	0.2088 mL	0.5220 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CCT2415331431697-96-9CCT 241533CCT-241533Checkpoint Kinase (Chk)Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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营业执照（三证合一）

CCT241533 hydrochloride

Customer Review

Other Forms of CCT241533 hydrochloride:

MCE 顾客使用本产品发表的 4 篇科研文献