CGK733 - CAS:905973-89-9 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	CGK733
英文名称:	CGK733
别名:	ATM/ATR Kinase
CAS No:	905973-89-9	分子式:	C₂₃H₁₈Cl₃FN₄O₃S	分子量:	555.84
CAS No:	905973-89-9
分子式:	C₂₃H₁₈Cl₃FN₄O₃S
分子量:	555.84

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C10034 CGK733 ≥98% (HPLC) (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO (>5 mg/ml

产品描述：

基本信息

产品编号：C10034
产品名称：CGK733
CAS:	905973-89-9	储存条件	粉末	2-8℃	四年

分子式：	C23H18Cl3FN4O3S		溶于液体	-80℃	两年
分子量	555.84			-20℃	一个月
化学名：	2,2-Diphenyl-N-(2,2,2-trichloro-1-(3-(4-fluoro-3-nitrophenyl)thioureido)ethyl)acetamide
Solubility (25°C)	体外	DMSO	100mg/mL (179.9mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内	现配现用
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.7991mL	8.9954mL	17.9908mL
5mM	0.3598mL	1.7991mL	3.5982mL
10mM	0.1799mL	0.8995mL	1.7991mL
50mM	0.0360mL	0.1799mL	0.3598mL

生物活性

产品描述

一种有效的ATM/ATR选择性抑制剂。

靶点/IC₅₀

ATM

200nM

ATR

200nM

体外研究

CGK733 (4.2ng/μL-12.5ng/μL) enhances taxol-induced cytotoxicity in HBV-positive HCC cells. CGK733 (4.2ng/μL)accelerates the formation of multinucleated cells and promotes the exit of mitosis in taxol-treated HBV-positive HCC cells.

CGK733 (10μM) causes the loss of cyclin D1 through the ubiquitin-dependent proteasomal degradation pathway in MCF-7 and T47D breast cancer cell lines. CGK733 (0.6-40μM) shows inhibitory activities against proliferation of LnCap prostate cancer cells, HCT116 colon cancer cells, MCF-7 and T47D estrogen receptor positive breast cancer cells, and MDA-MB436 ER negative breast cancer cells. Moreover, CGK733 inhibits proliferation of non-transformed mouse BALB/c 3T3 embryonic fibroblast cells. In addition, CGK733 (10μM) inhibits MCF-7 proliferation, and the effect can not be suppressed by pancaspase inhibition. CGK733 (10μM) results in 1.6-fold increase in ATM reporter activity in HEK-293 cells

体内研究

CGK733 (25 mg/kg, i.p.) increases the ATM reporter activity (reports inactivation of ATM kinase activity) compared to control mice, with 2.4-fold, 3.1-fold, and 1.3-fold changes at 1, 4, and 8 hours, respectively.

推荐实验方法(仅供参考)

细胞实验：

Cell Assay

Cells are seeded in 96-well plates at a predetermined optimal cell density to ensure exponential growth for duration of the assay. After a 24 h preincubation, growth medium is replaced with experimental medium containing the appropriate drug concentrations or 0.1% (v/v) vehicle control. After a 48 h incubation, cell proliferation is estimated using the sulforhodamine B colorimetric assay and expressed as the mean ± SE for six replicates as a percentage of vehicle control (taken as 100%). Experiments are performed independently at least three times. Statistical analyses are performed using a two-tailed Student's t test. P < 0.05 is considered to be statistically significant.

动物实验:

Animal Administration

Four to six weeks old athymic CD-1 female mice are acclimatized for at least one week before use. The mice are injected subcutaneously with 2×106 D54-ATMR cells in each flank. Tumors are allowed to grow to the size of 100-150 mm3. Mice are injected intraperitoneally with vehicle control (DMSO), CGK-733, KU-55933 (25mg/kg) or irradiated with 5 Gy to each flank. Bioluminescence is acquired on Xenogen IVIS Spectrum system after injecting 400μg/100μL of D-luciferin at baseline (-3h) as well as 1, 4, and 8 hours after drug administration.

保存条件：

2-8℃

UN码：

HazardClass：

危害声明：

安全说明：

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