[登录] [免费注册]
试剂仪器网
位置:首页 > 资料中心 > 化工字典 > 905973-89-9
关键词:       仅模糊查询
CAS: 905973-89-9
分子式: C23H18Cl3FN4O3S
分子量: 555.84
英文名称: 
cgk733
2,2-diphenyl-n-(2,2,2-trichloro-1-[3-(4-fluoro-3-nitrophenyl)thioureido]ethyl)acetamide
用途: CGK733是ATM/ATR选择性抑制剂,IC50为200 nM。
推荐供应商
货号品牌产品名称规格包装、参考价格
C793159MACKLINCGK73310mM in DMSO620元/1ml;   咨询
储存:-20°C
C860859MACKLINCGK73398%367元/10mg;   1060元/50mg;   2050元/100mg;   咨询
储存:-20℃
状态:浅黄色固体
折射率:light yellow solid
1564012J&KCGK73398%, 一种有效的 ATM/ATR 抑制剂1029元/10MG;   3291元/50MG;   咨询

基本信息

分子式C23H18Cl3FN4O3S
分子量555.84
存储条件Freezer -20℃

产品描述

CGK 733是一种有效的ATM/ATR选择性抑制剂,IC50约为200 nM。

靶点(IC50 & Targe)

ATM

ATR

体外研究

CGK 733能够使已经停止增殖的衰老细胞强劲生长。CGK 733处理的细胞中,与衰老相关的β-半乳糖苷酶(SA–β-gal)活性消失。CGK 733比LY294002(抑制ATM 和 ATR,IC50约为5 μM)更有效抑制ATM/ATR(IC50〜5微米ATM和ATR),是PI3K和PIKKs的泛抑制剂。[1] CGK 733 (30 μM)处理衰老的MCF-7细胞24小时,造成约60%细胞死亡。[2]CGK 733(20μM)作用于MCF-7和 T47D乳腺癌细胞系,通过泛素-蛋白酶体降解途径,诱导cyclin D1损失。CGK 733浓度范围为0.6-40 μM时,抑制MCF-7 和 T47D 雌激素受体 (ER) 阳性的乳腺癌细胞, MDA-MB436 ER 阴性的乳腺癌细胞, LnCap前列腺癌细胞,和 HCT116结肠癌细胞增殖。此外,CGK 733也抑制非转化的小鼠BALB/c 3T3胚胎成纤维细胞增殖。CGK 733-介导的抑制增殖作用是剂量依赖性的,剂量低至2.5 μM效果显著。[3]

细胞实验

Cell lines: 人类乳腺癌细胞 MCF-7

Concentrations: ~20 μM

Incubation Time: 2 天

Method: 细胞按预定的最佳细胞密度接种于96孔板中,确保在实验期间细胞呈指数生长状态。预温育24小时后,使用含适当浓度药物,或0.1% (v/v) 空白对照的实验培养基更换生长培养基。培养48小时后,使用Sulforhodamine B比色法测评细胞增殖。

(Only for Reference)

参考文献

[1] Won J, et al. Nat Chem Biol, 2006, 2(7), 369-374.

[2] Crescenzi E, et al. Clin Cancer Res, 2008, 14(6), 1877-1887.

[3] Alao JP, et al. Radiat Oncol, 2009, 4:51.

安全信息

图形或危害标志
提示语Warning
危险说明H302
H410
防范说明P264
P270
P273
P301+P312
P330
P391
P501
UN号码3077
危险分类9
包装等级III
118501Sigma-AldrichATM/ATR Kinase Inhibitor-CAS 905973-89-9-CalbiochemThe ATM/ATR Kinase Inhibitor, also referenced under CAS 905973-89-9, controls the biological activity of ATM/ATR Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Depho3806.77元/5 MG;   咨询

产品说明

一般描述

A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC50 = ~200 nM) without significant effect against other PIKK family members (PI 3-K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI 3-K/PDK1/Akt signaling pathway.
A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC50 ~ 200 nM) without significant effect against other PIKK family members (PI3K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI3K-PDK1-Akt signaling pathway.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
ATM/ATR
Product does not compete with ATP.
Reversible: no
Target IC50: ~200 nM against ATM and ATR

警告

Toxicity: Irritant (B)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Goldstein, M., et al. 2008. Toxicol. Appl. Pharmacol.in press.
Crescenzi, E., et al. 2008. Clin. Cancer Res.14, 1877.
Cruet-Hennequart, S., et al. 2008. DNA Repair7, 582.
Won, J., et al. 2006. Nat. Chem. Biol.2, 369. (RETRACTED)

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C23H18Cl3FN4O3S
分子量555.84

产品性质

质量水平100
测定≥95% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色pale yellow
溶解性DMSO: 5 mg/mL
运输ambient
储存温度2-8℃
InChI1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
InChI keyHLCDNLNLQNYZTK-UHFFFAOYSA-N

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
C9867Sigma-AldrichCGK733≥98% (HPLC), solid1445.69元/5 MG;   咨询

产品说明

包装

5 mg in glass bottle

生化/生理作用

Originally published as a selective ataxia telangiectasia-mutated (ATM) and ATM- and Rad3-related (ATR) kinase inhibitor, which causes reversible reprogramming of cellular lifespan, conferred robust growth to senescent cells that had ceased proliferation.

基本信息

经验(实验)分子式C23H18Cl3FN4O3S
分子量555.84
MDL编号MFCD09038682
PubChem化学物质编号24724454
NACRESNA.77

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
颜色 off-white
溶解性DMSO: >5 mg/mL
储存温度2-8℃
SMILES string[O-][N+](=O)c1cc(NC(=S)NC(NC(=O)C(c2ccccc2)c3ccccc3)C(Cl)(Cl)Cl)ccc1F
InChI1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
InChI keyHLCDNLNLQNYZTK-UHFFFAOYSA-N

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
CAS号首数字顺序排列: 1 2 3 4 5 6 7 8 9