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CP-466722 {[allProObj[0].p_purity_real_show]}

货号:A422631

CP-466722是一种强效且可逆的 ATM 抑制剂,对 ATR 无影响,且能抑制细胞中的 PI3K 或 PIKK 家族成员。

CP-466722 化学结构 CAS号:1080622-86-1
CP-466722 化学结构
CAS号:1080622-86-1
CP-466722 3D分子结构
CAS号:1080622-86-1
CP-466722 化学结构 CAS号:1080622-86-1
CP-466722 3D分子结构 CAS号:1080622-86-1
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CP-466722 纯度/质量文件 产品仅供科研

货号:A422631 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ATM ATR 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

DNA-PK,MLCK,PI3K 99%+
CP-466722 +

ATM, IC50: 410 nM

99%+
Torin 2 ++

ATM, EC50: 28 nM

++

ATR, EC50: 35 nM

mTOR,DNA-PK 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

96%
ETP-46464 +

ATM, IC50: 545 nM

+++

ATR, IC50: 14 nM

mTOR,DNA-PK 98%
CGK733 ++

ATM, IC50: 200 nM

++

ATR, IC50: 200 nM

99%+
AZD0156 99%+
Dactolisib +++

ATR, IC50: 21 nM

98+%
Ceralasertib ++++

ATR, IC50: 1 nM

99%+
Berzosertib +++

ATR, IC50: 19 nM

99%+
VE-821 +++

ATR, Ki: 13 nM

99%+
AZ20 ++++

ATR, IC50: 5 nM

mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

P-gp 98%
m-PEG25-NHS ester ++++

ATR, IC50: 7 nM

95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

CP-466722 生物活性

靶点
  • ATM

    ATM, IC50:410 nM

描述 CP-466722, a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.

CP-466722 细胞实验

Cell Line
Concentration Treated Time Description References
GBM12 cells 3 μM 14 days To evaluate the effect of CP-466722 on TMZ sensitivity, results showed that CP-466722 significantly sensitized GBM12 cells to TMZ J Neurooncol. 2012 Dec;110(3):349-57.
GBM12TMZ cells 3 μM 14 days To evaluate the effect of CP-466722 on TMZ sensitivity, results showed that CP-466722 had no significant effect on TMZ-resistant GBM12TMZ cells J Neurooncol. 2012 Dec;110(3):349-57.
HeLa cells 1-10 µM 30 min To evaluate the inhibitory effect of CP466722 on ATM kinase activity, the results showed that CP466722 almost completely inhibited ATM cellular activity at concentrations of 6μM and above. Cancer Res. 2008 Sep 15;68(18):7466-74.
MCF-7 cells 6μM 30 min To evaluate the inhibitory effect of CP466722 on ATM kinase activity, the results showed that CP466722 inhibited ATM-dependent phosphorylation events. Cancer Res. 2008 Sep 15;68(18):7466-74.
RH-luciferase (RH-luc) strain 0.702 µM 72 h To evaluate the inhibitory effect of CP-466722 on the growth of T. gondii, the results showed that CP-466722 had a dose-dependent inhibitory effect on the proliferation of T. gondii, with an IC50 value of 0.702 µM. Int J Mol Sci. 2024 Jun 25;25(13):6947.

CP-466722 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft model Intraperitoneal injection 10 mg/kg Once daily for 8 weeks Inhibition of ATM expression significantly reduced tumor metastasis in A549CisR cells. J Exp Clin Cancer Res. 2019 Apr 8;38(1):149
BALB/c mice T. gondii infection model Oral 20, 40, 60 mg/kg Once daily for 7 consecutive days To evaluate the protective effect of CP-466722 on T. gondii-infected mice, the results showed that CP-466722 had a slight protective effect on T. gondii-infected mice. Int J Mol Sci. 2024 Jun 25;25(13):6947.

CP-466722 参考文献

[1]Guo K, Shelat AA, et al. Development of a cell-based, high-throughput screening assay for ATM kinase inhibitors. J Biomol Screen. 2014 Apr;19(4):538-46.

[2]Rainey MD, Charlton ME, et al. Transient inhibition of ATM kinase is sufficient to enhance cellular sensitivity to ionizing radiation. Cancer Res. 2008 Sep 15;68(18):7466-74.

CP-466722 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.62mL

5.72mL

2.86mL

CP-466722 技术信息

CAS号1080622-86-1
分子式C17H15N7O2
分子量 349.35
SMILES Code NC1=NC(C2=NC=CC=C2)=NN1C3=C4C=C(OC)C(OC)=CC4=NC=N3
MDL No. MFCD17392566
别名
运输蓝冰
InChI Key ILBRKJBKDGCSCB-UHFFFAOYSA-N
Pubchem ID 44551660
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

DMSO: 1 mg/mL(2.86 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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