AZD 7762 hydrochloride

Modify Date: 2024-01-08 23:43:52

AZD 7762 hydrochloride Structure
AZD 7762 hydrochloride structure
Common Name AZD 7762 hydrochloride
CAS Number 1246094-78-9 Molecular Weight 398.88
Density N/A Boiling Point N/A
Molecular Formula C17H20ClFN4O2S Melting Point N/A
MSDS USA Flash Point N/A
Symbol GHS05 GHS07
GHS05, GHS07
Signal Word Danger

 Use of AZD 7762 hydrochloride


AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.

 Names

Name azd7762
Synonym More Synonyms

 AZD 7762 hydrochloride Biological Activity

Description AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
Related Catalog
Target

Chk1:5 nM (IC50)

Chk2:5 nM (IC50)

In Vitro AZD-7762 hydrochloride 在体外是一种同样有效的 Chk1 和 Chk2 抑制剂。AZD-7762 hydrochloride 有效抑制 Chk1 和 Chk2,消除 DNA 损伤诱导的 S 和 G2 检查点,增强 NSC 613327 和 SKF 104864A 的功效,并调节下游检查点通路蛋白。AZD-7762 hydrochloride 有效抑制 cdc25C 肽的 Chk1 磷酸化,通过闪烁亲近测定法测量,IC50 为 5 nM。AZD-7762 hydrochloride 的 Ki 确定为 3.6 nM。动力学表征表明 AZD-7762 hydrochloride 结合在 Chk1 的 ATP 结合位点,并被认为以可逆方式直接竞争 ATP 结合。AZD-7762 hydrochloride 显示可消除喜树碱诱导的 G2 阻滞,平均 EC50 为 10 nM (n=12),最大消除范围为 100 nM[1]。
In Vivo 在大鼠 H460-DNp53 异种移植研究中,AZD-7762 hydrochloride(10 mg/kg 和 20 mg/kg)以剂量依赖性方式增强 NSC 613327 的抗肿瘤活性。即随着剂量增加,抑制率 (%T/C) 分别降低至 48% 和 32%。在与 CPT-11 联合的小鼠异种移植研究中,AZD-7762 hydrochloride 与 CPT-11 联合处理,可显著增加 CPT-11 活性,%T/C 分别显着增加至 -66% 和 -67%[1]。AZD7762 hydrochloride 与 CX-5461 联合使用,在体外和体内诱导 Tp53-null (Tp53-/-) Eμ-Myc 淋巴瘤细胞死亡[2]。
References

[1]. Zabludoff SD, et al. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol Cancer Ther. 2008 Sep;7(9):2955-66.  

[2]. Quin J, et al. Inhibition of RNA polymerase I transcription initiation by CX-5461 activates non-canonical ATM/ATR signaling. Oncotarget. 2016 Aug 2;7(31):49800-49818.  

 Chemical & Physical Properties

Molecular Formula C17H20ClFN4O2S
Molecular Weight 398.88
Exact Mass 398.09800
PSA 124.49000
LogP 4.82160
Storage condition -20°C

 Safety Information

Symbol GHS05 GHS07
GHS05, GHS07
Signal Word Danger
Hazard Statements H302-H318
Precautionary Statements P280-P305 + P351 + P338
RIDADR NONH for all modes of transport

 Synonyms

AZD7762 hydrochloride
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