基本属性 生物活性靶点体外研究 用途与合成方法 供应商 供应信息
网站主页  化工产品目录 生物化工  生化试剂  激动剂抑制剂  (3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇

(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇

(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇

英文名称:CCT241533
CAS号:1262849-73-9
分子式:C23H27FN4O4
分子量:442.4832832
EINECS号:200-258-5
Mol文件:1262849-73-9.mol
(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇 结构式

(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇 性质

沸点 569.4±50.0 °C(Predicted)
密度 1.327
储存条件 Store at -20°C
溶解度 溶于二甲基亚砜
形态 结晶固体
酸度系数(pKa) 8.18±0.48(Predicted)

(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇 用途与合成方法

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

Chk2

3 nM (IC 50 )

Chk1

245 nM (IC 50 )

Chk2

1.16 nM (Ki)

CCT241533 hydrochloride inhibits CHK2 with an IC 50 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 IC 50 (GI 50 ) by SRB assay, is 1.7, 2.2 and 5.1 μM, respectively. CCT241533 hydrochloride is a potent CHK2 inhibitor (IC 50 =3 nM), with selectivity (63-fold) over CHK1(IC 50 =190 nM) and low hERG inhibition (IC 50 =22 μM).

(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇供应商 更多

上海佰世凯化学科技有限公司
联系电话:021-20908456
产品介绍:
英文名称:CCT 241533
CAS:1262849-73-9
备注:C14422
四川省维克奇生物科技有限公司
联系电话:028-81700200 18116577057
产品介绍:
英文名称:CCT241533
CAS:1262849-73-9
纯度:HPLC≥98%
包装信息:20mg/10
广州和为医药科技有限公司
联系电话: 18620099427
产品介绍:
英文名称:CCT241533
CAS:1262849-73-9
包装信息:1MG;2.5MG;5MG;10MG;25MG
成都点纯科技有限公司
联系电话:400-1166-196 18502815961
产品介绍:
中文名称:(3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-ALPHA,ALPHA-二甲基-3-吡咯烷甲醇
英文名称:CCT241533
CAS:1262849-73-9
纯度:99% HPLC
包装信息:10g;50g;100g;500g;1kg;5kg;25kg
上海源溪生物科技有限公司
联系电话:021-58447131 13564518121
产品介绍:
英文名称:CCT241533
CAS:1262849-73-9
纯度:98% HPLC
包装信息:100mg,250mg,1g

最新发布供应信息

CCT241533
四川省维克奇生物科技有限公司 2024-03-25