CCT241533
作者：齐岳
发布时间：2023-09-13
16:51:31
点击数：
产品名称：CCT241533
产品描述：
| 产品描述 | CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM). |
| 靶点活性 | Chk1:245 nM, Chk2:3 nM |
| 体外活性 | CCT241533 inhibits CHK2 (IC50: 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. 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. In HT-29, HeLa, and MCF-7, the cytotoxicity of CCT241533 (GI50) is 1.7, 2.2, and 5.1 μM, respectively [1]. CCT241533 hydrochloride is a potent CHK2 inhibitor (IC50: 3 nM), with selectivity (63-fold) over CHK1(IC50: 190 nM) and low hERG inhibition (IC50: 22 μM) [2]. |
| 分子量 | 442.491 |
| 分子式 | C23H27FN4O4 |
| CAS No. | 1262849-73-9 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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