CCT 241533 盐酸盐
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- CAS号:
- 1431697-96-9
- 英文名:
- CCT 241533 hydrochloride
- 英文别名:
- CCT241533 HCl;CCT 241533 hydrochloride;CCT-241533 hydrochloride;CCT241533 (hydrochloride);CCT-241533 HYDROCHLORIDE; CCT 241533 HYDROCHLORIDE;rel-4-Fluoro-2-(4-(((3R,4S)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl)amino)-6,7-dimethoxyquinazolin-2-yl)phenol hydrochloride;(3R,4S)-rel-4-[[2-(5-Fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl]amino]-alpha,alpha-dimethyl-3-pyrrolidinemethanol hydrochloride (1:1)
- 中文名:
- CCT 241533 盐酸盐
- 中文别名:
- CHK2抑制剂;化合物 T10718L;CCT 241533 盐酸盐;REL-4-氟-2-(4-(((3R,4S)-4-(2-羟基丙烷-2-基)吡咯烷-3-基)氨基)-6,7-二甲氧基喹唑啉-2-基)苯酚盐酸盐
- CBNumber:
- CB42666608
- 分子式:
- C23H28ClFN4O4
- 分子量:
- 478.9442232
- MOL File:
- 1431697-96-9.mol
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CCT 241533 盐酸盐化学性质
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溶解度:
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Soluble in DMSO
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形态:
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A crystalline solid
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颜色:
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White to light yellow
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CCT 241533 盐酸盐性质、用途与生产工艺
CCT241533 hydrochloride是有效，选择性的 CHK2 抑制剂，IC50 和 Ki 分别为 3 nM 和 1.16 nM。
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Chk2
3 nM (IC
50
)
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Chk1
245 nM (IC
50
)
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Chk2
1.16 nM (Ki)
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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).
CCT 241533 盐酸盐
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-14715B | CCT 241533 盐酸盐
CCT241533 hydrochloride | 1431697-96-9 | 2mg | 930元 |
| 2024/08/19 | HY-14715B | CCT 241533 盐酸盐
CCT241533 hydrochloride | 1431697-96-9 | 5mg | 1395元 |
1431697-96-9, CCT 241533 盐酸盐 相关搜索:
- 对照品
- 细胞生物学试剂
- C23H28ClFN4O4
- C23H27FN4O4HCl
- REL-4-氟-2-(4-(((3R,4S)-4-(2-羟基丙烷-2-基)吡咯烷-3-基)氨基)-6,7-二甲氧基喹唑啉-2-基)苯酚盐酸盐
- 化合物 T10718L
- CHK2抑制剂
- CCT 241533 盐酸盐
- 1431697-96-9
- rel-4-Fluoro-2-(4-(((3R,4S)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl)amino)-6,7-dimethoxyquinazolin-2-yl)phenol hydrochloride
- CCT-241533 HYDROCHLORIDE; CCT 241533 HYDROCHLORIDE
- CCT241533 HCl
- (3R,4S)-rel-4-[[2-(5-Fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl]amino]-alpha,alpha-dimethyl-3-pyrrolidinemethanol hydrochloride (1:1)
- CCT-241533 hydrochloride
- CCT241533 (hydrochloride)
- CCT 241533 hydrochloride