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1431697-96-9

中文名稱(chēng) CCT 241533 鹽酸鹽
英文名稱(chēng) CCT 241533 hydrochloride
CAS 1431697-96-9
分子式 C23H28ClFN4O4
分子量 478.944
MOL 文件 1431697-96-9.mol
更新日期 2024/11/12 15:28:21
1431697-96-9 結(jié)構(gòu)式 1431697-96-9 結(jié)構(gòu)式

基本信息

中文別名
CHK2抑制劑
CCT 241533 鹽酸鹽
英文別名
CCT241533 HCl
CCT 241533 hydrochloride
CCT-241533 hydrochloride
CCT241533 (hydrochloride)
CCT-241533 HYDROCHLORIDE
CCT 241533 HYDROCHLORIDE
(3R,4S)-rel-4-[[2-(5-Fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl]amino]-alpha,alpha-dimethyl-3-pyrrolidinemethanol hydrochloride (1:1)
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

溶解度溶于二甲基亞砜
形態(tài)A crystalline solid
顏色White to light yellow
CCT 241533 鹽酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-14715BCCT 241533 鹽酸鹽
CCT241533 hydrochloride
1431697-96-92mg930元
2024/11/08HY-14715BCCT 241533 鹽酸鹽
CCT241533 hydrochloride
1431697-96-95mg1395元
2024/11/08HY-14715BCCT 241533 鹽酸鹽
CCT241533 hydrochloride
1431697-96-910mM * 1mLin DMSO1470元

常見(jiàn)問(wèn)題列表

生物活性
CCT241533 hydrochloride是有效,選擇性的 CHK2 抑制劑,IC50 和 Ki 分別為 3 nM 和 1.16 nM。
靶點(diǎn)

Chk2

3 nM (IC 50 )

Chk1

245 nM (IC 50 )

Chk2

1.16 nM (Ki)

體外研究

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).

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