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135897-06-2

中文名称 SB218078
英文名称 SB218078
CAS 135897-06-2
分子式 C24H15N3O3
分子量 393.39
MOL 文件 135897-06-2.mol
135897-06-2 结构式 135897-06-2 结构式

基本信息

中文别名
化合物 T16848
英文别名
SB218078 ?SB-218078
9,10,11,12-Tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione
9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione, 9,10,11,12-tetrahydro-
所属类别
生物化工:抑制剂

物理化学性质

熔点>340 °C
密度1.80±0.1 g/cm3(Predicted)
储存条件Store at RT
溶解度≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
酸度系数(pKa)9.75±0.20(Predicted)
形态结晶固体
颜色Light yellow to yellow

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335

常见问题列表

生物活性
SB-218078 是一种有效的,选择性,ATP 竞争性且细胞可渗透的检查点激酶 1 (Chk1) 抑制剂,可抑制 cdc25C 的 Chk1 磷酸化,IC50 为 15 nM。SB-218078 对 Cdc2 (IC50 为 250 nM) 和 PKC (IC50 为 1000 nM) 的抑制作用较弱。SB-218078 通过 DNA 损伤和细胞周期停滞诱导细胞凋亡。
靶点

Chk1

15 nM (IC 50 )

Cdc2

250 nM (IC 50 )

PKC

1000 nM (IC 50 )

Apoptosis

体外研究

SB-218078 (2.5-5 μM; 18 hours; HeLa cells) treatment abrogates G2 cell cycle arrest caused by either γ-irradiation or a topoisomerase I Topotecan inhibition.
SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage .

Cell Cycle Analysis

Cell Line: HeLa cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 18 hours
Result: Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition.

Cell Cytotoxicity Assay

Cell Line: HeLa and HT-29 cells
Concentration: 500 nM, 625 nM
Incubation Time: 96 hours
Result: Enhanced cytotoxicity of DNA damage.
体内研究

SB-218078 (5 mg/kg; intraperitoneal injection; for 16 hours; C57/Bl6 mice) treatment could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen in Myc-induced lymphomas mouse model.

Animal Model: C57/Bl6 mice injected with ARF -/- lymphomas
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; for 16 hours
Result: Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma.
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