SB218078
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- CAS号:
- 135897-06-2
- 英文名:
- SB218078
- 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-
- 中文名:
- SB218078
- 中文别名:
- 化合物 T16848
- CBNumber:
- CB51075435
- 分子式:
- C24H15N3O3
- 分子量:
- 393.39
- MOL File:
- 135897-06-2.mol
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SB218078化学性质
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熔点:
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>340 °C
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密度:
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1.80±0.1 g/cm3(Predicted)
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储存条件:
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Store at RT
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溶解度:
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≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
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形态:
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crystalline solid
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酸度系数(pKa):
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9.75±0.20(Predicted)
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SB218078性质、用途与生产工艺
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。
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Chk1
15 nM (IC
50
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Cdc2
250 nM (IC
50
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PKC
1000 nM (IC
50
)
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Apoptosis
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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
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Cell Line:
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HeLa cells
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Concentration:
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2.5 μM, 5 μM
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Incubation Time:
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18 hours
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Result:
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Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition.
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Cell Cytotoxicity Assay
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Cell Line:
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HeLa and HT-29 cells
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Concentration:
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500 nM, 625 nM
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Incubation Time:
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96 hours
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Result:
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Enhanced cytotoxicity of DNA damage.
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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.
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Animal Model:
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C57/Bl6 mice injected with ARF
-/-
lymphomas
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Dosage:
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5 mg/kg
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Administration:
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Intraperitoneal injection; for 16 hours
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Result:
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Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma.
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SB218078
上下游产品信息
上游原料
下游产品
135897-06-2, SB218078 相关搜索:
- 对照品
- 化合物 T16848
- 135897-06-2
- 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-
- 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