CGP 52411
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- CAS号:
- 145915-58-8
- 英文名:
- DAPH
- 英文别名:
- DAPH-1
(DAPH;DAPH/CGP 52411;DAPH >=98% (HPLC), solid;1H-Isoindole-1,3(2H)-dione, 5,6-bis(phenylamino)-;4,5-Dianilinophthalimide, 5,6-Bis(phenylamino)-1H-isoindole-1,3(2H)-dione, CGP 52411
- 中文名:
- CGP 52411
- 中文别名:
- 化合物 T10782;化合物CGP52411;C275419] CGP 52411,EGFR的抑制剂;5,6-双(苯基氨基)-1H-异吲哚-1,3(2H)-二酮
- CBNumber:
- CB2498023
- 分子式:
- C20H15N3O2
- 分子量:
- 329.35
- MOL File:
- 145915-58-8.mol
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CGP 52411化学性质
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熔点:
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199-202℃
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密度:
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1.374
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储存条件:
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2-8°C
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溶解度:
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DMSO: ~30 mg/mL
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酸度系数(pKa):
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9.06±0.20(Predicted)
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形态:
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solid
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颜色:
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orange
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CGP 52411性质、用途与生产工艺
CGP52411 (DAPH) 是一种高选择性，有效，口服活性和 ATP 竞争性的 EGFR 抑制剂，IC50 为 0.3 μM。CGP52411 阻止有毒的 Ca2+ 离子流入神经元细胞，并显着抑制和逆转与阿尔茨海默症相关的 β-amyloid (Aβ42) 原纤维聚集物的形成。
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EGFR
0.3 μM (IC
50
)
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Amyloid-β
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CGP52411 (DAPH; 0-100 μM; 90 minutes; A431 cells) treatment inhibits autophosphorylation and c-src autophosphorylation in vitro in a dose-dependent manner with
IC
50
s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an
IC
50
value of 10 μM.
CGP52411 (DAPH) inhibits c-src kinase with an
IC
50
value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an
IC
50
of 80 μM. CGP52411 inhibits conventional PKC isozymes (cPKCs α, β-1, β-2, and γ) but not nonconventional PKC isozymes (nPKCs δ, ε, and ζ) or atypical PKC isozymes (aPKC η).
Western Blot Analysis
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Cell Line:
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A431 cells
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Concentration:
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0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
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Incubation Time:
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90 minutes
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Result:
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Inhibited autophosphorylation in vitro in a dose-dependent manner with an
IC
50
of 1 μM. c-src autophosphorylation was inhibited with an
IC
50
of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p
185c-erbB2
, with an estimated
IC
50
value of 10 μM.
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CGP52411 (3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg; oral administration; daily; for 15 days; female BALB/c nude mice) treatment in vivo against xenografts of the A431 and SK-OV-3 tumors, and has antitumor activity.
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Animal Model:
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Female BALB/c nude mice injected with A431cells
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Dosage:
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3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
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Administration:
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Oral administration; daily; for 15 days
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Result:
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Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg.
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CGP 52411
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2021/03/30 | S0745 | CGP 52411
CGP52411 | 145915-58-8 | 2mg | 3906.63元 |
145915-58-8, CGP 52411 相关搜索:
- C275419] CGP 52411,EGFR的抑制剂
- 化合物CGP52411
- 化合物 T10782
- 5,6-双(苯基氨基)-1H-异吲哚-1,3(2H)-二酮
- 145915-58-8
- DAPH >=98% (HPLC), solid
- 1H-Isoindole-1,3(2H)-dione, 5,6-bis(phenylamino)-
- DAPH-1
(DAPH
- 4,5-Dianilinophthalimide, 5,6-Bis(phenylamino)-1H-isoindole-1,3(2H)-dione, CGP 52411
- DAPH/CGP 52411