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145915-58-8

中文名稱 CGP 52411
英文名稱 DAPH
CAS 145915-58-8
分子式 C20H15N3O2
分子量 329.35
MOL 文件 145915-58-8.mol
更新日期 2023/03/17 20:03:06
145915-58-8 結(jié)構(gòu)式 145915-58-8 結(jié)構(gòu)式

基本信息

中文別名
5,6-雙(苯基氨基)-1H-異吲哚-1,3(2H)-二酮
英文別名
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

物理化學(xué)性質(zhì)

熔點(diǎn)199-202℃
密度1.374
儲(chǔ)存條件2-8°C
溶解度DMSO: ~30 mg/mL
酸度系數(shù)(pKa)9.06±0.20(Predicted)
形態(tài)solid
顏色orange

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H303
防范說明P312
安全說明36/37
WGK Germany3
CGP 52411價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2021/03/30S0745CGP 52411
CGP52411
145915-58-82mg3906.63元

常見問題列表

生物活性
CGP52411 (DAPH) 是一種高選擇性,有效,口服活性和 ATP 競爭性的 EGFR 抑制劑,IC50 為 0.3 μM。CGP52411 阻止有毒的 Ca2+ 離子流入神經(jīng)元細(xì)胞,并顯著抑制和逆轉(zhuǎn)與阿爾茨海默癥相關(guān)的 β-amyloid (Aβ42) 原纖維聚集物的形成。
靶點(diǎn)

EGFR

0.3 μM (IC 50 )

Amyloid-β

體外研究

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

Cell Line: A431 cells
Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 90 minutes
Result: 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.
體內(nèi)研究

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.

Animal Model: Female BALB/c nude mice injected with A431cells
Dosage: 3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
Administration: Oral administration; daily; for 15 days
Result: Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg.
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