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

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 圖譜信息 CGP 52411價(jià)格(試劑級(jí)) 常見問題列表

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

InChI1S/C20H15N3O2/c24-19-15-11-17(21-13-7-3-1-4-8-13)18(12-16(15)20(25)23-19)22-14-9-5-2-6-10-14/h1-12,21-22H,(H,23,24,25)

InChIKeyAAALVYBICLMAMA-UHFFFAOYSA-N

SMILESO=C1NC(=O)c2cc(Nc3ccccc3)c(Nc4ccccc4)cc12

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS) 有害 (GHS07)

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

存儲(chǔ)類別11 - Combustible Solids

圖譜信息

CGP 52411(145915-58-8)核磁圖(¹HNMR)

CGP 52411價(jià)格(試劑級(jí))

報(bào)價(jià)日期	產(chǎn)品編號(hào)	產(chǎn)品名稱	CAS號(hào)	包裝	價(jià)格
2021/03/30	S0745	CGP 52411 CGP52411	145915-58-8	2mg	3906.63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.