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1177798-88-7

中文名稱 化合物 T23819
英文名稱 N,N′-(9-(4-(Dimethylamino)phenylamino)acridine-3,6-diyl)bis(3-(pyrrolidin-1-yl)propanamide) trihydrochloride
CAS 1177798-88-7
分子式 C35H46Cl3N7O2
分子量 703.144
MOL 文件 1177798-88-7.mol
更新日期 2025/01/07 08:45:03
1177798-88-7 結(jié)構(gòu)式 1177798-88-7 結(jié)構(gòu)式

基本信息

中文別名
化合物 T23819
三鹽酸BRACO-19
N,N'-[9[[4-(二甲氨基)苯基]氨基]-3,6-吖啶二基]雙(1-吡咯烷丙酰胺)三鹽酸鹽
英文別名
BRACO19 hydrochloride
BRACO19 HCl
BRACO-19 (BRACO19)
BRACO19 trihydrochloride
N,N-[9[[4-(Dimethylamino)phenyl]amino]-3,6-acridinediyl]bis-1-pyrrolidinepropanamide Trihydrochlori
N,N'-[9[[4-(Dimethylamino)phenyl]amino]-3,6-acridinediyl]bis-1-pyrrolidinepropanamide trihydrochloride
N,N′-(9-(4-(Dimethylamino)phenylamino)acridine-3,6-diyl)bis(3-(pyrrolidin-1-yl)propanamide) trihydrochloride

物理化學性質(zhì)

儲存條件2-8°C
溶解度H2O:可溶5mg/mL,澄清
形態(tài)粉末
顏色黃色到棕色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
危險品標志T
危險類別碼25
安全說明45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3

常見問題列表

生物活性
Braco-19 trihydrochloride 是一種有效的端粒酶/端粒 (telomerase/telomere) 抑制劑,可防止端粒酶的催化作用。Braco-19 trihydrochloride 作為四聯(lián)體 (GQ) 結(jié)合配體,穩(wěn)定 GQ 四聯(lián)體在 3V 端粒 DNA 處的形成,并可以導致快速衰老或選擇性細胞死亡。Braco-19 trihydrochloride 也是一種HAdV病毒復制抑制劑。
靶點

IC50: telomerase

體外研究

Braco-19 trihydrochloride, as a well-known GQ binding ligand, interacts specifically with the HAdV GQs and increases their stability, and blocks the HAdV multiplication.BRACO-19 trihydrochloride (1.0-10 μM; 5 day) cause zero growth inhibition is found 1 μM, the IC 50 for BRACO-19 in UXF1138L cells is 2.5 μM, the IC 100 is 5 μM.BRACO-19 trihydrochloride (1 μM; 24 hours) shows dramatically reduced nuclear hTERT expression. However, residual cytoplasmic hTERT staining is observed accompanied by the occurrence of atypical mitoses.BRACO-19 trihydrochloride (0-40 μM; 24 hours) decreases the AdV virus growth in a dose-dependent manner in eGFP-transinfected HEK 293 cells.BRACO-19 trihydrochloride (0-150 μM; 24 hours) shows a decrease in band intensity in an increasing concentration-dependent manner.

Cell Viability Assay

Cell Line: HEK 293 cells
Concentration: 20 μM; 40 μM
Incubation Time: 24 hours
Result: Displayed low cytotoxicity and decreased the eGFP fluorescence.
體內(nèi)研究

BRACO-19 trihydrochloride (oral administration or intraperitoneal injection; 2 or 5 mg/kg; 3 weeks) oral dosing regimen are always inactive and the animals have to be sacrificed due to high tumor burden before overall termination of the study, Chronic, i.p. BRACO-19 administration, qdx5 is efficient in inhibiting tumor growth in earlystage xenografts but not advanced-stage xenografts. BRACO-19 trihydrochloride (intraperitoneal injection; 2 mg/kg; 3 weeks; starting 6 days after transplantation of UXF1138LX fragments) inhibits tumor growth significantly and under these conditions, marked single-agent antitumor activity is observed, with some animals in the group showing complete regressions (5 of 12 tumors).

Animal Model: Established UXF1138LX Xenografts in nude mice
Dosage: 2 mg/kg
Administration: Intraperitoneal injection; 3 weeks; starting 6 days after transplantation of UXF1138LX fragments
Result: Showed partial tumor regressions with an optimal T/C on day 28 of 4.1%, equal to 95.9% inhibition of tumor growth compared with control.
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