化合物 T23819

生物活性靶点体外研究体内研究化合物 T23819 试剂级价格

化合物 T23819

CAS号:1177798-88-7
英文名:N,N′-(9-(4-(Dimethylamino)phenylamino)acridine-3,6-diyl)bis(3-(pyrrolidin-1-yl)propanamide) trihydrochloride
中文名:化合物 T23819
CBNumber:CB02751065
分子式:C35H44ClN7O2
分子量:630.23
MOL File:1177798-88-7.mol

化合物 T23819化学性质

储存条件 :2-8°C
溶解度 :H2O: soluble5mg/mL, clear
形态 :powder
颜色 :yellow to brown
水溶解性 :H2O: 5mg/mL, clear

安全信息

危险品标志 :T
危险类别码 :25
安全说明 :45
危险品运输编号 :UN 2811 6.1 / PGIII
WGK Germany :3

化合物 T23819性质、用途与生产工艺

生物活性 Braco-19 trihydrochloride 是一种有效的端粒酶/端粒 (telomerase/telomere) 抑制剂，可防止端粒酶的催化作用。Braco-19 trihydrochloride 作为四联体 (GQ) 结合配体，稳定 GQ 四联体在 3V 端粒 DNA 处的形成，并可以导致快速衰老或选择性细胞死亡。Braco-19 trihydrochloride 也是一种HAdV病毒复制抑制剂。
靶点

IC50: telomerase

体外研究

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.

体内研究

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.