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351351-75-2

中文名称 BRACO 19
英文名称 BRACO 19
CAS 351351-75-2
分子式 C35H43N7O2
分子量 593.76
MOL 文件 351351-75-2.mol
更新日期 2024/08/11 22:53:06
351351-75-2 结构式 351351-75-2 结构式

基本信息

中文别名
化合物 T26892
BRACO 19 盐酸盐
英文别名
BRACO 19
BRACO 19 1-Pyrrolidinepropaneamide
1-Pyrrolidinepropanamide, N,N'-[9-[[4-(dimethylamino)phenyl]amino]-3,6-acridinediyl]bis-

物理化学性质

熔点>320 °C
沸点854.9±65.0 °C(Predicted)
密度1.274±0.06 g/cm3(Predicted)
酸度系数(pKa)12.93±0.43(Predicted)
形态Solid
颜色Brown to orange

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H301

常见问题列表

生物活性
Braco-19 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 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 也是一种 HAdV 病毒复制抑制剂。
靶点

IC50: telomerase/telomere

体外研究

Braco-19, as a well-known GQ binding ligand, interacts specifically with the HAdV GQs and increases their stability, and blocks the HAdV multiplication.BRACO-19 (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 (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 (0-40 μM; 24 hours) decreases the AdV virus growth in a dose-dependent manner in eGFP-transinfected HEK 293 cells.BRACO-19 (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 (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 (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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