BRACO 19
| 中文名称 | BRACO 19 |
|---|---|
| 中文同义词 | 化合物 T26892;BRACO 19 盐酸盐;CHEMBL336434 |
| 英文名称 | BRACO 19 |
| 英文同义词 | BRACO 19;BRACO 19 1-Pyrrolidinepropaneamide;1-Pyrrolidinepropanamide, N,N'-[9-[[4-(dimethylamino)phenyl]amino]-3,6-acridinediyl]bis- |
| CAS号 | 351351-75-2 |
| 分子式 | C35H43N7O2 |
| 分子量 | 593.76 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 351351-75-2.mol |
| 结构式 |  |
BRACO 19 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 | 固体 |
| 颜色 | 棕至橙色 |
IC50: telomerase/telomere
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. |
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. |