BRACO 19

生物活性靶点体外研究体内研究 BRACO 19 试剂级价格

BRACO 19

CAS号:351351-75-2
英文名:BRACO 19
中文名:BRACO 19
CBNumber:CB41855348
分子式:C35H43N7O2
分子量:593.76
MOL File:351351-75-2.mol

BRACO 19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

BRACO 19性质、用途与生产工艺

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.