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Braco-19 trihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Braco-19 trihydrochloride图片
CAS NO:1177798-88-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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。
生物活性

Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action oftelomerase. Braco-19 acts asG-quadruplex(GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also aHAdV virus replication inhibitor[1][2].

IC50& Target

IC50: telomerase[1]

体外研究
(In Vitro)

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[2].
BRACO-19 trihydrochloride (1.0-10 μM; 5 day) cause zero growth inhibition is found 1 μM, the IC50for BRACO-19 in UXF1138L cells is 2.5 μM, the IC100is 5 μM[1].
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[1].
BRACO-19 trihydrochloride (0-40 μM; 24 hours) decreases the AdV virus growth in a dose-dependent manner in eGFP-transinfected HEK 293 cells[2].
BRACO-19 trihydrochloride (0-150 μM; 24 hours) shows a decrease in band intensity in an increasing concentration-dependent manner[2].

Cell Viability Assay[1]

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
(In Vivo)

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[1].
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)[1].

Animal Model:Established UXF1138LX Xenografts in nude mice[1]
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.
分子量

703.14

性状

Solid

Formula

C35H46Cl3N7O2

CAS 号

1177798-88-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 22 mg/mL(31.29 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.4222 mL7.1110 mL14.2219 mL
5 mM0.2844 mL1.4222 mL2.8444 mL
10 mM0.1422 mL0.7111 mL1.4222 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。