Braco-19 trihydrochloride

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CAS NO:

1177798-88-7

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 mg

5 mg

10 mg

1 mM	1.4222 mL	7.1110 mL	14.2219 mL
5 mM	0.2844 mL	1.4222 mL	2.8444 mL
10 mM	0.1422 mL	0.7111 mL	1.4222 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。