Braco-19 trihydrochloride

CAS: 1177798-88-7 F: C35H46Cl3N7O2 W: 703.14

Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of te

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Bioactivity	Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-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 a HAdV virus replication inhibitor[1][2].
Target	IC50: telomerase
Invitro	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 IC50 for BRACO-19 in UXF1138L cells is 2.5 μM, the IC100 is 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:
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:
Name	Braco-19 trihydrochloride
CAS	1177798-88-7
Formula	C35H46Cl3N7O2
Molar Mass	703.14
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Angelika M Burger, et al. The G-quadruplex-interactive Molecule BRACO-19 Inhibits Tumor Growth, Consistent With Telomere Targeting and Interference With Telomerase Function. Cancer Res. 2005 Feb 15;65(4):1489-96. [2]. Prativa Majee, et al. Genome-wide Analysis Reveals a Regulatory Role for G-quadruplexes During Adenovirus Multiplication. Virus Res. . 2020 Jul 2;283:197960.