Braco-19

Braco-19 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK 293 cells Concentration: 20 μM; 40 μM Incubation Time: 24 hours Result: Displayed low cytotoxicity and decreased the eGFP fluorescence. In Vivo 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: telomerase/telomere

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