Braco-19

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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 IC50 for BRACO-19 in UXF1138L cells is 2.5 μM, the IC100 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.

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 miceDosage: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.

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Cell Cycle/DNA Damage

Telomerase

Telomerase | Antiviral

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351351-75-2

593.76

C35H43N7O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 33.33 mg/mL (56.13 mM; 超声助溶 )

O=C(NC=1C=CC2=C(N=C3C=C(C=CC3=C2NC4=CC=C(C=C4)N(C)C)NC(=O)CCN5CCCC5)C1)CCN6CCCC6

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(-20℃)

With Ice Pack

≥ 2 years