| Identification | Back Directory | [Name]
BRACO 19 | [CAS]
351351-75-2 | [Synonyms]
BRACO 19
BRACO 19 1-Pyrrolidinepropaneamide
1-Pyrrolidinepropanamide, N,N'-[9-[[4-(dimethylamino)phenyl]amino]-3,6-acridinediyl]bis- | [Molecular Formula]
C35H43N7O2 | [MDL Number]
MFCD10574844 | [MOL File]
351351-75-2.mol | [Molecular Weight]
593.76 |
| Chemical Properties | Back Directory | [Melting point ]
>320 °C | [Boiling point ]
854.9±65.0 °C(Predicted) | [density ]
1.274±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.93±0.43(Predicted) | [color ]
Brown to orange |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [Definition]
ChEBI: N,N'-(9-{[4-(dimethylamino)phenyl]amino}acridine-3,6-diyl)bis(3-pyrrolidin-1-ylpropanamide) is a member of acridines and a N-alkylpyrrolidine. | [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[1]. 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)[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. |
| [References]
[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. DOI:10.1158/0008-5472.CAN-04-2910
[2] Prativa Majee, et al. Genome-wide Analysis Reveals a Regulatory Role for G-quadruplexes During Adenovirus Multiplication. Virus Res. .?2020 Jul DOI:10.1016/j.virusres.2020.197960 |
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