BRACO 19
BRACO 19 Basic information
- Product Name:
- BRACO 19
- Synonyms:
-
- BRACO 19
- BRACO 19 1-Pyrrolidinepropaneamide
- 1-Pyrrolidinepropanamide, N,N'-[9-[[4-(dimethylamino)phenyl]amino]-3,6-acridinediyl]bis-
- N,N'-(9-((4-(Dimethylamino)phenyl)amino)acridine-3,6-diyl)bis(3-(pyrrolidin-1-yl)propanamide)
- N,N'-(9-((4-(Dimethylamino)phenyl)amino)acridine-3,6-diyl)bis(3-(pyrrolidin-1-yl)propanamide)
- CAS:
- 351351-75-2
- MF:
- C35H43N7O2
- MW:
- 593.76
- Mol File:
- 351351-75-2.mol
BRACO 19 Chemical Properties
- Melting point:
- >320 °C
- Boiling point:
- 854.9±65.0 °C(Predicted)
- Density
- 1.274±0.06 g/cm3(Predicted)
- pka
- 12.93±0.43(Predicted)
- form
- Solid
- color
- Brown to orange
BRACO 19 Usage And Synthesis
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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