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[CAS NO. 1177798-88-7] Braco-19trihydrochloride
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-15523A |
| Brand: | MCE |
| CAS: | 1177798-88-7 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 703.14 |
| Molecular Formula | C35H46Cl3N7O2 |
| SMILES | CN(C1=CC=C(NC2=C(C=CC(NC(CCN3CCCC3)=O)=C4)C4=NC5=CC(NC(CCN6CCCC6)=O)=CC=C52)C=C1)C.Cl.Cl.Cl |
2 Publications Citing Use of MCE
Summary
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] .
IC50 & Target
IC50: telomerase [1]
In Vitro
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 IC
50
for BRACO-19 in UXF1138L cells is 2.5 μM, the IC
100
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell 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 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
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)
Solvent & Solubility
H 2 O : 22 mg/mL ( 31.29 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4222 mL | 7.1110 mL | 14.2219 mL |
| 5 mM | 0.2844 mL | 1.4222 mL | 2.8444 mL |
| 10 mM | 0.1422 mL | 0.7111 mL | 1.4222 mL |
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.
- [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.
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