[CAS NO. 328543-09-5] AG14361
PRODUCTS SPECIFICATIONS [328543-09-5]
DESCRIPTION [328543-09-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 320.39 |
| Molecular Formula | C19H20N4O |
| SMILES | O=C1NCCN2C3=C1C=CC=C3N=C2C4=CC=C(C=C4)CN(C)C |
2 Publications Citing Use of MCE
Summary
AG14361 is a potent PARP-1 inhibitor, with a K i of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC 50 s are 29 nM and 14 nM, respectively.
IC50 & Target
|
PARP-1 0.5 nM (Ki) |
In Vitro
AG14361 is a potent PARP-1 inhibitor, with a K i of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC 50 s are 29 nM and 14 nM, respectively. AG14361 inhibits the proliferation of human cancer cells, such as A549, LoVo, and SW620 cells, with GI 50 s of 14 μM, 11.2 μM and 20 μM, respectively. Furthermore, AG14361 in combination with NSC 362856 markedly reduces the GI 50 value of NSC 362856 in LoVo and A549 cells, but does not exert such an effect in SW620 cells [1] . AG14361 suppresses breast cancer cells with IC 50 s of 17 μM and 25 μM for 92 J-wt-BRCA1 and 92 J-sh-BRCA1 cells, respectively. AG14361 induces caspase 3/7 activation and cell cycle abnormalities, and also inhibits NF-κB signaling [2] . AG14361 (0.4 μM) enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons, with no obvious effect on the formation and reversal of cleavable complexes, and increases the persistence of camptothecin-induced DNA single-strand breaks [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AG14361 (5 and 15 mg/kg, i.p.) has no toxicity and does not inhibit the growth of tumor. However, AG14361 markedly enhances NSC 362856 activity against LoVo xenografts and delays tumor growth when combined with NSC 362856. AG14361 (15 mg/kg, i.p.) treatment before irradiation dramaticly increases the sensitivity to radiation therapy of mice bearing LoVo xenografts [1] . AG14361 (30 mg/kg) synergizes lestaurtinib activity on inhibiting breast cancer tumors in allografts [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 156.06 mM ; ultrasonic and warming and heat to 80°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1212 mL | 15.6060 mL | 31.2120 mL |
| 5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL |
References
- [1] Calabrese CR, et al. Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361. J Natl Cancer Inst. 2004 Jan 7;96(1):56-67.
- [2] Vazquez-Ortiz G, et al. Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells. Breast Cancer Res. 2014
- [3] Smith LM, et al. The novel poly(ADP-Ribose) polymerase inhibitor, AG14361, sensitizes cells to topoisomerase I poisons by increasing the persistence of DNA strand breaks. Clin Cancer Res. 2005 Dec 1;11(23):8449-57.