TAS 103
TAS 103 Basic information
- Product Name:
- TAS 103
- Synonyms:
-
- TAS 103
- 6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one
- TAS-103 HC1
- TA103(bms-247615)
- TAS-103 base
- BMS-247615
- TAS-103(salt)
- CS-1287
- CAS:
- 174634-08-3
- MF:
- C20H19N3O2
- MW:
- 333.38
- Mol File:
- 174634-08-3.mol
TAS 103 Chemical Properties
- Melting point:
- 216-217 °C(Solv: ethanol (64-17-5))
- Boiling point:
- 589.5±50.0 °C(Predicted)
- Density
- 1.350±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 7.88±0.20(Predicted)
TAS 103 Usage And Synthesis
Uses
TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
Biological Activity
TAS-103 is a dual DNA topoisomerase I/II (topoisomerase I/II) inhibitor for cancer research.
in vivo
TAS-103 (30 mg/kg, iv) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103.
target
| Topoisomerase I
| Topoisomerase II
|
IC 50
Topoisomerase I; Topoisomerase II
References
[1] Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II DOI:10.1016/s0006-2952(00)00402-0
[2] Shimizu K, et al. Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent. Biol Pharm Bull. 2002 Oct;25(10):1385-7. DOI:10.1248/bpb.25.1385
[3] Yoshida M, et al. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 2008 Mar;73(3):987-94. Epu DOI:10.1124/mol.107.043307
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