TAS-103 - CAS 174634-09-4
Catalog number: 174634-09-4
Category: Inhibitor
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TAS-103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models. TAS-103 has been reported to be a potent topoisomerase II poison. TAS-103 showed the strongest antitumor activity among the conventional anticancer agents for colorectal cancer (p<0.05). The combination with CDDP augmented the antitumor activity of TAS-103 (p<0.05), indicating that CDDP is one of the most potent candidates to be used in combination with TAS-103
Related CAS:
174634-08-3 (Free base)
Red solid powder
6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride; TAS103; TAS-103; TAS 103; BMS247615; BMS 247615; BMS-247615
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Current Developer:
Taiho (Originator), Bristol-Myers Squibb (Licensee)
1.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.
Shimizu K1, Takada M, Asai T, Kuromi K, Baba K, Oku N. Biol Pharm Bull. 2002 Oct;25(10):1385-7.
A novel anti-tumor agent, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride (TAS-103), effectively inhibits both topoisomerase I and II activities. To enhance anti-tumor efficacy and to reduce the side effects of the agent, liposomalization of TAS-103 was performed. TAS-103 was effectively entrapped in liposomes by a remote-loading method, and was stable at 4 degrees C and in the presence of 50% serum. To evaluate the anti-tumor efficacy of liposomal TAS-103, the growth inhibition against Lewis lung carcinoma cells in vitro and the therapeutic efficacy against solid tumor-bearing mice in vivo were examined. Liposomal TAS-103 showed strong cytotoxic effect against Lewis lung carcinoma cells in a dose dependent manner and effectively suppressed solid tumor growth accompanying longer survival time of tumor-bearing mice in comparison with the mice treated with free TAS-103. These results suggest that liposomal TAS-103 is useful for cancer therapy.
2.Self-association and unique DNA binding properties of the anti-cancer agent TAS-103, a dual inhibitor of topoisomerases I and II.
Ishida K1, Asao T. Biochim Biophys Acta. 2002 Jul 18;1587(2-3):155-63.
The objective of our study was to investigate the self-association and DNA-binding properties of the DNA topoisomerases I (Topo I) and II (Topo II) dual inhibitor: 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinoline-7-one dihydrochloride (TAS-103), by means of 1H-NMR and 31P-NMR spectroscopy, structure computation techniques, thermal melting study, and UV-Visible spectroscopy. In aqueous solution, all chemical shifts of TAS-103 underwent upfield shifts depending with an increase in concentration. The two-dimensional (2D)-NMR spectra and structure computations indicated that TAS-103 self-associated through pi-pi stacking and hydrophobic interactions of the aromatic chromophores. Thermal melting indicated that the binding of TAS-103 to DNA with a potency equal to that of ethidium bromide (EtBr). The UV-Visible spectra of TAS-103 titrated by several DNA exhibited hypochromic and hypsochromic effects. The 31P-NMR spectrum of the 6:1 TAS-103/d(CGCGAATTCGCG)(2) complex showed two broadening signals.
3.Promising antitumor activity of a novel quinoline derivative, TAS-103, against fresh clinical specimens of eight types of tumors measured by flow cytometric DNA analysis.
Fujimoto S1. Biol Pharm Bull. 2007 Oct;30(10):1923-9.
TAS-103, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno-[2,1-c]quinolin-7-one dihydrochloride, is a dual topoisomerases I and II inhibitor. Antitumor activities of TAS-103 against fresh surgical specimens resected from 525 patients (32 types of tumors) were examined by flow cytometric (FCM) analysis of DNA integrity of tumor cells, and compared with those of five other investigational new drugs and 31 clinically available anticancer agents. Concentrations of clinically available anticancer agents were set at one-tenth of the peak plasma concentration (PPC) of the clinically recommended doses. On the other hand, since PPCs of investigational new drugs in humans were frequently unknown, these were estimated by a method that determines the theoretically achievable concentration in body fluid (TAC method). Correlations between TAC and PPC were examined for 16 clinically available anticancer agents, and it was found that TAC at 7n (the modified Fibonacci's dose-escalation scheme) of 14 drugs corresponded well with each one-tenth of PPC.
4.DNA topoisomerase II poison TAS-103 transactivates GC-box-dependent transcription via acetylation of Sp1.
Torigoe T1, Izumi H, Wakasugi T, Niina I, Igarashi T, Yoshida T, Shibuya I, Chijiiwa K, Matsuo K, Itoh H, Kohno K. J Biol Chem. 2005 Jan 14;280(2):1179-85. Epub 2004 Nov 8.
Drug-induced modifications of transcription factors play important roles in both apoptosis and survival signaling. The data presented here show that the DNA topoisomerase II poison TAS-103 transactivated the SV40 promoter in a GC-box-dependent manner and induced Sp1 acetylation in cells expressing p300. This activity was not observed in cells lacking p300. TAS-103 treatment also enhanced the p300 content of the nucleus and the interaction of p300 with Sp1. Cellular susceptibility to TAS-103 was correlated with p300 expression but not with topoisomerase II expression. Furthermore, the presence of p300 significantly sensitized cancer cells to TAS-103 but not to cisplatin. Taken together, these findings demonstrate novel genomic responses to anticancer agents that modulate Sp1 acetylation and Sp1-dependent transcription in an apoptotic pathway.
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CAS 174634-09-4 TAS-103

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