S83947 |
TAS-103 (dihydrochloride) |
源葉(MedMol) | 98% |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.461 ml | 12.306 ml | 24.612 ml |
5 mM | 0.492 ml | 2.461 ml | 4.922 ml |
10 mM | 0.246 ml | 1.231 ml | 2.461 ml |
50 mM | 0.049 ml | 0.246 ml | 0.492 ml |
- 提示:詳情請(qǐng)下載說(shuō)明書(shū)。
- 產(chǎn)品描述: TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
- 靶點(diǎn): Topoisomerase I;Topoisomerase II;Topoisomerase
- 體外研究:
TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103. TAS-103 inhibits the viability of HeLa cells, with an IC50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation
- 體內(nèi)研究:
TAS-103 (30 mg/kg, i.v.) 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
- 參考文獻(xiàn):
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 cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000 Sep 15;60(6):817-21. 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. 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.
- 溶解性: Soluble in H2O
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.461 ml 12.306 ml 24.612 ml 5 mM 0.492 ml 2.461 ml 4.922 ml 10 mM 0.246 ml 1.231 ml 2.461 ml 50 mM 0.049 ml 0.246 ml 0.492 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)