Anaxirone - CAS 77658-97-0
Catalog number: 77658-97-0
Category: Inhibitor
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Anaxirone is a synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis.
triglycidylurazol; Abbreviation: TGU; 1,2,4-triglycidylurazol.
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1.Colony assay with human tumor xenografts, murine tumors and human bone marrow. Potential for anticancer drug development.
Fiebig HH1, Schmid JR, Bieser W, Henss H, Lohr GW. Eur J Cancer Clin Oncol. 1987 Jul;23(7):937-48.
The colony formation of human tumor xenografts from nude mice, of murine tumors, and of human bone marrow (CFU-C) has been investigated in vitro using a modification of the double-layer agar assay described by Hamburger and Salmon. Systematic modification of growth conditions and careful selection of viable tumor tissue enhanced the growth rate (at least 30 colonies per dish) of human tumor xenografts to 86% (98/114). The median plating efficiency was 0.07% which is comparable to the results observed by others using fresh human tumors. The growth of human bone marrow was stimulated with a placenta-conditioned medium, which allowed growth of granulocytic stem cell colonies (CFU-C). The median plating efficiency of the bone marrow was 0.08%. The murine tumors P388, L1210, B16 melanoma, Lewis lung carcinoma and colon carcinoma 38 grew very well in vitro. Excluding the Lewis lung carcinoma, the plating efficiency of these tumors was markedly higher than that of the human tumor xenografts and human bone marrow.
2.Phase II trial of anaxirone (1,2,4-triglycidylurazol, TGU) in patients with advanced ovarian carcinoma: an EORTC Gynecological Cancer Cooperative Group Study.
George M1, Scotto V, Carnino F, Dodion P, ten Bokkel Huinink WW, Rotmensz N, Vermorken JB. Eur J Cancer Clin Oncol. 1987 Jun;23(6):867-9.
Sixteen patients with advanced ovarian carcinoma were treated with anaxirone (1,2,4-triglycidylurazol, TGU), 600 mg/m2 every 4 weeks. Anaxirone was the second or later line of therapy. All patients had evaluable tumors and evidence of failure of prior therapy. None of the patients responded. Two had stabilization of the disease for 4 months. In one patient WHO grade 4 leukopenia and grade 4 thrombocytopenia were observed after the second TGU cycle starting on day 41 and persisted until the patient died due to tumor progression (day 50). No patient experienced thrombophlebitis.
3.Phase II trial of anaxirone (TGU) in advanced colorectal cancer: an EORTC Early Clinical Trials Group (ECTG) study.
Holdener EE1, Clavel M, Sessa C, ten Bokkel Huinink W, Siegenthaler P, Ludwig C, Klepp O, Renard G, Decoster G, Pinedo HM. Eur J Cancer. 1994;30A(3):394-5.
Anaxirone, a rationally synthesised triepoxide derivative, was given to 46 patients with metastatic colorectal cancer. Good risk patients received 800 mg/m2 as a rapid intravenous injection every 4 weeks, whereas poor risk patients received 650 mg/m2. Of 46 patients, 45 were evaluable for toxicity and 42 for efficacy analysis. There were 37/45 patients with poor risk, showing no difference in toxicity as compared to good risk patients. The major toxic effect was myelosuppression with 34% of all patients experiencing grade 3 or 4 leucopenia; thrombocytopenia was less frequent. Locoregional phlebitis occurred in 66% of the patients. There was no objective tumour response to anaxirone in 42 evaluable patients. Only 4 patients achieved stabilisation of the disease lasting maximally up to 248 days. Anaxirone is inactive in metastatic colorectal cancer.
4.Phase II study of 1,2,4-triglycidylurazol (TGU) in previously untreated and treated patients with small cell lung cancer.
Lund B1, Hansen F, Hansen M, Hansen HH. Eur J Cancer Clin Oncol. 1987 Jul;23(7):1031-3.
Six previously untreated poor prognosis patients and eight previously treated patients with small cell lung cancer (SCC) were treated with 1,2,4-triglycidylurazol (TGU, NSC-332488) 800 and 650 mg/m2 every 4 weeks, respectively. No responses were observed. The survival time of the previously untreated patients was short, a median of 7 weeks (range 5-10 weeks). Myelosuppression was severe and prolonged with white blood count, WHO grade 3-4, in four previously untreated patients and in two previously patients, and with platelets, WHO grade 3-4, in both four previously untreated and in four previously treated patients. Gastrointestinal toxicity was mild to moderate. It is concluded that TGU is inactive in SCC.
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CAS 77658-97-0 Anaxirone

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