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Chemical Compound Review

AN-204     (7S,9R)-7-[(2S,4S,5S,6S)-4- (2,3...

Synonyms: LS-94618, AN 201, AN 204, AC1L3OD8, C31H33NO11, ...
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Disease relevance of AN-204

  • Preliminary studies in animal models of breast and prostate cancers showed that AN-238 is less toxic than AN-201 and more potent in inhibiting tumor growth [1].
  • Lung metastases were found in 83% of controls and 50% of AN-201 treated animals, but none occurred in mice treated with AN-238 [2].
  • The effects of repeated administration of AN-238 and AN-201 were also evaluated on xenografted Panc-1, MiaPaCa-2, CFPAC-1, Capan-1, and Capan-2 pancreatic cancers [3].
  • The mortality due to toxicity was 25% in the group receiving AN-201 and 12.5% in the AN-207-treated group [4].
  • Cytotoxic analogs of LH-RH, AN-152 and AN-207, containing doxorubicin (DOX) or 2-pyrrolino-DOX (AN-201), respectively, target LH-RH receptors and can be used for the treatment of prostatic, breast, ovarian and endometrial cancers and melanomas [5].

High impact information on AN-204


Chemical compound and disease context of AN-204


Biological context of AN-204


Anatomical context of AN-204


Associations of AN-204 with other chemical compounds

  • Nude mice bearing xenografts of these cancers were injected i.v. with 250 nmol/kg doses of cytotoxic radical AN-201, cytotoxic analog AN-238 or the unconjugated mixture of AN-201 and sst analog RC-121 [15].
  • As in the case of DOX, AN-201 was coupled to carrier peptide [D-Lys6]LHRH to form a superactive targeted cytotoxic LHRH analog, AN-207 [16].

Gene context of AN-204

  • We also studied the effects of AN-238 and AN-201 on the expression of MDR-1, MRP-1 and LRP by real-time PCR [17].
  • In all 3 endometrial carcinoma lines, AN-238 caused a weaker induction of MDR-1 than AN-201 [18].
  • In vivo studies in nude mice demonstrated that AN-238, AN-201, and DOX were equally effective on HCT-116 tumors that express wild-type p53 [19].
  • MRP-1 and BCRP were not induced by AN-215 or AN-201 [20].
  • To investigate the efficacy of SST receptor-targeted chemotherapy in metastatic RCC, three i.v. injections of AN-238 or AN-201 at 150 nmol/kg were given at biweekly intervals to nude mice implanted with 786-0 tumors under the renal capsule [2].

Analytical, diagnostic and therapeutic context of AN-204

  • In this study, we investigated the effects of cytotoxic analog AN-207, designed for targeted chemotherapy and radical AN-201 on pituitary function in rats [21].
  • The effects of three i.v. injections of 150 nmol/kg of AN-238 or AN-201, given on days 1, 8, and 21, were evaluated in groups of nude mice bearing s.c. xenografts of SW-839 and 786-0 RCC [2].
  • Four weeks after the injection of 110 nmol/kg AN-201, mean tumor volume was reduced by 35.1 % (P < 0.05), as compared with controls [22].
  • After 6 weeks, the weight of orthotopic tumors treated with AN-238 (55.3 +/- 44.3 mg) was significantly lower (87% reduction; P < 0.001) than that in the control group (414.2 +/- 41.0 mg) or in animals given AN-201 (270.2 +/- 603 mg; P < 0.05) [2].
  • In contrast, after treatment with cytotoxic radical AN-201, MDA-MB-231 and MCF-7-MIII tumors grew steadily and the regression of MX-1 tumors was only transitory in most animals [15].


  1. Synthesis and biological evaluation of cytotoxic analogs of somatostatin containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin. Nagy, A., Schally, A.V., Halmos, G., Armatis, P., Cai, R.Z., Csernus, V., Kovács, M., Koppán, M., Szepesházi, K., Kahán, Z. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  2. Inhibition of metastatic renal cell carcinomas expressing somatostatin receptors by a targeted cytotoxic analogue of somatostatin AN-238. Plonowski, A., Schally, A.V., Nagy, A., Kiaris, H., Hebert, F., Halmos, G. Cancer Res. (2000) [Pubmed]
  3. Targeting of cytotoxic somatostatin analog AN-238 to somatostatin receptor subtypes 5 and/or 3 in experimental pancreatic cancers. Szepeshazi, K., Schally, A.V., Halmos, G., Sun, B., Hebert, F., Csernus, B., Nagy, A. Clin. Cancer Res. (2001) [Pubmed]
  4. Effective treatment of metastatic MDA-MB-435 human estrogen-independent breast carcinomas with a targeted cytotoxic analogue of luteinizing hormone-releasing hormone AN-207. Chatzistamou, L., Schally, A.V., Nagy, A., Armatis, P., Szepeshazi, K., Halmos, G. Clin. Cancer Res. (2000) [Pubmed]
  5. Chemotherapy targeted to cancers through tumoral hormone receptors. Schally, A.V., Nagy, A. Trends Endocrinol. Metab. (2004) [Pubmed]
  6. Selective induction of apoptosis by the cytotoxic analog AN-207 in cells expressing recombinant receptor for luteinizing hormone-releasing hormone. Danila, D.C., Schally, A.V., Nagy, A., Alexander, J.M. Proc. Natl. Acad. Sci. U.S.A. (1999) [Pubmed]
  7. Design, synthesis, and in vitro evaluation of cytotoxic analogs of bombesin-like peptides containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin. Nagy, A., Armatis, P., Cai, R.Z., Szepeshazi, K., Halmos, G., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  8. Targeted cytotoxic analog of luteinizing hormone-releasing hormone AN-207 inhibits growth of OV-1063 human epithelial ovarian cancers in nude mice. Miyazaki, M., Schally, A.V., Nagy, A., Lamharzi, N., Halmos, G., Szepeshazi, K., Armatis, P. Am. J. Obstet. Gynecol. (1999) [Pubmed]
  9. Effective treatment of experimental DU-145 prostate cancers with targeted cytotoxic somatostatin analog AN-238. Plonowski, A., Schally, A.V., Nagy, A., Sun, B., Halmos, G. Int. J. Oncol. (2002) [Pubmed]
  10. Inhibition of growth of experimental human and hamster pancreatic cancers in vivo by a targeted cytotoxic bombesin analog. Szepeshazi, K., Schally, A.V., Nagy, A., Halmos, G. Pancreas (2005) [Pubmed]
  11. Administration of a targeted cytotoxic analog of luteinizing hormone-releasing hormone inhibits growth of estrogen-independent MDA-MB-231 human breast cancers in nude mice. Kahán, Z., Nagy, A., Schally, A.V., Halmos, G., Arencibia, J.M., Groot, K. Breast Cancer Res. Treat. (2000) [Pubmed]
  12. In vitro targeting of a cytotoxic analog of luteinizing hormone-releasing hormone AN-207 to ES-2 human ovarian cancer cells as demonstrated by microsatellite analyses. Arencibia, J.M., Schally, A.V., Halmos, G., Nagy, A., Kiaris, H. Anticancer Drugs (2001) [Pubmed]
  13. Dipeptide-based highly potent doxorubicin antibody conjugates. Jeffrey, S.C., Nguyen, M.T., Andreyka, J.B., Meyer, D.L., Doronina, S.O., Senter, P.D. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
  14. Potent induction of apoptosis in human hepatoma cell lines by targeted cytotoxic somatostatin analogue AN-238. Lasfer, M., Vadrot, N., Schally, A.V., Nagy, A., Halmos, G., Pessayre, D., Feldmann, G., Reyl-Desmars, F.J. J. Hepatol. (2005) [Pubmed]
  15. Inhibition of growth of MX-1, MCF-7-MIII and MDA-MB-231 human breast cancer xenografts after administration of a targeted cytotoxic analog of somatostatin, AN-238. Kahán, Z., Nagy, A., Schally, A.V., Hebert, F., Sun, B., Groot, K., Halmos, G. Int. J. Cancer (1999) [Pubmed]
  16. Targeting of cytotoxic luteinizing hormone-releasing hormone analogs to breast, ovarian, endometrial, and prostate cancers. Nagy, A., Schally, A.V. Biol. Reprod. (2005) [Pubmed]
  17. Effective therapy of experimental human malignant melanomas with a targeted cytotoxic somatostatin analogue without induction of multi-drug resistance proteins. Keller, G., Schally, A.V., Nagy, A., Baker, B., Halmos, G., Engel, J.B. Int. J. Oncol. (2006) [Pubmed]
  18. Targeted therapy with a cytotoxic somatostatin analog, AN-238, inhibits growth of human experimental endometrial carcinomas expressing multidrug resistance protein MDR-1. Engel, J.B., Schally, A.V., Halmos, G., Baker, B., Nagy, A., Keller, G. Cancer (2005) [Pubmed]
  19. Targeted cytotoxic somatostatin analogue AN-238 inhibits somatostatin receptor-positive experimental colon cancers independently of their p53 status. Szepeshazi, K., Schally, A.V., Halmos, G., Armatis, P., Hebert, F., Sun, B., Feil, A., Kiaris, H., Nagy, A. Cancer Res. (2002) [Pubmed]
  20. Experimental therapy of human endometrial cancers with a targeted cytotoxic bombesin analog AN-215: low induction of multidrug resistance proteins. Engel, J.B., Schally, A.V., Halmos, G., Baker, B., Nagy, A., Keller, G. Eur. J. Cancer (2005) [Pubmed]
  21. Recovery of pituitary function after treatment with a targeted cytotoxic analog of luteinizing hormone-releasing hormone. Kovacs, M., Schally, A.V., Nagy, A., Koppan, M., Groot, K. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  22. Targeted cytotoxic analogue of somatostatin AN-238 inhibits growth of androgen-independent Dunning R-3327-AT-1 prostate cancer in rats at nontoxic doses. Koppan, M., Nagy, A., Schally, A.V., Arencibia, J.M., Plonowski, A., Halmos, G. Cancer Res. (1998) [Pubmed]
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