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MedKoo product information:
Description of AN-207:
new targeted cytotoxic analog of LH-RH.
consists of the agonist [D-Lys(6)]LH-RH linked to
2-pyrrolino-doxorubicin, an intensely potent derivative of
doxorubicin. LHRH receptors expressed in a high percentage of human
NHL specimens can be used for effective targeted therapy with the
cytotoxic LHRH analogue
Targeted chemotherapy with
could be considered for treatment of advanced prostate cancer.
MedKoo Code#: 204371
Code name: AN-207.
MedKoo Code#: 204371
Chemical Formula: C95H121N19O26
Exact Mass: 1943.87302
Molecular Weight: 1945.09
Elemental Analysis: C, 58.66; H, 6.27; N, 13.68; O, 21.39
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Information about this agent
AN-207 is a potent derivative of
2-pyrrolinodoxorubicin conjugated to [D-Lys6] luteinizing
hormone-releasing hormone (LH-RH), which was demonstrated to be less
toxic than the nonconjugated chemotherapeutic radical and significantly
more active in slowing neoplastic cellular growth. In this study we
investigate the molecular mechanisms underlying the cytotoxic action of
stably transfected COS cells with a LH-RH receptor (LH-RH-Rc) mammalian
expression vector and examined the effect of
known markers of cellular apoptosis. Apoptotic induction by
measured by Bax and Bcl-2 protein levels, was increased in stable cells
that express LH-RH-Rc compared with parental cells. DNA fragmentation
also was increased by
AN-207 treatment when compared with AN-201. Clinically used LH-RH
antagonists partially inhibited apoptotic Bax expression and DNA
fragmentation induced by
induced down-regulation of Bcl-2 steady-state protein levels. In cell
proliferation studies, after 72 h
exhibited greater cytotoxicity than AN-201 at equivalent concentrations,
in COS cells expressing LH-RH-Rc but not in parental COS cells. In
addition, survival of LH-RH-Rc positive cells treated with
partially restored by LH-RH antagonist. This study demonstrates the
receptor-specific cytotoxic effect of 2-pyrrolinodoxorubicin conjugated
to [D-Lys6] LH-RH, exerted through induction of apoptosis and modulation
of Bax, Bcl-2, and DNA fragmentation (source: Proc Natl Acad Sci U S
A. 1999 Jan 19;96(2):669-73.).
1: Keller G, Schally AV, Gaiser T, Nagy A,
Baker B, Halmos G, Engel JB. Receptors for luteinizing hormone releasing
hormone (LHRH) expressed in human non-Hodgkin's lymphomas can be
targeted for therapy with the cytotoxic LHRH analogue AN-207. Eur J
Cancer. 2005 Sep;41(14):2196-202. PubMed PMID: 16182122.
2: Stangelberger A, Schally AV, Nagy A, Szepeshazi K, Kanashiro CA,
Halmos G. Inhibition of human experimental prostate cancers by a
targeted cytotoxic luteinizing hormone-releasing hormone analog AN-207.
Prostate. 2006 Feb 1;66(2):200-10. PubMed PMID: 16173040.
3: Engel JB, Keller G, Schally AV, Nagy A, Chism DD, Halmos G. Effective
treatment of experimental human endometrial cancers with targeted
cytotoxic luteinizing hormone-releasing hormone analogues AN-152 and
AN-207. Fertil Steril. 2005 Apr;83 Suppl 1:1125-33. PubMed PMID:
4: Arencibia JM, Bajo AM, Schally AV, Krupa M, Chatzistamou I, Nagy A.
Effective treatment of experimental ES-2 human ovarian cancers with a
cytotoxic analog of luteinizing hormone-releasing hormone AN-207.
Anticancer Drugs. 2002 Oct;13(9):949-56. PubMed PMID: 12394258.
5: Plonowski A, Schally AV, Nagy A, Groot K, Krupa M, Navone NM,
Logothetis C. Inhibition of in vivo proliferation of MDA-PCa-2b human
prostate cancer by a targeted cytotoxic analog of luteinizing
hormone-releasing hormone AN-207. Cancer Lett. 2002 Feb 8;176(1):57-63.
PubMed PMID: 11790454.
6: Arencibia JM, Schally AV, Halmos G, Nagy A, Kiaris H. 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. Anticancer Drugs. 2001 Jan;12(1):71-8. PubMed
7: Chatzistamou L, Schally AV, Nagy A, Armatis P, Szepeshazi K, Halmos
G. Effective treatment of metastatic MDA-MB-435 human
estrogen-independent breast carcinomas with a targeted cytotoxic
analogue of luteinizing hormone-releasing hormone AN-207. Clin Cancer
Res. 2000 Oct;6(10):4158-65. PubMed PMID: 11051271.
8: Kahán Z, Nagy A, Schally AV, Halmos G, Arencibia JM, Groot K.
Complete regression of MX-1 human breast carcinoma xenografts after
targeted chemotherapy with a cytotoxic analog of luteinizing
hormone-releasing hormone, AN-207. Cancer. 1999 Jun 15;85(12):2608-15.
PubMed PMID: 10375109.
9: Miyazaki M, Schally AV, Nagy A, Lamharzi N, Halmos G, Szepeshazi K,
Armatis P. Targeted cytotoxic analog of luteinizing hormone-releasing
hormone AN-207 inhibits growth of OV-1063 human epithelial ovarian
cancers in nude mice. Am J Obstet Gynecol. 1999 May;180(5):1095-103.
PubMed PMID: 10329861.
10: Koppán M, Nagy A, Schally AV, Plonowski A, Halmos G, Arencibia JM,
Groot K. Targeted cytotoxic analog of luteinizing hormone-releasing
hormone AN-207 inhibits the growth of PC-82 human prostate cancer in
nude mice. Prostate. 1999 Feb 1;38(2):151-8. PubMed PMID: 9973101.
11: Danila DC, Schally AV, Nagy A, Alexander JM. Selective induction of
apoptosis by the cytotoxic analog AN-207 in cells expressing recombinant
receptor for luteinizing hormone-releasing hormone. Proc Natl Acad Sci U
S A. 1999 Jan 19;96(2):669-73. PubMed PMID: 9892691; PubMed Central
12: Jungwirth A, Schally A, Nagy A, Pinski J, Groot K, Galvan G,
Szepeshazi K, Halmos G. Regression of rat Dunning R-3327-H prostate
carcinoma by treatment with targeted cytotoxic analog of luteinizing
hormone-releasing hormone AN-207 containing 2-pyrrolinodoxorubicin. Int
J Oncol. 1997 May;10(5):877-84. PubMed PMID: 21533457.
(Keyword; CAS#; MedKoo code#)