CF-102, also known as 2-Cl-IB-MECA, is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. Adenosine A3 receptor agonist CF102 selectively binds to and activates the cell surface-expressed A3AR, deregulating Wnt and NF-kB signal transduction pathways downstream, which may result in apoptosis of A3AR-expressing tumor cells. A3AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of various solid tumor cell types, including hepatocellular carcinoma (HCC) cells, and plays an important role in cellular proliferation.
1: Soares AS, Costa VM, Diniz C, Fresco P. The combination of Cl-IB-MECA with paclitaxel: a new anti-metastatic therapeutic strategy for melanoma. Cancer Chemother Pharmacol. 2014 Oct;74(4):847-60. doi: 10.1007/s00280-014-2557-y. Epub 2014 Aug 14. PubMed PMID: 25119183.
2: Soares AS, Costa VM, Diniz C, Fresco P. Potentiation of cytotoxicity of paclitaxel in combination with Cl-IB-MECA in human C32 metastatic melanoma cells: A new possible therapeutic strategy for melanoma. Biomed Pharmacother. 2013 Oct;67(8):777-89. doi: 10.1016/j.biopha.2013.08.003. Epub 2013 Aug 23. PubMed PMID: 24035253.
3: Kim GD, Oh J, Jeong LS, Lee SK. Thio-Cl-IB-MECA, a novel A3 adenosine receptor agonist, suppresses angiogenesis by regulating PI3K/AKT/mTOR and ERK signaling in endothelial cells. Biochem Biophys Res Commun. 2013 Jul 19;437(1):79-86. doi: 10.1016/j.bbrc.2013.06.040. Epub 2013 Jun 21. PubMed PMID: 23791876.
4: Montinaro A, Forte G, Sorrentino R, Luciano A, Palma G, Arra C, Adcock IM, Pinto A, Morello S. Adoptive immunotherapy with Cl-IB-MECA-treated CD8+ T cells reduces melanoma growth in mice. PLoS One. 2012;7(9):e45401. doi: 10.1371/journal.pone.0045401. Epub 2012 Sep 24. PubMed PMID: 23028986; PubMed Central PMCID: PMC3454429.
5: Kim TH, Kim YK, Woo JS. The adenosine A3 receptor agonist Cl-IB-MECA induces cell death through Ca2⁺/ROS-dependent down regulation of ERK and Akt in A172 human glioma cells. Neurochem Res. 2012 Dec;37(12):2667-77. doi: 10.1007/s11064-012-0855-5. Epub 2012 Aug 10. PubMed PMID: 22878643.
6: Lee HS, Chung HJ, Lee HW, Jeong LS, Lee SK. Suppression of inflammation response by a novel A3 adenosine receptor agonist thio-Cl-IB-MECA through inhibition of Akt and NF-κB signaling. Immunobiology. 2011 Sep;216(9):997-1003. doi: 10.1016/j.imbio.2011.03.008. Epub 2011 Apr 7. PubMed PMID: 21514967.
7: Morello S, Sorrentino R, Montinaro A, Luciano A, Maiolino P, Ngkelo A, Arra C, Adcock IM, Pinto A. NK1.1 cells and CD8 T cells mediate the antitumor activity of Cl-IB-MECA in a mouse melanoma model. Neoplasia. 2011 Apr;13(4):365-73. PubMed PMID: 21472141; PubMed Central PMCID: PMC3071085.
8: Forte G, Sorrentino R, Montinaro A, Pinto A, Morello S. Cl-IB-MECA enhances TNF-α release in peritoneal macrophages stimulated with LPS. Cytokine. 2011 May;54(2):161-6. doi: 10.1016/j.cyto.2011.02.002. Epub 2011 Feb 26. PubMed PMID: 21354814.
9: Kim H, Kang JW, Lee S, Choi WJ, Jeong LS, Yang Y, Hong JT, Yoon do Y. A3 adenosine receptor antagonist, truncated Thio-Cl-IB-MECA, induces apoptosis in T24 human bladder cancer cells. Anticancer Res. 2010 Jul;30(7):2823-30. PubMed PMID: 20683018.
10: Morello S, Sorrentino R, Porta A, Forte G, Popolo A, Petrella A, Pinto A. Cl-IB-MECA enhances TRAIL-induced apoptosis via the modulation of NF-kappaB signalling pathway in thyroid cancer cells. J Cell Physiol. 2009 Nov;221(2):378-86. doi: 10.1002/jcp.21863. PubMed PMID: 19562684.
Chemical |
CAS Num |
163042-96-4 |
Chemical Formula |
C18H18ClIN6O4 |
Molecular Weight |
544.73079 |
IUPAC Chemical Name |
(2S,3S,4R,5R)-5-(2-chloro-6-((3-iodobenzyl)amino)-9H-purin-9-yl)-3,4-dihydroxy-N-methyltetrahydrofuran-2-carboxamide |
Exact Mass |
544.01227 |
Elemental Analysis |
C, 39.69; H, 3.33; Cl, 6.51; I, 23.30; N, 15.43; O, 11.75 |
Synonym |
CF102; CF-102; CF 102; Cl-IB-MECA; 2-Cl-IB-MECA. |
Solubility |
Soluble in DMSO, not in water |
SMILES Code |
O[C@H]1[C@H](N2C=NC3=C(NCC4=CC=CC(I)=C4)N=C(Cl)N=C23)O[C@H](C(NC)=O)[C@H]1O |
Biological |
Targets and Effects |
N/A |
Pathways |
Apoptosis |
Physical |
Appearance |
Solid powder |
Purity |
>98% (or refer to the Certificate of Analysis) |
Shipping Condition |
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition |
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life |
>2 years if stored properly |