- Obatoclax
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Obatoclax 
2-(2-((3,5-Dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-1H-indoleOther namesGX15-070Identifiers CAS number 803712-67-6 
, 803712-79-0 (mesylate) PubChem 11404337, 16681698 (mesylate) ChemSpider 24539359 Jmol-3D images Image 1 - Cc1cc([nH]c1/C=C/2\C(=CC(=N2)c3cc4ccccc4[nH]3)OC)C
- InChI=1S/C20H19N3O/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17/h4-11,21-22H,1-3H3/b19-10+
Properties Molecular formula C20H19N3O Molar mass 317.38 g mol−1 Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) Infobox references Obatoclax is an experimental drug candidate for the treatment of various types of cancer. It was discovered by Gemin X, which was acquired by Cephalon.[1] It is in Phase II clinical trials for the treatment of leukemia, lymphoma, myelofibrosis, and mastocytosis.[2][3][4]
Mechanism of action
Obatoclax is an inhibitor of the Bcl-2 family of proteins.[5] This inhibition induces apoptosis in cancer cells, preventing tumor growth.
References
- ^ Cephalon Announces Definitive Agreement to Acquire Gemin X, March 21, 2011
- ^ Parikh, Sameer A.; Kantarjian, Hagop; Schimmer, Aaron; Walsh, William; Asatiani, Ekatherine; El-Shami, Khaled; Winton, Elliott; Verstovsek, Srdan (2010). "Phase II study of obatoclax mesylate (GX15-070), a small-molecule BCL-2 family antagonist, for patients with myelofibrosis". Clinical Lymphoma, Myeloma & Leukemia 10 (4): 285–289. doi:10.3816/CLML.2010.n.059.
- ^ Gemin X Presents New Data on Obatoclax at the American Society of Hematology Meeting, Dec 9, 2008
- ^ Obatoclax at ClinicalTrials.gov
- ^ Konopleva, Marina; Watt, Julie; Contractor, Rooha; Tsao, Twee; Harris, David; Estrov, Zeev; Bornmann, William; Kantarjian, Hagop; Viallet, Jean; Samudio, Ismael; Andreeff, Michael (2008). "Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax)". Cancer Research 68 (9): 3413–3420. doi:10.1158/0008-5472.CAN-07-1919. PMID 18451169.
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