Obatoclax
 | |
| Names | |
|---|---|
| IUPAC name
2-(2-((3,5-Dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-1H-indole | |
| Other names
GX15-070 | |
| Identifiers | |
803712-67-6  803712-79-0 (mesylate) | |
| ChemSpider | 24539359 |
| |
| Jmol-3D images | Image |
| PubChem | 11404337 16681698 (mesylate) |
| |
| Properties | |
| Molecular formula |
C20H19N3O |
| Molar mass | 317.38 g·mol−1 |
| Except where noted otherwise, data is given for materials in their standard state (at 25 °C (77 °F), 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.