Obatoclax

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Obatoclax
Obatoclax.svg
Identifiers
CAS number 803712-67-6 YesY, 803712-79-0 (mesylate) YesY
PubChem 11404337, 16681698 (mesylate)
ChemSpider 24539359
Jmol-3D images Image 1
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 (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[edit]

Obatoclax is an inhibitor of the Bcl-2 family of proteins.[5] This inhibition induces apoptosis in cancer cells, preventing tumor growth.

References[edit]

  1. ^ Cephalon Announces Definitive Agreement to Acquire Gemin X, March 21, 2011
  2. ^ 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. 
  3. ^ Gemin X Presents New Data on Obatoclax at the American Society of Hematology Meeting, Dec 9, 2008
  4. ^ Obatoclax at ClinicalTrials.gov
  5. ^ 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. 

See also[edit]