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BIOLOGICAL INFO
Solubility:
DMSO
Application(s):
Iinhibitor of the Bcl-2 family of proteins
Form:
Mesylate
Research Area:
Cancer
REVIEW 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. It is in Phase II clinical trials for the treatment of leukemia, lymphoma, myelofibrosis, and mastocytosis. Obatoclax is an inhibitor of the Bcl-2 family of proteins. is a novel Bcl-2 homology domain-3 (BH3) mimetic. This inhibition induces apoptosis in cancer cells, preventing tumor growth.
REFERENCES
[1]
Konopleva M, Watt J, Contractor R, Tsao T, Harris D, Estrov Z, Bornmann W, Kantarjian H, Viallet J, Samudio I, Andreeff M. Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax). Cancer Res. 2008 May 1;68(9):3413-20.
[2]
Li J, Viallet J, Haura EB. A small molecule pan-Bcl-2 family inhibitor, GX15-070, induces apoptosis and enhances cisplatin-induced apoptosis in non-small cell lung cancer cells. Cancer Chemother Pharmacol. 2008 Mar;61(3):525-34.
[3]
Schimmer AD, O'Brien S, Kantarjian H, Brandwein J, Cheson BD, Minden MD, Yee K, Ravandi F, Giles F, Schuh A, Gupta V, Andreeff M, Koller C, Chang H, Kamel-Reid S, Berger M, Viallet J, Borthakur G. A phase I study of the pan bcl-2 family inhibitor obatoclax mesylate in patients with advanced hematologic malignancies. Clin Cancer Res. 2008 Dec 15;14(24):8295-301.
[4]
Schimmer AD, O'Brien S, Kantarjian H, Brandwein J, Cheson BD, Minden MD, Yee K, Ravandi F, Giles F, Schuh A, Gupta V, Andreeff M, Koller C, Chang H, Kamel-Reid S, Berger M, Viallet J, Borthakur G. A phase I study of the pan bcl-2 family inhibitor obatoclax mesylate in patients with advanced hematologic malignancies. Clin Cancer Res. 2008 Dec 15;14(24):8295-301.
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