Obatoclax

• CAT Number: I004929
• CAS Number: 803712-79-0
• Molecular Formula: C20H19N3O • CH3SO3H
• Molecular Weight: 413.5
• Purity: ≥95%
• Target: Bcl-2 Family
• Solubility: DMSO: ≥ 48.8 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 3 uM
• IUPAC Name: (2Z)-2-[(5Z)-5-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-4-methoxypyrrol-2-ylidene]indole;methanesulfonic acid
• InChI: InChI=1S/C20H19N3O.CH4O3S/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;1-5(2,3)4/h4-11,21,23H,1-3H3;1H3,(H,2,3,4)/b18-17-,19-10-
• InChIKey: ZVAGBRFUYHSUHA-LZOXOEDVSA-N
• SMILES: CC1=CC(=C(N1)C=C2C(=CC(=C3C=C4C=CC=CC4=N3)N2)OC)C.CS(=O)(=O)O

Obatoclax (Cat.No:I004929) is a synthetic small molecule that functions as a pan-Bcl-2 inhibitor. It targets the Bcl-2 family of proteins, which play a role in regulating apoptosis. Obatoclax has shown potential as an anticancer agent, disrupting the survival pathways in cancer cells and inducing apoptosis. Clinical trials are underway to evaluate its therapeutic efficacy.

Reference

[1]. Marina Konopleva et al Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax) Cancer Res May 1, 2008 68; 3413
[2]. Oki Y, Copeland A, Hagemeister F, Fayad LE, Fanale M, Romaguera J, Younes A.Experience with obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist in patients with relapsed or refractory classical Hodgkin lymphoma.Blood. 2012 Mar 1;119(9):2171-2.
[3]. Joudeh J, Claxton D.Obatoclax mesylate : pharmacology and potential for therapy of hematological neoplasms.Expert Opin Investig Drugs. 2012 Mar;21(3):363-73. Epub 2012 Feb 11.
[4]. Parikh SA, Kantarjian H, Schimmer A, Walsh W, Asatiani E, El-Shami K, Winton E, Verstovsek S.Phase II study of obatoclax mesylate (GX15-070), a small-molecule BCL-2 family antagonist, for patients with myelofibrosis.Clin Lymphoma Myeloma Leuk. 2010 Aug;10(4):285-9.
[5]. Paik PK, Rudin CM, Brown A, Rizvi NA, Takebe N, Travis W, James L, Ginsberg MS, Juergens R, Markus S, Tyson L, Subzwari S, Kris MG, Krug LM.A phase I study of obatoclax mesylate, a Bcl-2 antagonist, plus topotecan in solid tumor malignancies.Cancer Chemother Pharmacol. 2010 Nov;66(6):1079-85. Epub 2010 Feb 18.