Description
Apogossypolone (ApoG2) is a pan Bcl-2 inhibitor for Bcl-2, Bcl-XL and Mcl-1 with IC50 of 35 nM, 660 nM and 25 nM, respectively.
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
Bcl-2, Bcl-XL, Mcl-1
IC50
35 nM; 660 nM; 25 nM
Molecular Formula
C28H26O8
Chemical Name
[2,2'-Binaphthalene]-1,1',4,4'-tetrone, 6,6',7,7'-tetrahydroxy-3,3'-dimethyl-5,5'-bis(1-methylethyl)-
Solubility
DMSO mg/mL; Water mg/mL; Ethanol mg/mL
In vitro
Apogossypolone (ApoG2) is a semi-synthesized derivative of Gossypol. ApoG2 is a pan Bcl-2 inhibitor for Bcl-2, Bcl-XL and Mcl-1 with IC50 of 35 nM, 660 nM and 25 nM, respectively. ApoG2 blocks the formation of heterodimers between Bcl-XL and Bim. ApoG2 effectively inhibits growth of DLCL2 cells at least partly by inducing apoptosis, with IC50 of 350 nM for a treatment of 72 h. ApoG2 inhibits the growth of WSU-FSCCL, with IC50 of 109 nM, and decreases cell number of fresh lymphoma cells. ApoG2 activates caspases-9, -3, and -8, and the cleavage of PARP and AIF.ApoG2 selectively inhibits the proliferation of 3 nasopharyngeal carcinoma (NPC) cell lines (C666-1, CNE-1 and CNE-2) that highly expresses Bcl-2 proteins, with IC50 values of 1.7, 2.055, 4.915 μM.ApoG2 inhibits proliferation of breast cancer cell line MCF-7 by inducing cell apoptosis and autophagy, with 89.20% inhibition for ApoG2 at 40 μM at 72 h.ApoG2 induces ER stress-dependent apoptosis in gastric cancer cells, with IC50 of 18.7 μM at 72 h.
In vivo
ApoG2 treatment at 600 mg/kg results in significant growth inhibition of WSU-DLCL2 xenografts. In the WSU-FSCCL-SCID xenograft model, ApoG2 shows a significant antilymphoma effect, with %ILS of 84% in the intravenous and 63% in intraperitoneal treated mice.ApoG2 effectively suppresses tumor growth of NPC xenografts in nude mice.ApoG2 has anticancer effect in subcutaneous gastric cancer cell xenografts in mice.
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