Technical Data

255353
CAS Number
2752-65-0
Grade
Purified
Molecular Formula
C38H44O8
Molecular Weight
628.75
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
4°C
Gambogic Acid
(2Z)-2-Methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-butenyl)-11-(4-methyl-3-pentenyl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-2-butenoic acid

Gambogic Acid is an apoptosis inducer in sever tumor cell lines via regulation of Bax and inhibition of Bcl-2 genes. Induces EGFR degredation through AMPK dependant-LRIG1 upregulation in glioma cells. Apoptosis inducer in several tumor cell lines including T47D cells. Activates caspases (EC50 values are 0.78 - 1.64uM) and competitively inhibits antiapoptotic Bcl-2 family proteins (IC50 values are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79uM for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 respectively). Reverses gefitinib-resistance in mice bearing tumors with EGFR-T790M mutation. Also blocks Kir2.1 channels (EC50 ≤100nM).

Molecular Formula
C38H44O8
Molecular Weight
628.75
Storage and Stability
Store at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.

References
Zhang et al (2004) Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay. Bioorg.Med.Chem. 12 309 PMID: 14723951|Zhai et al (2008) Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol.Cancer Ther. 7 1639 PMID: 18566235|Qi et al (2008) Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells. Biochem.Cell Biol. 86 386 PMID: 18923540|Zaks-Makhina et al (2009) Specific and slow inhibition of the Kir2.1 K+ channel by Gambogic acid. J.Biol.Chem. 284 15432 PMID: 19366693|Wang et al (2015) Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer. Oncol.Lett. 10 2063 PMID: 26622796
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