Gambogic Acid (Synonyms: Beta-Guttiferrin)

Name: Gambogic Acid
Brand: MedChemExpress
SKU: HY-N0087
Rating: 5.0 (6 reviews)

Cat. No.: HY-N0087 Purity: 98.34%: Data Sheet
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Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC₅₀s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.

For research use only. We do not sell to patients.

CAS No. : 2752-65-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Gambogic Acid:

Gambogic Acid (Standard) Get quote

6 Publications Citing Use of MCE Gambogic Acid

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

In Vivo Efficacy Study

Flow Cytometry

: Gambogic Acid purchased from MedChemExpress. Usage Cited in: Cell Signal. 2025 Nov:135:112024. [Abstract]; Intracellular Fe²⁺ levels were measured using the iron ion assay kit in HCT116 after treatment with GA (Gambogic Acid; 0.5-1 μM; 24 h) at different concentrations (HCT116: 0 μM, 0.5 μM, 1 μM; HT29: 0 μM, 0.75 μM, 1.5 μM).

: Gambogic Acid purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Sep:75:103277. [Abstract]; Analysis of LDH release in E. coli-infected J774A.1 cells treated with GA (Gambogic Acid, 0.5-1 μM). n = 3 per group.

: Gambogic Acid purchased from MedChemExpress. Usage Cited in: Drug Dev Res. 2024 Feb;85(1):e22141.; Liver morphology and nodule status in nude mice 4 weeks after intraperitoneal injection of HT-29 cells and GA (Gambogic Acid; 20 mg/kg) treatment. It was observed that compared to the PC + DMSO group, the PC + GA group had fewer liver metastatic nodules.

: Gambogic Acid purchased from MedChemExpress. Usage Cited in: Drug Dev Res. 2024 Feb;85(1):e22141.; The percentages of CD68 + CD86 cells and CD68 + CD206 cells were measured by flow cytometry, N = 6. The results displayed that relative to the PC + DMSO group, the levels of CD68+CD86 cells in the PC + GA (Gambogic Acid; 20 mg/kg; i.p.; 4 weeks) group obviously rised, while the levels of CD68+CD206 cells were prominently reduced (all p < .001).

: Gambogic Acid purchased from MedChemExpress. Usage Cited in: Sci Rep. 2022 Mar 8;12(1):4038. [Abstract]; Viability of TNBC cell line MDA-MB-231 with Gambogic acid, an antagonist of antiapoptotic Bcl-2 family. Bar graph represents MDA-MB-231 MTT cell viability assay after treatment with Gambogic acid (0.06-1 μM) in the combination of with/without CAP treatment at 80p 5 min at 3 L/min He.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Bcl-B

0.66 μM (IC₅₀)

Mcl-1

0.79 μM (IC₅₀)

Bfl-1

1.06 μM (IC₅₀)

Bcl-2

1.21 μM (IC₅₀)

Bcl-xL

1.47 μM (IC₅₀)

Bcl-W

2.02 μM (IC₅₀)

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.29 μM Compound: Gambogic acid	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
A549	IC₅₀	0.5 μg/mL Compound: GA	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	[PMID: 22595179]
A549	IC₅₀	1.1 μM Compound: 1, GA	Cytotoxicity against human A549 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human A549 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 23167526]
A549	IC₅₀	1.1 μM Compound: GA	Antiproliferative activity against human A549 cells after 24 hrs by MTT assay Antiproliferative activity against human A549 cells after 24 hrs by MTT assay	[PMID: 22472167]
A549	IC₅₀	1.1 μM Compound: GA	Cytotoxicity against human A549 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 25958244]
A549	IC₅₀	1.2 μM Compound: 1; GA	Antiproliferative activity against human A549 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human A549 cells assessed as growth inhibition by MTT assay	[PMID: 27527413]
A549	IC₅₀	1.47 μM Compound: GA	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31047774]
A549	IC₅₀	3.4 μM Compound: 4	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 to 48 hrs by Presto Blue assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 to 48 hrs by Presto Blue assay	[PMID: 27216998]
A549	IC₅₀	3.65 μM Compound: GA	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 20605273]
A549	IC₅₀	5.81 μM Compound: gambogic acid, GA	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 18996626]
A549/CDDP	IC₅₀	0.29 μM Compound: Gambogic acid	Antiproliferative activity against human A549/CDDP cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549/CDDP cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
A549/TR	IC₅₀	0.29 μM Compound: Gambogic acid	Antiproliferative activity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
Bel-7402	IC₅₀	0.75 μM Compound: 1, GA	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 22153338]
Bel-7402	IC₅₀	2.08 μM Compound: GA	Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay	[PMID: 20605273]
Bel-7402	IC₅₀	3.31 μM Compound: gambogic acid, GA	Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay	[PMID: 18996626]
BEL-7404 tumor cell line	IC₅₀	4.7 μM Compound: 1, GA	Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay	[PMID: 22153338]
BGC-823	IC₅₀	2.35 μM Compound: 1, GA	Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay	[PMID: 21334116]
BGC-823	IC₅₀	2.83 μM Compound: GA	Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay	[PMID: 20605273]
BGC-823	IC₅₀	4.51 μM Compound: gambogic acid, GA	Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay	[PMID: 18996626]
BJ	EC₅₀	0.21 μM Compound: Gambogic acid	Cytotoxicity against human BJ cells Cytotoxicity against human BJ cells	[PMID: 25316317]
Breast carcinoma cell	IC₅₀	0.42 μM Compound: GBA; 1	Cytotoxicity against patient derived inflammatory breast cancer cell spheroids assessed as increase in spheroid dissolution incubated for 24 hrs by propidium iodide/Acridine orange staining based dual-fluorescence viability assay Cytotoxicity against patient derived inflammatory breast cancer cell spheroids assessed as increase in spheroid dissolution incubated for 24 hrs by propidium iodide/Acridine orange staining based dual-fluorescence viability assay	[PMID: 30831408]
DU-145	IC₅₀	0.3 μg/mL Compound: GA	Cytotoxicity against human DU145 cells by MTT assay Cytotoxicity against human DU145 cells by MTT assay	[PMID: 22595179]
HCT-116	EC₅₀	0.7 μM Compound: 1, GA	Induction of apoptosis in human HCT116 cells assessed as caspase 3 activation after 24 hrs Induction of apoptosis in human HCT116 cells assessed as caspase 3 activation after 24 hrs	[PMID: 18337106]
HCT-116	GI₅₀	0.1 μM Compound: 1, GA	Growth inhibition of human HCT116 cells after 48 hrs by CellTiter-Glo assay Growth inhibition of human HCT116 cells after 48 hrs by CellTiter-Glo assay	[PMID: 18337106]
HCT-116	IC₅₀	0.29 μM Compound: Gambogic acid	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
HCT-116	IC₅₀	3.11 μM Compound: GA	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay	[PMID: 31047774]
HEK293	EC₅₀	0.21 μM Compound: Gambogic acid	Cytotoxicity against HEK293 cells Cytotoxicity against HEK293 cells	[PMID: 25316317]
HEK293	IC₅₀	1.72 μM Compound: 4	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 24 to 48 hrs by trypan blue dye based fluorescence assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 24 to 48 hrs by trypan blue dye based fluorescence assay	[PMID: 27216998]
HeLa	GI₅₀	1.5 μM Compound: 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay	[PMID: 21486005]
HeLa	IC₅₀	0.7 μM Compound: 6a, R-gambogic acid	Cytotoxicity against human HeLa cells after 1 to 11 days by MTT assay Cytotoxicity against human HeLa cells after 1 to 11 days by MTT assay	[PMID: 19072548]
HepG2	EC₅₀	<2 μM Compound: Gambogic acid	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 25316317]
HepG2	IC₅₀	0.29 μM Compound: Gambogic acid	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
HepG2	IC₅₀	0.89 μM Compound: 1, GA	Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 23167526]
HepG2	IC₅₀	0.89 μM Compound: GA	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 25958244]
HepG2	IC₅₀	1.17 μM Compound: 1, GA	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 22153338]
HepG2	IC₅₀	1.55 μM Compound: Gambogic acid	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay	[PMID: 30594028]
HepG2	IC₅₀	2.19 μM Compound: 1; GA	Antiproliferative activity against human HepG2 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human HepG2 cells assessed as growth inhibition by MTT assay	[PMID: 27527413]
HepG2	IC₅₀	2.36 μM Compound: GA	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay	[PMID: 31047774]
HepG2	IC₅₀	2.4 μM Compound: 1, GA	Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 21334116]
HepG2	IC₅₀	2.4 μM Compound: GA	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 20338759]
HL-60	GI₅₀	0.3 μM Compound: Gambogic acid	Growth inhibition of human HL60 cells measured after 3 days by trypan blue assay Growth inhibition of human HL60 cells measured after 3 days by trypan blue assay	[PMID: 29565129]
HL-60	IC₅₀	0.17 μM Compound: 54	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 3 days by trypan blue dye based hemocytometer counting method Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 3 days by trypan blue dye based hemocytometer counting method	[PMID: 30830783]
HT-29	ED₅₀	0.48 μM Compound: 1	Anticancer activity aganist human HT-29 cells Anticancer activity aganist human HT-29 cells	[PMID: 21067206]
HT-29	IC₅₀	2.37 μM Compound: 1; GA	Antiproliferative activity against human HT-29 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human HT-29 cells assessed as growth inhibition by MTT assay	[PMID: 27527413]
HT-29	IC₅₀	3.52 μM Compound: GA	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 20605273]
HT-29	IC₅₀	5.61 μM Compound: gambogic acid, GA	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 18996626]
K562	GI₅₀	0.6 μM Compound: Gambogic acid	Growth inhibition of human K562 cells measured after 3 days by trypan blue assay Growth inhibition of human K562 cells measured after 3 days by trypan blue assay	[PMID: 29565129]
K562	IC₅₀	0.62 μM Compound: Gambogic acid	Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 48 to 72 hrs by MTS assay Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 48 to 72 hrs by MTS assay	[PMID: 35551036]
KB	IC₅₀	0.3 μg/mL Compound: GA	Cytotoxicity against human KB cells by MTT assay Cytotoxicity against human KB cells by MTT assay	[PMID: 22595179]
MCF7	GI₅₀	2 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay	[PMID: 21486005]
MCF7	IC₅₀	0.5 μM Compound: GA	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 20338759]
MCF7	IC₅₀	1.25 μM Compound: 1; GA	Antiproliferative activity against human MCF7 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition by MTT assay	[PMID: 27527413]
MCF7	IC₅₀	2.19 μM Compound: 1, GA	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 21334116]
MDA-MB-231	IC₅₀	1.33 μM Compound: GA	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 31047774]
MKN-45	IC₅₀	4.27 μM Compound: GA	Antiproliferative activity against human MKN45 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells incubated for 72 hrs by MTT assay	[PMID: 31047774]
PC-3	IC₅₀	1.19 μM Compound: 1; GA	Antiproliferative activity against human PC3 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human PC3 cells assessed as growth inhibition by MTT assay	[PMID: 27527413]
Raji	EC₅₀	0.24 μM Compound: Gambogic acid	Cytotoxicity against human Raji cells Cytotoxicity against human Raji cells	[PMID: 25316317]
SGC-7901	IC₅₀	1.47 μM Compound: GA	Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay	[PMID: 20338759]
SK-BR-3	GI₅₀	0.8 μM Compound: 1	Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay	[PMID: 21486005]
SK-BR-3	IC₅₀	0.89 μM Compound: 1; GA	Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition by MTT assay	[PMID: 27527413]
SK-OV-3	IC₅₀	3.06 μM Compound: gambogic acid, GA	Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay	[PMID: 18996626]
SMMC-7721	IC₅₀	1.13 μM Compound: 1, GA	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay	[PMID: 22153338]
SMMC-7721	IC₅₀	3.2 μM Compound: 1, GA	Antiproliferative activity against human SMMC7721 cells after 24 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells after 24 hrs by MTT assay	[PMID: 21334116]
SNU-398	EC₅₀	0.7 μM Compound: 1, GA	Induction of apoptosis in human SNU398 cells assessed as caspase 3 activation after 24 hrs Induction of apoptosis in human SNU398 cells assessed as caspase 3 activation after 24 hrs	[PMID: 18337106]
SNU-398	GI₅₀	0.2 μM Compound: 1, GA	Growth inhibition of human SNU398 cells after 48 hrs by CellTiter-Glo assay Growth inhibition of human SNU398 cells after 48 hrs by CellTiter-Glo assay	[PMID: 18337106]
T47D	EC₅₀	0.7 μM Compound: 1, GA	Induction of apoptosis in human T47D cells assessed as caspase 3 activation after 24 hrs Induction of apoptosis in human T47D cells assessed as caspase 3 activation after 24 hrs	[PMID: 18337106]
T47D	GI₅₀	0.2 μM Compound: 1, GA	Growth inhibition of human T47D cells after 48 hrs by CellTiter-Glo assay Growth inhibition of human T47D cells after 48 hrs by CellTiter-Glo assay	[PMID: 18337106]
T98G	IC₅₀	<=300 nM Compound: GA	Antiproliferative activity against human T98G cells after 24 hrs by EZ-Tox assay Antiproliferative activity against human T98G cells after 24 hrs by EZ-Tox assay	[PMID: 26631318]
T98G	IC₅₀	≤ 300 nM Compound: GA	Antiproliferative activity against human T98G cells after 24 hrs by EZ-Tox assay Antiproliferative activity against human T98G cells after 24 hrs by EZ-Tox assay	[PMID: 26631318]
U-251	IC₅₀	0.29 μM Compound: Gambogic acid	Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
U-251	IC₅₀	2.56 μM Compound: 1, GA	Cytotoxicity against human U251 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human U251 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 23167526]
U-251	IC₅₀	2.56 μM Compound: GA	Antiproliferative activity against human U251 cells after 24 hrs by MTT assay Antiproliferative activity against human U251 cells after 24 hrs by MTT assay	[PMID: 22472167]
U-251	IC₅₀	2.56 μM Compound: GA	Cytotoxicity against human U251 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human U251 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 25958244]

In Vitro

Gambogic Acid (Beta-Guttiferrin) is a medicinal compound derived from the gamboges resin of the tree, Garcinia hanburyi. Gambogic Acid has documented cytotoxic activity against tumor cell lines in culture, with concentrations required for killing 50% of cells (LD₅₀ of ~1 μM). The activity of Gambogic Acid against the 6 human anti-apoptotic Bcl-2-family proteins is contrasted, using FPAs. Gambogic Acid displaces to various extents FITC-BH3 peptide binding to all 6 proteins, with apparent IC₅₀ 1.47 μM for Bcl-X_L, 1.21 μM for Bcl-2, 2.02 μM for Bcl-W, 0.66 μM for Bcl-B, 1.06 μM for Bfl-1, and 0.79 μM for Mcl-1^[1]. The growth inhibitory effects of Gambogic Acid or Cisplatin (CDDP) on A549, NCI-H460, and NCI-H1299 cells are assessed by the MTT assay after 48?h exposure. A concentration-dependent inhibition of cell growth is observed with Gambogic Acid and CDDP, with IC₅₀s of 3.56±0.36 and 21.88±3.21?μM for A549 cells, 4.05±0.51 and 25.76±4.03?μM for NCI-H460 cells, and 1.12±0.31?μM and 25.21±4.38?μM for NCI-H1299 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

To further investigate whether Gambogic Acid (Beta-Guttiferrin) synergises CDDP against tumour growth in vivo, A549 tumors are implanted in SCID mice. When mice are treated with CDDP combined with Gambogic Acid, the tumor inhibition rate is 69.3%, whereas those of mice treated with CDDP and GA alone are 57.2% and 29.0%, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

628.75

Formula

C₃₈H₄₄O₈

CAS No.

2752-65-0

Appearance

Solid

Color

Yellow to orange

SMILES

O=C(O)/C(C)=C\C[C@@]1(C2=O)OC(C)(C)[C@@](C[C@@]2([H])C=C34)([H])[C@]31OC5=C(C(O)=C(C=C[C@](CC/C=C(C)/C)(C)O6)C6=C5C/C=C(C)\C)C4=O

Structure Classification

Others

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (79.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5905 mL	7.9523 mL	15.9046 mL
5 mM	0.3181 mL	1.5905 mL	3.1809 mL
10 mM	0.1590 mL	0.7952 mL	1.5905 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.34%

Select Batch:

Data Sheet (284 KB) SDS (479 KB)

COA (257 KB) HNMR (290 KB) RP-HPLC (260 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Zhai D, et al. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2008 Jun;7(6):1639-46. [Content Brief]

[2]. Wang LH, et al. Gambogic acid synergistically potentiates cisplatin-induced apoptosis in non-small-cell lung cancer through suppressing NF-κB and MAPK/HO-1 signalling. Br J Cancer. 2014 Jan 21;110(2):341-52. [Content Brief]

Cell Assay ^[2]	The in vitro cell viability effects of Gambogic Acid, CDDP alone, or combined treatments are determined by MTT assay. The cells (2×10⁴ cells per mL) are seeded into 96-well culture plates. After overnight incubation, A549 cells are treated with Gambogic Acid (0.44, 0.88, 1.75, 3.5, 7, 10.5 and 14 μM); NCI-H460 cells are treated with Gambogic Acid (0.5, 1, 2, 4, 8, 12 and 16 μM); NCI-H1299 cells are treated with Gambogic Acid (0.125, 0.25, 0.5, 1, 2 and 4 μM). For the combined treatment in NSCLC cells, three sequences are tested: (a) Gambogic Acid followed by CDDP cells are exposed to Gambogic Acid for 48 h, and then after washout of Gambogic Acid, cells are treated with CDDP for an additional 48 h; (b) CDDP followed by Gambogic Acid cells are exposed to CDDP for 48 h, and then after washout of CDDP, cells are treated with Gambogic Acid for an additional 48 h; and (c) concurrent treatment cells are exposed to both Gambogic Acid and ADM for 48 h. The nature of the drug interaction is analysed by using the combination index (CI)^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] To determine the in vivo antitumour activity of Gambogic Acid combined with CDDP, viable A549 cells (5×10⁶/100 μL PBS per mouse) are subcutaneously injected into the right flank of 7- to 8-week-old male SCID mice. When the average tumor volume reach 100 mm³, the mice are randomly divided into four treatment groups, including control (saline only, n=5), Gambogic Acid (3.0 mg/kg per 2 days, intravenously; n=6), CDDP (4 mg/kg per week, intravenously; n=6), and sequential combination (CDDP treatment one day before Gambogic Acid treatment, n=6). CDDP (4 mg/kg, weekly) is generally administered at doses less than the maximum-tolerated dose in an attempt to allow any additive effects of combination treatment with platinum-based agents and Gambogic Acid to be more easily detected. Tumor size is measured once every 2 days with a calipre. Body weight is recorded once every 2 days. After 14 days, the mice are killed and the tumors are excised and stored at -80 °C until further analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhai D, et al. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2008 Jun;7(6):1639-46. [Content Brief] [2]. Wang LH, et al. Gambogic acid synergistically potentiates cisplatin-induced apoptosis in non-small-cell lung cancer through suppressing NF-κB and MAPK/HO-1 signalling. Br J Cancer. 2014 Jan 21;110(2):341-52. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5905 mL	7.9523 mL	15.9046 mL	39.7614 mL
	5 mM	0.3181 mL	1.5905 mL	3.1809 mL	7.9523 mL
	10 mM	0.1590 mL	0.7952 mL	1.5905 mL	3.9761 mL
	15 mM	0.1060 mL	0.5302 mL	1.0603 mL	2.6508 mL
	20 mM	0.0795 mL	0.3976 mL	0.7952 mL	1.9881 mL
	25 mM	0.0636 mL	0.3181 mL	0.6362 mL	1.5905 mL
	30 mM	0.0530 mL	0.2651 mL	0.5302 mL	1.3254 mL
	40 mM	0.0398 mL	0.1988 mL	0.3976 mL	0.9940 mL
	50 mM	0.0318 mL	0.1590 mL	0.3181 mL	0.7952 mL
	60 mM	0.0265 mL	0.1325 mL	0.2651 mL	0.6627 mL

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Gambogic Acid2752-65-0Beta-GuttiferrinBcl-2 FamilyAutophagyInhibitorinhibitorinhibit

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Gambogic Acid (Synonyms: Beta-Guttiferrin)

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