| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
FGFR; EZH2
Gambogenic acid targets multiple cellular pathways involved in cancer cell survival and proliferation. It has been shown to induce apoptosis through the mitochondrial pathway, involving the activation of caspases and the modulation of Bcl-2 family proteins. Gambogenic acid also inhibits the NF-κB signaling pathway, which is involved in inflammation and cancer. The compound's anticancer activity is mediated through its effects on cell cycle regulation and apoptosis. |
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| ln Vitro |
Gambogenic acid is a novel agent that specifically and covalently binds to Cys668 within the EZH2‐SET domain, causing EZH2 degradation through ubiquitination at the COOH terminus of the Hsp70-interacting protein (CHIP). Gambogenic acid effectively reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes and significantly suppresses H3K27Me3. In an EZH2-dependent manner, gambogenic acid significantly suppresses the growth of tumors.[1]
In vitro, Gambogenic acid has been shown to inhibit the proliferation of various cancer cell lines, including breast, lung, liver, and colon cancer cells. It induces apoptosis in a concentration-dependent manner, as evidenced by the activation of caspases and the cleavage of PARP. Gambogenic acid also inhibits the migration and invasion of cancer cells. The compound has been shown to have anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines. |
| ln Vivo |
Gambogenic acid derivative GNA002 dramatically lowers H3K27Me3 levels in tumor tissues and the volumes of tumors derived from Cal-27 in xenograft mice.
In vivo, Gambogenic acid has been shown to inhibit tumor growth in xenograft mouse models of various cancers. The compound is typically administered intraperitoneally or intravenously. Gambogenic acid has been shown to reduce tumor volume and weight in a dose-dependent manner. The compound's anticancer activity is associated with the induction of apoptosis and the inhibition of angiogenesis in the tumor tissue. |
| Enzyme Assay |
In vitro enzyme inhibition assays for Gambogenic acid typically involve measuring its effect on various kinases and other enzymes involved in cancer cell signaling. The compound is incubated with the enzyme and its substrate, and the enzymatic activity is measured. The IC50 value for inhibition of the enzyme is determined. The selectivity of Gambogenic acid for different enzymes can be assessed.
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| Cell Assay |
GNA002 or 2 μM GNA is applied to cancer cells for a full day. Subsequently, the cells are collected and mixed again with 500 μl of binding buffer. Different cell dyes are added to the 100 μl of cell suspension and incubated. Fluorescence-activated cell sorting is used to analyze the stained cells using a flow cytometry apparatus.
In vitro cell-based studies with Gambogenic acid typically involve cultured cancer cell lines. Cells are treated with Gambogenic acid at various concentrations for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining or by detecting caspase activity. The effect of Gambogenic acid on cell cycle progression and signaling pathways is examined by Western blot analysis. |
| Animal Protocol |
In vivo animal studies with Gambogenic acid are typically conducted in xenograft mouse models. Tumor-bearing mice are treated with Gambogenic acid via intraperitoneal or intravenous administration at various doses. Tumor growth is measured over time, and tumor growth inhibition is calculated. Tumor tissues are collected for histopathological analysis and for assessment of apoptosis and angiogenesis markers. Pharmacokinetic studies are performed by measuring compound concentrations in plasma and tissues.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Gambogenic acid have been studied in preclinical settings. Following administration, the compound is distributed to various tissues. Gambogenic acid is metabolized in the liver. The elimination half-life is relatively short. Detailed PK parameters such as Cmax, Tmax, AUC, and half-life have been reported in the literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of Gambogenic acid has been evaluated in preclinical studies. The compound has been shown to have a relatively low toxicity in animal models at therapeutic doses. However, higher doses can cause adverse effects, including hepatotoxicity and nephrotoxicity. The compound is for research use only and is not approved for human therapeutic use.
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| References | |
| Additional Infomation |
It has been reported that plants in the genus Garcinia hanburyi contain gambogia acid, and relevant data are available for reference.
Gambogenic acid is a natural product with anticancer, anti-inflammatory, and antiviral properties. It is a research compound that has been studied for its potential therapeutic applications in cancer and other diseases. Gambogenic acid is not an FDA-approved drug and is not commercially available as a pharmaceutical product. The compound continues to be an active area of research. |
| Molecular Formula |
C38H46O8
|
|---|---|
| Molecular Weight |
630.7671
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| Exact Mass |
630.319
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| Elemental Analysis |
C, 72.36; H, 7.35; O, 20.29
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| CAS # |
173932-75-7
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| Related CAS # |
173932-75-7
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| PubChem CID |
10794070
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
818.6±65.0 °C at 760 mmHg
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| Flash Point |
253.0±27.8 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
9.42
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
46
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| Complexity |
1440
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1C(C([H])([H])[H])(C([H])([H])[H])C2([H])C([H])([H])[C@@]3([H])C([H])=C4C(C5=C(C(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])=C(C(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])=C5O[C@@]24C1(C([H])([H])/C(/[H])=C(\C(=O)O[H])/C([H])([H])[H])C3=O)O[H])O[H])=O
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| InChi Key |
RCWNBHCZYXWDOV-VSFMGBBVSA-N
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| InChi Code |
InChI=1S/C38H46O8/c1-20(2)10-9-11-22(5)13-15-25-30(39)26(14-12-21(3)4)33-29(31(25)40)32(41)27-18-24-19-28-36(7,8)46-37(34(24)42,38(27,28)45-33)17-16-23(6)35(43)44/h10,12-13,16,18,24,28,39-40H,9,11,14-15,17,19H2,1-8H3,(H,43,44)/b22-13+,23-16-/t24-,28+,37+,38-/m1/s1
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| Chemical Name |
(Z)-4-[(1S,2S,13S,15R)-7-[(2E)-3,7-dimethylocta-2,6-dienyl]-6,8-dihydroxy-17,17-dimethyl-5-(3-methylbut-2-enyl)-10,14-dioxo-3,16-dioxapentacyclo[11.4.1.02,11.02,15.04,9]octadeca-4,6,8,11-tetraen-15-yl]-2-methylbut-2-enoic acid
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| Synonyms |
GNA; Gambogenic Acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~158.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5854 mL | 7.9268 mL | 15.8536 mL | |
| 5 mM | 0.3171 mL | 1.5854 mL | 3.1707 mL | |
| 10 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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