Pabgraminone C
Pabgraminone C (IM502) is a Fungal metabolite and PI3Kγ inhibitor with an IC50 of 61.7 nM against PI3Kγ. Pabgraminone C shifts the STAT signaling pathway in cells from an immunosuppressive STAT3/STAT6-dominant profile to an immunostimulatory STAT1/STAT2-dominant profile, driving cells toward a pro-inflammatory phenotype. Pabgraminone C reprograms cells from an immunosuppressive state to an immunostimulatory state, reversing their suppressive effect on anti-tumor immunity. Pabgraminone C inhibits established tumor growth and metastasis across multiple cancer types. Pabgraminone C overcomes resistance to PD-1 checkpoint blockade strategies. Pabgraminone C can be used in research related to liver cancer, melanoma, and colorectal cancer.
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- CAS No.: 3061276-55-6
- Formule: C16H20O4
- Masse moléculaire:276.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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PI3Kγ 61.7 nM (IC50) |
PI3Kα 252.3 nM (IC50) |
PI3Kβ 532.5 nM (IC50) |
PI3Kδ 407.9 nM (IC50) |
STAT3 |
STAT6 |
STAT1 |
STAT2 |
Fungal Metabolite |
Pabgraminone C (0-1500 nM; 30 min) potently inhibits the activity of purified PI3Kγ enzyme, with an IC50 of 61.7 nM[1].
Pabgraminone C (10 μM; 24 h) reverses the immunosuppressive effect of monocyte-derived macrophages polarized by TCM, and promotes CD8+ T cell proliferation and cytokine production[1].
Pabgraminone C (10 μM; 6 h) alleviates oxidative stress in mouse TCM-polarized macrophages, reduces the levels of ROS and lipid peroxidation, and restores mitochondrial function and antioxidant levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human monocyte-derived macrophages and human CD8+ T cells
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Concentration:10 μM
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Incubation Time:24 h (macrophage pre-treatment)
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Result:Restored human CD8+ T cell proliferation and increased secretion of IFNγ and IL-2.
Pabgraminone C (6 mg/kg; intravenous injection; administered twice on day 0 and day 3 after tumor inoculation) inhibits experimental melanoma lung metastasis by more than 50% in immunocompetent mice[1].
Pabgraminone C (1.5 mg/kg; intravenous injection) enhances the antitumor efficacy of Sorafenib (HY-10201) in orthotopic liver tumors, and exhibits superior inhibitory effects on tumor growth and metastasis compared with either single-agent treatment[1].
Pabgraminone C (1.5 mg/kg; intravenous injection; administered once every 2 days for a total of 4 doses starting when the tumor volume reaches ~17 mm2) does not inhibit the growth of subcutaneous MC38 tumors in immunodeficient Rag2-/- mice, which confirms that its antitumor activity is immune-mediated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J WT (6-8 weeks old); Balb/C WT[1]
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Dosage:1.5 mg/kg
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Administration:i.v.; 4 doses every 2 days starting when tumors reached ~17 mm2
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Result:Significantly reduced mean tumor growth in Hepa1-6BL hepatocellular carcinoma, B16F10 melanoma, CT26 colorectal carcinoma, and MC38 colorectal carcinoma subcutaneous models compared to control.
Achieved comparable efficacy to first-line chemotherapy FOLFOX in MC38 tumor-bearing mice, reducing tumor weight significantly compared to control.
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Animal Model:C57BL/6J WT (6-8 weeks old)[1]
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Dosage:6 mg/kg
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Administration:i.v.; 2 doses on days 0 and 3 post-tumor inoculation
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Result:Reduced B16F10 lung metastasis by >50% compared to control.
Chemical Information
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CAS No. 3061276-55-6
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Masse moléculaire 276.33
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Formule C16H20O4
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SMILES
[H][C@@]12CC[C@@]([C@@]1([H])[C@@H](O)C3=C(C(C=CC3=O)=O)C2(C)C)(C)O
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Synonyms
IM502
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pabgraminone C Related Classifications
HY-184119 Related Classifications
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