Efrapeptin F
Efrapeptin F is a mitochondrial complex V inhibitor and cytotoxic agent with in vivo antitumor activity. Efrapeptin F induces cell death in glucose-limiting conditions, with preferential cytotoxicity to nutrient-deprived cancer cells under hypoxic conditions. Efrapeptin F can be used for the research of pancreatic cancer, prostate cancer, breast cancer, central nervous system cancer, colon cancer, lung cancer, melanoma, ovarian cancer, kidney cancer, stomach cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 131353-66-7
- Fòrmula: C82H141N18O16+
- Peso molecular:1635.11
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
25 μM
Compound: 53
|
Cytotoxicity against human HepG2 cells assessed as decrease in cell viability measured after 48 hrs by MTS assay
Cytotoxicity against human HepG2 cells assessed as decrease in cell viability measured after 48 hrs by MTS assay
|
[PMID: 33565879] |
| PANC-1 | IC50 |
52 nM
Compound: Efrapeptin F
|
Anticancer activity against human PANC-1 cells assessed as reduction in cell viability by measuring ATP level incubated for 24 hrs by CellTiter-Glo assay
Anticancer activity against human PANC-1 cells assessed as reduction in cell viability by measuring ATP level incubated for 24 hrs by CellTiter-Glo assay
|
[PMID: 32942072] |
In Vitro
Efrapeptin F (0.001-10 μmol/L; 24 h) potently inhibits the survival of glucose-deprived human pancreatic cancer PANC-1 cells with an IC50 of 0.052 μmol/L, which is over 100 times more potent than its effect on PANC-1 cells in nutrient-sufficient medium[1].
Efrapeptin F (0.001-10 μmol/L; 24 h) exhibits preferential cytotoxicity to human pancreatic cancer PANC-1 cells under glucose-limiting conditions (≤100 mg/L glucose), regardless of amino acid or serum availability[1].
Efrapeptin F (0.001-10 μmol/L; 24 h under 1% O2) exhibits preferential cytotoxicity to glucose-deprived human pancreatic cancer PANC-1 cells under hypoxic (1% O2) conditions, similar to its effect under normoxic conditions[1].
Efrapeptin F (0.06 μmol/L; 24 h) causes a 100-fold reduction in cellular ATP levels in glucose-deprived human pancreatic cancer PANC-1 cells, but only a minor reduction in nutrient-sufficient PANC-1 cells[1].
Efrapeptin F potently inhibits the growth of diverse human cancer cell lines in the JFCR39 panel, with a mean GI50 of 135 nmol/L, and shows high potency (GI50 = 1 nmol/L) against multiple breast, central nervous system, lung, ovarian, stomach, and prostate cancer cell lines[1].
Efrapeptin F (0.1 μmol/L; 24 h) induces significant early and late apoptosis in glucose-deprived human pancreatic cancer PANC-1 cells, but not in nutrient-sufficient PANC-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human pancreatic cancer PANC-1 cells
-
Concentration:0.001, 0.01, 0.1, 1, 10 μmol/L
-
Incubation Time:24 h
-
Result:Exhibited preferential cytotoxicity to PANC-1 cells in nutrient-deprived medium (NDM (-)) with an IC50 of 0.052 μmol/L.
Showed an IC50 of >10 μmol/L in nutrient-sufficient DMEM (10% FBS), making the cytotoxic effect over 100 times stronger under glucose-deprived conditions.
-
Cell Line:human pancreatic cancer PANC-1 cells
-
Concentration:0.1 μmol/L
-
Incubation Time:24 h
-
Result:Resulted in 99% viable cells, 0% early apoptotic cells, 1% late apoptotic cells, and 0% necrotic cells in nutrient-sufficient DMEM (10% FBS).
Induced 22% viable cells, 43% early apoptotic cells, 31% late apoptotic cells, and 4% necrotic cells in glucose-deprived NDM (-), representing a significant increase in apoptotic cell death.
-
Cell Line:human pancreatic cancer PANC-1 cells
-
Concentration:0.001, 0.01, 0.1, 1, 10 μmol/L
-
Incubation Time:24 h
-
Result:Induced preferential cell death in PANC-1 cells only under glucose-deprived conditions, regardless of the presence or absence of amino acids and serum.
Showed no cytotoxicity in media with 1000 or 500 mg/L glucose, but exhibited cytotoxicity in media with glucose concentrations ≤100 mg/L.
-
Cell Line:human pancreatic cancer PANC-1 cells
-
Concentration:0.001, 0.01, 0.1, 1, 10 μmol/L
-
Incubation Time:24 h (under 1% O2 hypoxic conditions)
-
Result:Showed preferential cytotoxicity to PANC-1 cells in glucose-deprived NDM (-) under hypoxic conditions, with a sharp reduction in cell survival at concentrations ≥0.1 μmol/L.
Maintained high cell survival in nutrient-sufficient DMEM (10% FBS) under the same hypoxic conditions.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:SCID (male, 6 weeks old, human prostate cancer PC-3 cells subcutaneously injected)[1]
-
Dosage:0.125 mg/kg; 0.0625 mg/kg
-
Administration:i.v.; twice weekly; 3 weeks
-
Result:Reduced mean tumor weight by 31% relative to control (0.63 g vs control 0.92 g) at 0.125 mg/kg.
Reduced mean tumor weight by 14% relative to control (0.79 g vs control 0.92 g) at 0.0625 mg/kg.
Did not reduce body weight of treated mice at tested doses.
Resulted in one death at day 23 in the 0.125 mg/kg group, with remaining 6 mice surviving until study end without anatomical toxic effects in critical organs.
Chemical Information
-
No. CAS 131353-66-7
-
Peso molecular 1635.11
-
Fòrmula C82H141N18O16+
-
SMILES
O=C([C@H]1N(CCCC1)C(C(C)(C)NC(C(C)(C)NC(CNC(CCNC([C@H](CC(C)C)NC(C(C)(C)NC(C(C)(C)NC([C@H]2N(CCCC2)C(C(C)(C)NC([C@H]3N(CCCC3)C(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC(C)(C)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@](CC)(C)C(N[C@@H](CC(C)C)C[N+]4=C5N(CCC4)CCC5)=O)=O)=O)=O
-
Structure Classification
-
Initial Source
Tolypocladium geodes
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Efrapeptin F Related Classifications
HY-N19739 Related Classifications
Powered by Bioz