GEM-5
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
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- No. CAS: 2233543-49-0
- Fòrmula: C32H29F2N5O8
- Peso molecular:649.60
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
IC50: 30 nM (HIF-1α) in A2780[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.03 μM
Compound: GEM-5
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Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
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[PMID: 33992863] |
| A2780 | IC50 |
0.13 μM
Compound: GEM-5
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Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33992863] |
| A549 | IC50 |
0.37 μM
Compound: GEM-5
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33992863] |
| A549 | IC50 |
3.03 μM
Compound: GEM-5
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
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[PMID: 33992863] |
| L02 | IC50 |
3.04 μM
Compound: GEM-5
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
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[PMID: 33992863] |
| L02 | IC50 |
4.43 μM
Compound: GEM-5
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33992863] |
| MCF7 | IC50 |
2.6 μM
Compound: GEM-5
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33992863] |
GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780 cells[1]
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Concentration:0.5 μM
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Incubation Time:72 hours
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Result:Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.
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Cell Line:A2780 cells[1]
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Concentration:0.5 μM
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Incubation Time:24 hours
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Result:Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).
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Cell Line:A2780 cells[1]
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Concentration:0.1 and 1 μM
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Incubation Time:24 hours
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Result:Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
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Dosage:125 or 271 mg/kg
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Administration:Tail vein injection, once a week for 4 weeks
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Result:Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.
Chemical Information
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No. CAS 2233543-49-0
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Peso molecular 649.60
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Fòrmula C32H29F2N5O8
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SMILES
NC(C=CN1[C@@H]2O[C@@H]([C@H](C2(F)F)O)COC(CCC(OCC3=CC=C(O3)C4=NN(C5=C4C=CC=C5)CC6=CC=CC=C6)=O)=O)=NC1=O
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Envío
Room temperature in continental US; may vary elsewhere.
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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)
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