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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- CAS 番号: 2233543-49-0
- 分子式: C32H29F2N5O8
- 分子量:649.60
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保管条件:
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]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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
|
[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.
化学情報
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CAS 番号 2233543-49-0
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分子量 649.60
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GEM-5 関連分類
HY-146540 関連分類
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