| Bioactivity | 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[1]. |
| Target | IC50: 30 nM (HIF-1α) in A2780 |
| Invitro | 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]. Apoptosis Analysis Cell Line: |
| In Vivo | 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]. Animal Model: |
| Name | GEM-5 |
| CAS | 2233543-49-0 |
| Formula | C32H29F2N5O8 |
| Molar Mass | 649.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214. |