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^[1].

IC₅₀: 30 nM (HIF-1α) in A2780^[1]

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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

649.60

C₃₂H₂₉F₂N₅O₈

2233543-49-0

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]