Glufosfamide

Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma^[1][2][3]. In Vitro:Glufosfamide (10-1000 μM, 24-72 h) exhibits cytotoxicity in a concentration- and time-dependent manner in HepG2 cells, with lower IC₅₀ values (24 h: 112.32 μM; 48 h: 83.23 μM; 72 h: 51.66 μM)^[1].
Glufosfamide (10-50 μM, 48-72 h) induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in HepG2, LNCaP and PC-3 cells^[1][3].
Glufosfamide (10-50 μM, 48-72 h) downregulates Bcl2 gene expression and reduces mitochondrial membrane potential and cellular ATP levels in HepG2 cells^[1].
Glufosfamide (10 mg/mL, 24 h) combined with Gemcitabine (HY-17026) (1 mg/mL) shows a more significant inhibitory effect on the growth of MiaPaCa-2, H766t, and PANC-1 pancreatic cancer cells in proliferation assays compared to single-agent treatmentand induces slightly more than additive apoptosis (sub-G1 phase)^[2].
Glufosfamide (0.1-300 μM, 72 h) exhibits concentration-dependent cytotoxicity in LNCaP and PC-3 prostate cancer cells, with IC₅₀ values of 86.8 μM and 70 μM, respectively^[3].
Glufosfamide (0.1-300 μM, 72 h) combined with Docetaxel (HY-B0011) down-regulates Bcl-2 expression and up-regulates Bax, caspase-3, and caspase-9 expression in LNCaP and PC-3 prostate cancer cells^[3].
In Vivo:Glufosfamide (3-100 mg/kg, i.v., daily, 14 days) shows dose-dependent tumor growth inhibition in MiaPaCa-2-RFP orthotopic nude mouse model^[2].
Glufosfamide (10-30 mg/kg, i.v., daily, 14 days) significantly reduces tumor volume when combined with Gemcitabine in MiaPaCa-2-RFP orthotopic nude mouse model^[2].