Evofosfamide
Chemical Name: (1-Methyl-2-nitro-1H-imidazol-5-yl)methyl N,N'-bis(2-bromoethyl)phosphorodiamidate
Purity: ≥98%
Biological Activity
Evofosfamide is a hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM). Evofosfamide is stable under normoxic conditions but is activated by cellular reductases in hypoxic conditions (IC50 values are 5.1 μM and 0.019 μM, in NSCLC cells under normoxic and hypoxic conditions, respectively). Br-IPM acts as a DNA alkylating agent, inducing intrastrand and interstrand crosslinks. Evofosfamide inhibits NEPC PDX tumor growth by 84.5% in adeno-CRPC and NEPC patient-derived xenograft models. When combined with gemcitabine (Cat. No. 3259), Evofosfamide inhibits primary tumor growth by 96% and significantly extends the survival time in the MIA PaCa-2 human pancreatic cancer orthotopic xenograft model.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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ONECUT2 is a driver of neuroendocrine prostate cancer.
Guo H, Ci X, Ahmed M et al.
Nat Commun
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