Evofosfamide

Product Description

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.

Solubility

Preparing Stock Solutions for Evofosfamide

The following data is based on the product molecular weight 449.04

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.23 mL	11.13 mL	22.27 mL
5 mM	0.45 mL	2.23 mL	4.45 mL
10 mM	0.22 mL	1.11 mL	2.23 mL
50 mM	0.04 mL	0.22 mL	0.45 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Guo ONECUT2 is a driver of neuroendocrine prostate cancer. Nat.Commun. 2019 PMID: 30655535
• Duan Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs. J.Med.Chem. 2008 PMID: 18257544