Evofosfamide

Name: Evofosfamide
Brand: Tocris Bioscience
SKU: 7507

Tocris Bioscience, part of Bio-Techne | Catalog # 7507

Citations (1)

COA / SDS

Hypoxia-activated DNA alkylating agent prodrug

Key Product Details

Description:	Hypoxia-activated DNA alkylating agent prodrug
Chemical Name:	(1-Methyl-2-nitro-1H-imidazol-5-yl)methyl N,N'-bis(2-bromoethyl)phosphorodiamidate
Purity:	≥98% (HPLC)
Molecular Weight:	449.04

View Full Technical Details for Evofosfamide

Technical Data
Citations

Biological Activity for Evofosfamide

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 for Evofosfamide

M. Wt	449.04
Formula	C₉H₁₆Br₂N₅O₄P
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	918633-87-1
PubChem ID	11984561
InChi Key	UGJWRPJDTDGERK-UHFFFAOYSA-N
Smiles	CN1C(COP(NCCBr)(NCCBr)=O)=CN=C1[N+]([O-])=O

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.

Solubility for Evofosfamide

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	2.25	5
	DMSO	44.9	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for Evofosfamide

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