l General Information |
Product Name | Evofosfamide (TH-302) |
General description | TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism. |
Synonym | Evofosfamide; 2-bromo-N-[(2-bromoethylamino)-[(3-methyl-2-nitroimidazol-4-yl)methoxy]phosphoryl]ethanamine |
Purity | ≥98.0%(HPLC) | CAS Number | 918633-87-1 |
Formula | C9H16Br2N5O4P | Molecular Weight | 449.04 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | Solid |
Solubility(25°C) | DMSO | ≥50mg/mL |
Ethanol | ≥50mg/mL |
Water | ≥5mg/mL |
l Biological Information |
Biochem/Physiol
Actions | Evofosfamide is a hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM) conjugated with 2-nitroimidazole, with potential antineoplastic activity. When exposed to hypoxic conditions, such as those found in hypoxic tumors, the 2-nitroimidazole moiety of evofosfamide is reduced. This releases the DNA-alkylating Br-IPM moiety, which introduces intra- and inter-strand DNA crosss in nearby cells; the crosss inhibit both DNA replication and cell division, and may lead to apoptosis of cells in the tumor. The inactive form of the prodrug is stable under normoxic conditions, which may limit systemic toxicity. |
l Storage |
Storage temp. | -20°C |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
