Product Name | Evofosfamide (TH-302) |
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CAS | 918633-87-1 |
Formula | C9H16Br2N5O4P |
MW | 449.04 |
Appearance | White to yellow powder |
Storage condition | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
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Product Name | Evofosfamide (TH-302) |
---|---|
CAS | 918633-87-1 |
Formula | C9H16Br2N5O4P |
MW | 449.04 |
Appearance | White to yellow powder |
Storage condition | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
Evofosfamide (TH-302) is potent and selective that has an IC50 of 19 nM. It exhibits 270-fold increased cytotoxicity under hypoxia compared to their potency under aerobic conditions and is stable to cytochrome P450 metabolism. Under hypoxia, TH-302 is selectively potent and liver microsomes tolerate it well. With a high hypoxic selectivity [Hypoxia cytotoxicity ratio (HCR) = 270], replacing the chlorine with bromine in the phosphorus mustard in 3b results in a 10-fold increase in potency. Under N2, TH-302 exhibits strong cytotoxicity against human lung cancer H460 cells and human colon cancer HT29 cells. With an IC90 of 0.1 μM and 0.2 μM, respectively, TH-302 inhibits HT29 cells and H460 cells.