依伏磷酰胺 | 艾伏磷酰胺
Evofosfamide (Synonyms: TH-302)
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基本信息
中文名称依伏磷酰胺 | 艾伏磷酰胺
英文名称 Evofosfamide (Synonyms: TH-302)
CAS号918633-87-1
分子式C9H16Br2N5O4P
分子量449.04
外观White to yellow powder
储存条件Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years).
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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.
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