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Submit ReviewEvofosfamide 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.
分子量 | 449.04 |
公式 | C9H16Br2N5O4P |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 2.25 | 5 | |
DMSO | 44.9 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
Duan et al (2008) Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs. J.Med.Chem. 51 2412 PMID: 18257544
Guo et al (2019) ONECUT2 is a driver of neuroendocrine prostate cancer. Nat.Commun. 10 278 PMID: 30655535
If you know of a relevant reference for Evofosfamide, please let us know.
关键词: Evofosfamide, Evofosfamide supplier, hypoxia, activated, prodrug, DNA, crosslink, antitumor, alkylating, agent, phosphoramide, mustard, Cell, Cycle, Inhibitors, Apoptosis, Inducers, 7507, Tocris Bioscience
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.