Evofosfamide

Pricing Availability   Qty
说明: Hypoxia-activated DNA alkylating agent prodrug
化学名: (1-Methyl-2-nitro-1H-imidazol-5-yl)methyl N,N'-bis(2-bromoethyl)phosphorodiamidate
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (1)
通路 (1)

生物活性 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.

技术数据 for Evofosfamide

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.

溶解性数据 for Evofosfamide

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 2.25 5
DMSO 44.9 100

制备储备液 for Evofosfamide

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for Evofosfamide

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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Programmed Cell Death Poster

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Pathways for Evofosfamide

Apoptosis Signaling Pathway

Apoptosis Signaling Pathway

Apoptosis is a physiological process for cell death that is critical during aging and development. It may also be referred to as cell 'suicide'. Apoptosis can be triggered by events both inside and outside of the cell.