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Submit ReviewWZ 4002 is a potent irreversible mutant selective EGFR tyrosine kinase inhibitor. It blocks ATP-dependent autophosphorylation of EGFR carrying the T790M or L858R mutation (IC50 = 8 nM). WZ 4002 exhibits selectivity for mutant EGFR over wild-type. In mice bearing T790M mutant lung cancer cell lines WZ 4002 inhibits EGFR, AKT and ERK1/2 phosphorylation and results in significant tumor regression.
Sold under license from Dana-Farber Cancer Institute.
分子量 | 494.98 |
公式 | C25H27ClN6O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1213269-23-8 |
PubChem ID | 44607530 |
InChI Key | ITTRLTNMFYIYPA-UHFFFAOYSA-N |
Smiles | COC1=C(NC2=NC=C(Cl)C(OC3=CC(NC(C=C)=O)=CC=C3)=N2)C=CC(N4CCN(C)CC4)=C1 |
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 | |||
DMSO | 4.95 | 10 |
以下数据基于产品分子量 494.98。 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 |
---|---|---|---|
0.1 mM | 20.2 mL | 101.01 mL | 202.03 mL |
0.5 mM | 4.04 mL | 20.2 mL | 40.41 mL |
1 mM | 2.02 mL | 10.1 mL | 20.2 mL |
5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
参考文献是支持产品生物活性的出版物。
Zhou et al (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462 1070 PMID: 20033049
If you know of a relevant reference for WZ 4002, please let us know.
关键词: WZ 4002, WZ 4002 supplier, WZ4002, potent, EGFR, epidermal, growth, factor, receptor, tyrosine, kinase, inhibitors, inhibits, mutant-selective, T790M, L858R, 6290, Tocris Bioscience
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