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Submit ReviewNeratinib is a potent, irreversible inhibitor of HER-2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50 = 59 nM and 92 nM, respectively). Neratinib reduces receptor autophosphorylation and proliferation of EGFR-dependent cancer cells, blocks cell-cycle progression and inhibits HER-2 signaling pathways. Neratinib suppresses proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR. Also inhibits MST1 (IC50 = 37.7 nM). Orally bioavailable.
分子量 | 557.05 |
公式 | C30H29ClN6O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 698387-09-6 |
PubChem ID | 9915743 |
InChI Key | JWNPDZNEKVCWMY-VQHVLOKHSA-N |
Smiles | N(C=1C2=C(C=C(OCC)C(NC(/C=C/CN(C)C)=O)=C2)N=CC1C#N)C3=CC(Cl)=C(OCC4=CC=CC=N4)C=C3 |
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 | 2.79 | 5 |
以下数据基于产品分子量 557.05。 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 |
---|---|---|---|
0.05 mM | 35.9 mL | 179.52 mL | 359.03 mL |
0.25 mM | 7.18 mL | 35.9 mL | 71.81 mL |
0.5 mM | 3.59 mL | 17.95 mL | 35.9 mL |
2.5 mM | 0.72 mL | 3.59 mL | 7.18 mL |
参考文献是支持产品生物活性的出版物。
Rabindran et al (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 64 3958 PMID: 15173008
Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc.Natl.Acad.Sci.U.S.A. 102 7665 PMID: 15897464
Yun et al (2008) The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc.Natl.Acad.Sci.U.S.A. 105 2070 PMID: 18227510
If you know of a relevant reference for Neratinib, please let us know.
关键词: Neratinib, Neratinib supplier, potent, irreversible, HER2, ERBB2, tyrosine, kinase, inhibitors, inhibitory, inhibition, EGFR, epidermal, growth, factor, receptor, MST1, Other, Kinases, 7371, Tocris Bioscience
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