Neratinib

Pricing Availability   Qty
说明: Potent HER2 receptor tyrosine kinase and EGFR kinase inhibitor
化学名: (2E)-N-[4-[[3-Chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (1)

生物活性 for Neratinib

Neratinib 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.

技术数据 for Neratinib

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.

溶解性数据 for Neratinib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 2.79 5

制备储备液 for Neratinib

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.

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
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

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参考文献 for Neratinib

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


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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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