EGFR/ErbB2 Inhibitor

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CAS NO:

179248-61-4

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	387.4
Cas No.	179248-61-4
Formula	C₂₃H₂₁N₃O₃
Solubility	≤1mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name	6,7-dimethoxy-N-[4-(phenylmethoxy)phenyl]-4-quinazolinamine
Canonical SMILES	COC1=C(OC)C=C(C(NC2=CC=C(OCC3=CC=CC=C3)C=C2)=NC=N4)C4=C1
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

IC50: 20 and 79 nM for EGFR and c-ErbB2, respectively

EGFR/ErbB2 Inhibitor is an EGFR and c-ErbB2 inhibitor.

EGFR and c-ErbB-2 are members of the epidermal growth factor receptor subfamily of protein tyrosine kinases. Their cellular overexpression causes transformation, so that the cells will grow in the absence of growth factors. An inhibitor of thse kinases should block the receptor signalling, subsequent transformation and inappropriate growth.

In vitro: EGFR/ErbB2 Inhibitor was identified as a potent inhibitor of both c-erbB-2 and EGFr [IC50: 0.079 μM for c-erbB-2, 0.020 μM for EGFr (isolated enzyme), 2.0 μM for HB4aC5.2 cells, 1.2 μM for BT474, both overexpressing c-erbB-2; 2.5 μM for HN5 cells overexpressing EGFr]. This combined potency was contrast to smaller, previously reported anilinoquinazolines and its subsequent analogues [1].

In vivo: GW974, a analog of EGFR/ErbB2 Inhibitor, was evaluated in the fast growing N87 gastric tumour xenograft in SCID mice. Results showed that GW974 at bid dose of 10 mg/kg po led to a 50% inhibition of tumour growth over the 20-day dosing period. Moreover, GW974 at 10 mg/kg po bid had complete inhibition of tumour growth over the 20-day dosing period in the BT474 breast tumour xenograft model. A longer-term study with initial dosing at 30 mg/kg po bid produced tumour shrinkage [1].

Clinical trial: Up to now, EGFR/ErbB2 Inhibitor is still in the preclinical development stage.

Reference:
[1] S. Cockerill, C. Stubberfield, J. Stables, et al. Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorganic & Medicinal Chemistry Letters 11, 1401-1405 (2001).