EGFR/ErbB2 Inhibitor
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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).
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 |
SDF | Download SDF |
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 | 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。 |