CL-387785 (EKI-785)
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.
IC50:370 pM
EGFR(170 kDa)包括胞外配体结合域\单个跨膜结构域以及胞内酪氨酸激酶结构域.在肺\脑\膀胱\前列腺\头颈等多种肿瘤中,EGFR被高度激活.以往实验表明,4-苯胺喹唑啉与ATP竞争并结合到EGFR,从而抑制EGF诱导的EGFR酪氨酸残基自磷酸化,并抑制EGF介导的生长.CL-387785是EGFR的不可逆抑制剂.
体外:CL-387785共价结合到EGFR.此外,CL-387785也特异性抑制EGFR激酶活性,阻断EGF诱导的细胞内受体自磷酸化,在过表达EGFR或c-erbB-2的细胞系中,CL-387785主要以抑制细胞生长的方式抑制细胞增殖[1].
体内:在裸鼠侧腹中,皮下植入人肿瘤异种移植物,以评价CL-387785对肿瘤生长的作用.腹腔注射或口服给予CL-387785可以抑制A431细胞源肿瘤生长.在治疗起始7天内,观察到CL-387785的抑制作用.CL-387785对未过表达EGFR细胞系来源的肿瘤无效,包括人乳腺癌MDA-MB-435[1].
临床试验:到目前为止,CL-387785仍处于临床前开发阶段.
参考文献：
[1] Discafani CM, Carroll ML, Floyd MB Jr, Hollander IJ, Husain Z, Johnson BD, Kitchen D, May MK, Malo MS, Minnick AA Jr, Nilakantan R, Shen R, Wang YF, Wissner A, Greenberger LM. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785). Biochem Pharmacol. 1999 Apr 15;57(8):917-25.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 381.23 |
| Cas No. | 194423-06-8 |
| Formula | C18H13BrN4O |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥16.85 mg/mL in DMSO |
| Chemical Name | N-(4-((3-bromophenyl)amino)quinazolin-6-yl)but-2-ynamide |
| SDF | Download SDF |
| Canonical SMILES | CC#CC(NC1=CC(C(NC2=CC=CC(Br)=C2)=NC=N3)=C3C=C1)=O |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
