Icotinib Hydrochloride
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.
Icotinib Hydrochloride是上皮生长因子受体酪氨酸激酶(EGFR-TKI)的高效高选择性抑制剂,其IC50值为5 nM。
EGFR是一种癌症驱动蛋白,在正常细胞和癌细胞的表面表达[1],体细胞突变特别是外显子19缺失或外显子21 L858R突变的病人的酪氨酸激酶域存在激活突变,导致不受控制的细胞增殖[2]。在多种类型的癌症中发现,EGFR过表达引起抗凋亡Ras信号通路不正常活化[3]。
Icotinib是喹唑啉衍生物,可逆的结合到EGFR蛋白的ATP结合位点,阻止信号转导级联反应[4]。Icotinib抑制胞内上皮生长因子受体(EGFR)相关酪氨酸激酶(TK)的磷酸化[5]。
Icotinib用于EGFR突变阳性、晚期或转移性非小细胞肺癌(NSCLC)病人的二线或三线治疗,这些病人经历过至少一次施用含铂药物化疗失败[6]。
参考文献:
1. A Douglas Laird,and Julie M Cherrington. Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. 2003, 12(1): 51-64.
2. Raymond E, Faivre S, Armand JP: Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs. 2000;60 Suppl 1:15-23.
3. Sordella,R. "Gefitinib-Sensitizing EGFR Mutations in Lung Cancer Activate Anti-Apoptotic Pathways". Science ,2004, 305 (5687): 1163-1167.
4. Bulgaru AM. et al. Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase. Expert Rev Anticancer Ther. 2003 Jun;3(3):269-79.
5. Dudek AZ.et al. Skin rash and bronchoalveolar histology correlates with clinical benefit in patients treated with gefitinib as a therapy for previously treated advanced or metastatic non-small cell lung cancer. Lung Cancer. 2006, 51(1):89-96.
6. C Delbaldo, S Faivre, E Raymond. Les inhibiteurs des récepteurs de l’Epidermal Growth Factor (EGF) Epidermal growth factor inhibitors. La Revue de Médecine Interne. 2003,24(6): 372–383.
Storage | Store at -20°C |
M.Wt | 427.88 |
Cas No. | 1204313-51-8 |
Formula | C22H22ClN3O4 |
Synonyms | BPI-2009H |
Solubility | Soluble in DMSO |
Chemical Name | N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride |
SDF | Download SDF |
Canonical SMILES | Cl[H].[H]C1=C2C(N=C([H])N=C2N([H])C3=C([H])C([H])=C([H])C(C#C[H])=C3[H])=C([H])C4=C1OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])O4 |
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。 |
Description | Icotinib Hydrochloride是上皮生长因子受体(EGFR)酪氨酸激酶的高效特异性抑制剂,其IC50值为5 nM。 | |||||
靶点 | EGFR | |||||
IC50 | 5 nM |