Erlotinib 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.
盐酸厄洛替尼(Erlotinib hydrochloride)(商品名特罗凯?)是表皮生长因子受体(EGFR / HER-1)酪氨酸激酶的直接抑制剂,IC50值为2 nM。
表皮生长因子受体(EGFR)是ErbB家族的成员。ErbB家族包括EGFR(ErbB1)、ErbB2、ErbB3和ErbB4。EGFR的激活依赖于多肽生长因子与受体的结合。在许多癌症中,EGFR突变的存在导致EGFR的激活,从而引起细胞增殖和其它癌症过程[1]。
Erlotinib hydrochloride对EGFR酪氨酸激酶的选择性抑制导致癌症生长和发育的破坏,包括细胞迁移、增殖、血管生成和细胞凋亡。例如,erlotinib hydrochloride诱导肝癌细胞Bxpc-3 和PANC-1中细胞凋亡和G0/G1期细胞周期停滞,从而增强其对细胞抑制剂的敏感性[2,3]。
此外,该产品被广泛研究用于人非小细胞肺癌(NSCLC)的治疗[4]。据报道,在胰腺癌中,erlotinib hydrochloride也具有抗肿瘤效应[5]。
参考文献:
1. Melosky B. Review of EGFR TKIs in Metastatic NSCLC, Including Ongoing Trials. Front Oncol 2014,4:244.
2. Zheng YT, Yang HY, Li T, Zhao B, Shao TF, Xiang XQ, et al. Amiloride sensitizes human pancreatic cancer cells to erlotinib in vitro through inhibition of the PI3K/AKT signaling pathway. Acta Pharmacol Sin 2015,36:614-626.
3. Huether A, Hopfner M, Sutter AP, Schuppan D, Scherubl H. Erlotinib induces cell cycle arrest and apoptosis in hepatocellular cancer cells and enhances chemosensitivity towards cytostatics. J Hepatol 2005,43:661-669.
4. Singh N, Jindal A, Behera D. Erlotinib usage after prior treatment with gefitinib in advanced non-small cell lung cancer: A clinical perspective and review of published literature. World J Clin Oncol 2014,5:858-864.
5. Renouf DJ, Tang PA, Hedley D, Chen E, Kamel-Reid S, Tsao MS, et al. A phase II study of erlotinib in gemcitabine refractory advanced pancreatic cancer. Eur J Cancer 2014,50:1909-1915.
- 1. Shuchen Chen, Honglin Zhu, et al. "Molecular and clinical characteristics of IDH mutations in Chinese NSCLC patients and potential treatment strategies." Cancer Med. 2022 May 8. PMID: 35526267
- 2. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID: 31862381
- 3. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID: 31063758
- 4. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID: 30038713
- 5. Deng W, Gu L, et al. "CD24 associates with EGFR and supports EGF/EGFR signaling via RhoA in gastric cancer cells." J Transl Med. 2016 Feb 1;14:32. PMID: 26830684
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 429.91 |
Cas No. | 183319-69-9 |
Formula | C22H24ClN3O4 |
Synonyms | Tarceva; CP-358774; OSI-774; NSC 718781 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥6.44 mg/mL in DMSO with gentle warming |
Chemical Name | N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine;hydrochloride |
SDF | Download SDF |
Canonical SMILES | COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl |
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。 |
细胞实验: [1] | |
细胞系 |
Calu1细胞 |
制备方法 |
该化合物在DMSO中的溶解度小于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
1 ?M,24 hours |
实验结果 |
Erlotinib(1 ?M,24 小时)、docetaxel?(50 nM,18小时)或erlotinib和docetaxel?共同使用处理细胞。Txt-> OSI-774->培养基序列处理的细胞死亡程度最大,而用OSI-774>Txt->培养基序列处理的细胞在处理后72小时恢复增殖。两种药物同时处理,Txt-> OSI-774的序列中检测到切割PARP和Caspase-3,但在OSI-774->Txt的序列中没有检测到。此外,切割PARP和Caspase-3持续至Txt-> OSI-774处理后的72小时。这些数据与亚G1细胞的结果一致,从分子水平上表现出凋亡效应。 |
动物实验: [2] | |
动物模型 |
注射H460a细胞的雌性无胸腺nu/nu-nuBR裸鼠 |
给药剂量 |
口服,100mg/kg,每天,持续三周 |
实验结果 |
Erlotinib具有显著的剂量依赖性功效。在100 mg/kg组中抑制61%的细胞生长。其他组具有以下生长抑制:25 mg/kg:46%;12.5 mg/kg:36%;6.25 mg/kg:28%。没有产生部分或完全消退。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1] Kimura T, Mahaffey C M, Pryde B J, et al. Apoptotic effects of the docetaxel→ OSI-774 combination in non-small cell lung carcinoma (NSCLC) cells//Proc Am Soc Clin Oncol. 2004, 22: 7143. [2] Higgins B, Kolinsky K, Smith M, et al. Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models. Anti-cancer drugs, 2004, 15(5): 503-512. |
描述 | Erlotinib HCl (OSI-744)是EGFR的抑制剂,IC50值为2 nM,对EGFR的敏感性比对人c-Src或v-Abl高1000倍以上。 | |||||
靶点 | HER1/EGFR | |||||
IC50 | 2 nM |
质量控制和MSDS
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