Erlotinib
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.
Erlotinib(厄洛替尼,NSC 718781,CP 358,774)是一种有效的和可口服的表皮生长因子受体(EGFR)酪氨酸激酶抑制剂,选择性地和可逆地抑制细胞内EGFR相关酪氨酸激酶的自磷酸化。Erlotinib抑制纯化EGFR酪氨酸激酶和完整细胞内EGFR的自磷酸化,IC50值分别为2 nmol/L和20 nmol/L。Erlotinib竞争结合EGFR胞内结构域上的ATP结合位点,导致下游信号传导途径的抑制,这些途径参与血管生成、细胞增殖和细胞存活。Erlotinib浓度依赖性地抑制EGFR介导的信号传导,对表达EGFR的肿瘤具有突出的抗肿瘤活性,且具有可耐受的毒理学曲线。
参考文献:
Janine Smith. Erlotinib: small-molecule targeted therapy in the treatment of non-small-cell lung cancer. Clinical Therapeutics 2005; 27(10): 1513-1534
2. Shen M, Jiang YZ, et al. "Tinagl1 Suppresses Triple-Negative Breast Cancer Progression and Metastasis by Simultaneously Inhibiting Integrin/FAK and EGFR Signaling." Cancer Cell. 2019 Jan 14;35(1):64-80.e7. PMID:30612941
3. Zheng J, Duan B, et al."Folliculin Interacts with Rab35 to Regulate EGF-Induced EGFR Degradation." Front Pharmacol. 2017 Sep 26;8:688. PMID:29018350
4. Wang Y, Deng W, et al. "MICAL2 Promotes Breast Cancer Cell Migration by Maintaining EGFR Stability and EGFR/P38 Signaling Activation." Acta Physiol (Oxf). 2017 Jul 18. PMID:28719045
5. Lee HS, Park SB, et al. "A novel HDAC inhibitor, CG200745, inhibits pancreatic cancer cell growth and overcomes gemcitabine resistance." Sci Rep. 2017 Jan 30;7:41615. PMID:28134290
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 393.44 |
Cas No. | 183321-74-6 |
Formula | C22H23N3O4 |
Synonyms | NSC 718781;OSI-744;R-1415;OSI744;OSI 744;R1415;R 1415 |
Solubility | insoluble in H2O; ≥19.65 mg/mL in DMSO; ≥30.27 mg/mL in EtOH with gentle warming |
Chemical Name | N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine |
SDF | Download SDF |
Canonical SMILES | COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC |
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。 |
激酶实验[1]: | |
结合实验 |
激酶反应在50 μl的反应体系50 mM HEPES(pH 7.3)中进行,含有125 mM NaCl、24 mM MgCl2、0.1 mM原钒酸钠、20 μM ATP、1.6 μg/ml EGF和15 ng EGFR。加入溶于DMSO的化合物,DMSO的最终浓度为2.5%。加入ATP引发磷酸化,并在室温下持续振荡8分钟。通过抽吸反应混合物终止激酶反应,并用洗涤缓冲液洗涤4次。每孔用50μl HRP缀合的PY54抗磷酸酪氨酸抗体(使用封闭缓冲液稀释至0.2 μg/ml,封闭液是包含3%BSA和0.05%TWEEN 20的PBS)孵育25分钟,测定磷酸化POT,通过抽吸除去抗体,并用洗涤缓冲液洗涤板4次。加入TMB微孔过氧化物酶底物(每孔50μl)开发比色信号,每孔加入50 μl 0.09M硫酸终止反应。通过测量450nm的吸光度估计磷酸酪氨酸。 |
Cell experiment [1-3]: | |
细胞系 |
人非小细胞肺癌细胞系H322、A549、H1650和H1975 |
溶解方法 |
该化合物在DMSO中的溶解度大于19.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
2 μmol/L、24h |
应用 |
在H322细胞中,Erlotinib诱导大约80%的G1期停滞。Erlotinib(2 μM)显著抑制AsPC-1和BxPC-3胰腺细胞的生长。Erlotinib可有效抑制HNS人头颈部肿瘤细胞、DiFi人结肠癌细胞和MDA MB-468人乳腺癌细胞中的EGFR活化。Erlotinib(1 μM)诱导DiFi人结肠癌细胞凋亡。 |
动物实验 [4]: | |
动物模型 |
H460a和A549肿瘤模型 |
给药剂量 |
100 mg/kg |
应用 |
在H460a和A549肿瘤模型中,Erlotinib(100 mg/kg)在MTD处表现出抗肿瘤活性。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Moyer J D, Barbacci E G, Iwata K K, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase[J]. Cancer research, 1997, 57(21): 4838-4848. [2]. Li T, Ling Y H, Goldman I D, et al. Schedule-dependent cytotoxic synergism of pemetrexed and erlotinib in human non–small cell lung cancer cells[J]. Clinical Cancer Research, 2007, 13(11): 3413-3422. [3]. Ali S, Banerjee S, Ahmad A, et al. Apoptosis-inducing effect of erlotinib is potentiated by 3, 3′-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer[J]. Molecular cancer therapeutics, 2008, 7(6): 1708-1719. [4]. 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[J]. Anti-cancer drugs, 2004, 15(5): 503-512. |
质量控制和MSDS
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