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Erlotinib

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Chemical Structure| 183321-74-6 同义名 : CP-358774;NSC 718781;OSI-774
CAS号 : 183321-74-6
货号 : A121900
分子式 : C22H23N3O4
纯度 : 95%
分子量 : 393.44
MDL号 : MFCD08063588
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(7.63 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+30% PEG 300+5% Tween 80+water 3 mg/mL

生物活性
靶点

  • EGFR/ErbB1

    HER1/EGFR, IC50:2 nM

  • EGFR/ErbB1

    EGFR, IC50:2 nM
描述 EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1 - 4) with an external domain that binds activating ligands, such as EGF, and is overexpressed in a significant percentage of carcinomas and contributes to the malignant phenotype. Upon activation, EGFR phosphorylates both the receptor itself and a variety of “effector” protein. Erlotinib is a direct inhibitor of EGFR kinase with IC50 value of 2 nM (measured by purified EGFR kinase activity). Potent inhibition of EGF-induced EGFR autophosphorylation by Erlotinib can be seen in different cell lines, such as HNS human head and neck tumor cells, DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib is selective for the EGFR kinase pathway that inhibits EGF-stimulated mitogenesis with an IC50 of 70 nM but inhibits mitogenesis stimulated by the other factors at concentrations of >1 μM. Erlotinib induced both anti-proliferation and apoptosis in DiFi human colon tumor cells. Consistent with in vitro studies, treatment with Erlotinib at dose of 100 mg/kg prevents EGF-induced autophosphorylation of the EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR in the treated mice[1].
作用机制 Erlotinib is an ATP-competitive inhibitor of EGFR[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A431 cells Function assay Inhibition of EGFR in human A431 cells by HTRF assay, IC50=0.42 μM. 19815412
human SKBR3 cells Function assay Inhibition of HER2 in human SKBR3 cells by HTRF assay, IC50=1.89 μM. 19815412
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.71mL

2.54mL

1.27mL

25.42mL

5.08mL

2.54mL
参考文献

[1]Moyer JD, Barbacci EG, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997 Nov 1;57(21):4838-48.

[2]Marchetti S, de Vries NA, et al. Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice. Mol Cancer Ther. 2008 Aug;7(8):2280-7.

[3]Abraham J, Nelon LD, et al. Preclinical testing of erlotinib in a transgenic alveolar rhabdomyosarcoma mouse model. Sarcoma. 2011;2011:130484.

[4]Pharmacokinetics of erlotinib