Desmethyl Erlotinib (OSI-420 free base) 是 Erlotinib 的活性代谢物。厄洛替尼是一种有效的 EGFR 酪氨酸激酶抑制剂。
Cas No. | 183321-86-0 |
别名 | 2-[[4-[(3-乙炔基苯基)氨基]-7-(2-甲氧基乙氧基)-6-喹唑啉基]氧基]乙醇,OSI-420 free base; CP-373420 |
Canonical SMILES | C#CC1=CC(NC2=NC=NC3=CC(OCCOC)=C(OCCO)C=C32)=CC=C1 |
分子式 | C21H21N3O4 |
分子量 | 379.4 |
溶解度 | DMF: 50 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 25 mg/ml,Ethanol: 0.25 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Desmethyl erlotinib is a metabolite of erlotinib . Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM). This inhibits tumor growth in human head and neck carcinoma HN5 tumor xenografts in mice with an ED50 value of 9 mg/kg. Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 µM) and JAK2 mutant JAK2V617F positive hematopoietic progenitor cells (IC50 = 5 µM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia. Formulations containing erlotinib have been used to treat certain forms of cancer, including non-small cell lung cancer. |