| 货号 | 包装规格 | 操作 |
|---|---|---|
| SMB00950-5MG | 5 mg |
O-Desmethyl Gefitinib, a key metabolite of the anticancer drug gefitinib, belongs to the quinazoline family and is present in human plasma. Its formation is facilitated by the cytochrome P450 isoform CYP2D6. This compound exhibits significant activity as an inhibitor of tyrosine residue phosphorylation in EGFR, with an IC50 of 36 nM in subcellular assays. While its effectiveness is comparable to that of gefitinib, O-Desmethyl Gefitinib shows slightly reduced activity in whole-cell assays, with an IC50 of 760, in contrast to gefitinib′s 49 nM. Studies conducted in LoVo tumor mouse xenograft models have revealed that the tumor concentration of O-Desmethyl Gefitinib is notably lower than that of gefitinib, without causing a substantial reduction in tumor growth. Remarkably, increased plasma concentrations of O-Desmethyl Gefitinib in individuals homozygous for CYP2D6 do not lead to an increase in adverse effectsPMID 27154635. O-Desmethyl Gefitinib holds promise for biochemical and biomedical research, providing potential insights into drug development and cancer treatment.
O-去甲基吉非替尼可用于代谢组学和药物发现研究，特别是癌症和肿瘤管理的研究。
O-去甲基吉非替尼是吉非替尼在体内代谢过程中，通过甲基基团从吉非替尼上去除而产生的。
适合多种研究应用的高品质化合物与各种色谱和光谱技术兼容
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本产品仅用于研究目的，不用于人类消费。
| 英文名称 | O-Desmethyl gefitinib |
| CAS 号 | 847949-49-9 |
| 经验分子式 | C21H22ClFN4O3 |
| 分子量 | 432.88 |
| UNSPSC | 12352205 |
| NACRES | NA.77 |
| 形态 | 固体 |
| SMILES字符串 | Fc1c（cc（cc1）Nc2ncnc3c2cc（c（c3）O）OCCCN4CCOCC4）Cl |
| InChI | 1S/C21H22ClFN4O3/c22-16-10-14（2-3-17（16）23）26-21-15-11-20（19（28）12-18（15）24-13-25-21）30-7-1-4-27-5-8-29-9-6-27/h2- 3，10 -13，28H，1，4-9H2，（H，24，25，26） |
| InChI key | IFMMYZUUCFPEHR-UHFFFAOYSA-N |
| 生物来源 | 合成 |
| 含量测定 | ≥95% |
| 技术 | 高效液相色谱（HPLC）：适用 |
| 颜色 | 淡黄色至黄色 |
| 储存温度 | −20°C |
| 质量等级 | 100 |
| 包装规格（货号 SMB00950-5MG） | 5 mg |
