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| 货号： | K1007 |
| CAS号： | 152459-95-5 |
| 英文名： | Imatinib (Gleevec)（Targets：v-Abl，c-Kit，PDGFR） |
| 供应商： | 上海高创 |
| 保质期： | 2年 |
| 保存条件： | - 20℃ |
| 规格： | 2mg |
Information
| SKU:K1007 | M. Wt:493.6 | ||
| Formula:C29H31N7O | Solubility:DSMO 3 mg/mL Water <1 mg/ml Ethanol <1 mg/ml | ||
| Purity:>99% | Storage:2 years at -20 degrees centigrade | ||
| CAS No.:152459-95-5 | |||
| Chemical NameN/A | |||
Biological Activity
| Description | Imatinib inhibits c-kit, PDGFR and c-ABL by perfectly binding to adenosine triphosphate (ATP)-binding sites of the c-kit protooncogene product, platelet-derived growth factor receptor (PDGFR), and abelson kinase (c-ABL). | |||||
|---|---|---|---|---|---|---|
| Targets | v-Abl | c-Kit | PDGFR | |||
| IC50 | 0.6 uM | 0.1 uM | 0.1 uM | |||
| In vitro | Imatinib inhibits c-kit, PDGFR and c-ABL by perfectly binding to adenosine triphosphate (ATP)-binding sites of the c-kit protooncogene product, platelet-derived growth factor receptor (PDGFR), and abelson kinase (c-ABL). In vitro, imatinib inhibition of PDGFRs and c-kit phosphorylation was concentration dependent, with an IC50 value of 0.1 to 0.5 uM. By inhibiting bcr-abl kinase activity, Imatinib would induce cytogenetic remissions in the majority of chronic myeloid leukemia patients. Imatinib has been approved as an effective treatment for chronic myeloid leukemia. | |||||
| IN vivo | Imatinib treatment (48 hours) of Leydig tumor cells cultured can reduce the growth rate of MA10 and LC540 cells by 50% to 60% with an IC50 of 5 umol/L. And in the 48 hours, the antiproliferative and apoptotic effect of imatinib is dose-dependent. | |||||
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