产品说明书
Tesevatinib
 |
同义名 : | EXEL-7647;XL647;KD-019 |
| CAS号 : | 781613-23-8 | |
| 货号 : | A100327 | |
| 分子式 : | C24H25Cl2FN4O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 491.385 | |
| MDL号 : | MFCD22124889 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(213.68 mM)，配合低频超声助溶，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： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | XL647 is a selective EGFR inhibitor with IC50 values of 0.3nM, 16nM, 1.5nM, 8.7nM and 1.4nM for EGFR, ErbB2, KDR, Flt-4 and EphB4, respectively. XL647 inhibited cellular WT and mutant EGFR phosphorylation with IC50 values of 1nM, 12nM, 5nM, 10nM, 5nM and 74nM for EGFR WT (A431), EGFR WT (pCMV/Lx-1), EGFR L858R (pCMV/Lx-1), EGFR L861Q (pCMV/Lx-1), EGFR WT (pTet-On/Lx-1) and EGFR Variant III (pTet-On/Lx-1), respectively. It inhibitsed cellular proliferation and EGFR pathway activation, including p-AKT and p-ERK, in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. Oral administration of XL647 at doses of 10mg/kg, 30mg/kg and 100mg/kg, once daily for 28 days, dose-dependently inhibited tumor growth in athymic mice xenograft A431 tumors. Similarly, significant tumor growth inhibition by administration of XL647 at dose of 100mg/kg could be observed in severe combined immunodeficient mice subcutaneously implantated with H1975 tumor and nude mice subcutaneously implantated with MDA-MB-231 tumor in mammary fat pad. In vivo efficacy studies showed that XL647 reduced both tumor EGFR signaling and tumor vessel density[2]. | ||
| 作用机制 | XL647 is a reversible and ATP competitive inhibitor.[2] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.18mL 2.04mL 1.02mL |
20.35mL 4.07mL 2.04mL |
| 参考文献 |
|---|