Tucatinib
产品说明书
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同义名 : | - |
| CAS号 : | 937263-43-9 | |
| 货号 : | A100992 | |
| 分子式 : | C26H24N8O2 | |
| 纯度 : | 98% | |
| 分子量 : | 480.521 | |
| MDL号 : | MFCD22380467 | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 40 mg/mL(83.24 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Human epidermal growth factor receptor (EGFR; HER1,erbB1), human epidermal growth factor r eceptor 2 (HER2; erbB2), HER3 (erbB3) and HER4 (erbB4) are members of the ErbB family of transmembrane receptor tyrosine kinases. Among them, HER2 is a validated and high-value target. Approximately 30% of breast cancers have an amplification of the HER2/neu gene or overexpression of its protein product, HER2. Also, overexpression of HER2 occurs in gastric, colorectal, NSCLC and ovarian cancers. Irbinitinib is a selective and potent HER2 inhibitor with IC50 value of 8nM, ~500-fold selective for HER2 than EGFR, thus avoiding EGFR-related side effects[1]. Irbinitinib had very good PK/ADME properties both in vitro and in vivo and showed excellent activity in numerous mouse tumor models, including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. Daily oral treatment with Irbinitinib for 90 days achieved tumor growth inhibition by 50% at 50mg/kg and 96% at 100mg/kg in BT-474 model. Daily oral treatment with Irbinitinib, BID, for 90 days achieved tumor growth inhibition by 39% at 50 mg/kg and by 96% at 100 mg/kg in an SKOV-3 model[2]. | ||
| 作用机制 | ARRY-380 an ATP-competitive inhibitor.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.41mL 2.08mL 1.04mL |
20.81mL 4.16mL 2.08mL |
