产品说明书

Rociletinib

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Chemical Structure| 1374640-70-6 同义名 : -
CAS号 : 1374640-70-6
货号 : A254041
分子式 : C27H28F3N7O3
纯度 : 98%
分子量 : 555.552
MDL号 : MFCD26793864
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: 120 mg/mL(216 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
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • EGFR/ErbB1

    EGFR (wt), Ki:303.3 nM

    EGFR (L858R/T790M), Ki:21.5 nM
描述 Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A431 ~5 μM Kinase assay inhibits pEGFR with IC50 of >4331 nM 24065731
A431 ~5 μM Growth inhibitory assay GI50=547 nM 24065731
Ba/F3 (ASV) ~10 μM Growth inhibitory assay IC50=5290 nM 26515464
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

18.00mL

3.60mL

1.80mL
参考文献

[1]Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.