规格

价格

库存

数量

2 mg

¥ 252

5日内发货

5 mg

¥ 413

5日内发货

10 mg

¥ 663

5日内发货

25 mg

¥ 1,130

5日内发货

1 mL x 10 mM (in DMSO)

¥ 578

5日内发货

生物活性

产品描述	Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).
靶点活性	EGFR (L858R/T790M):21.5 nM （ki）, EGFR (T790M):303.3 nM （ki）
体外活性	Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition. Rociletinib selectively inhibits the growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly. It inhibits more than 50% of 23 targets.
体内活性	Rociletinib (50 mg/kg bid, p.o.) shows anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice. Rociletinib (100 mg/kg/day, p.o.) displays anti-tumor activity in NSCLC EGFR mutant xenograft models.
别名	CO-1686 (hydrobromide), CNX-419 hydrobromide, AVL-301 hydrobromide

化学信息

分子量	636.46
分子式	C₂₇H₂₉BrF₃N₇O₃
CAS No.	1446700-26-0
Smiles	Br.COc1cc(ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F)N1CCN(CC1)C(C)=O
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 59 mg/mL (92.7 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (3.93 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO