您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > CNX-2006
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
CNX-2006
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CNX-2006图片
CAS NO:1375465-09-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
CNX-2006是不可逆的EGFR突变体抑制剂;对 EGFRT790MIC50值小于20 nM。
生物活性

CNX-2006 is a mutant-selective and irreversibleEGFRinhibitor with anIC50below 20 nM forEGFRT790M.

IC50& Target[1]

EGFRT790M

20 nM (IC50)

EGFRL858R/T790M

 

体外研究
(In Vitro)

CNX-2006 inhibits EGFR-T790M cells growth up to 1000-fold more compared to wild-type EGFR cells. EGFR inhibition is observed in cells harbouring the T790M mutation at IC50values below 20 nM after 1 hour exposure to the drug. CNX-2006 also significantly reduces the volume of tumor spheres derived from H1975 cells[1]. CNX-2006 exhibits specificity and potent activity against T790M. The drug also shows activity against uncommon EGFR mutations including G719S, L861Q, an exon 19 insertion mutant (I744-K745insKIPVAI), and T854A, but not an exon 20 insertion (H773-V774HVdup). In anin vitroresistance model, CNX-2006 significantly inhibits the emergence of resistant cells. Chronic exposure to escalating doses of CNX-2006 fails to select for and/or enhance T790M-mediated resistance using PC-9 or HCC827 cells (both harboring exon 19 deletions), or PC-9/ER and HCC827/ER cells with existing T790M and resistance to erlotinib[2].

分子量

545.53

性状

Solid

Formula

C26H27F4N7O2

CAS 号

1375465-09-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 52 mg/mL(95.32 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8331 mL9.1654 mL18.3308 mL
5 mM0.3666 mL1.8331 mL3.6662 mL
10 mM0.1833 mL0.9165 mL1.8331 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。