貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S80307-5mg	≥98%	￥890.00 S80307-5mg ￥890.00 現(xiàn)貨	5 5	-	-	-
S80307-10mg	≥98%	￥1330.00 S80307-10mg ￥1330.00 現(xiàn)貨	5 5	-	-	-
S80307-25mg	≥98%	￥2610.00 S80307-25mg ￥2610.00 現(xiàn)貨	4 4	-	-	-
S80307-50mg	≥98%	￥3810.00 S80307-50mg ￥3810.00 現(xiàn)貨	1 1	-	-	-
S80307-100mg	≥98%	￥7200.00 S80307-100mg ￥7200.00 現(xiàn)貨	2 2	-	-	-
S80307-250mg	≥98%	￥14419.00 S80307-250mg ￥14419.00 現(xiàn)貨	1 1	-	-	-

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產(chǎn)品介紹

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

產(chǎn)品描述：

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

靶點(diǎn)：

CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M.;EGFR

體外研究：

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 IC50 values below 20 nM after 1 hour exposure to the drug. CNX-2006 also significantly reduces the volume of tumor spheres derived from H1975 cells. 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 an in vitro resistance 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.

體內(nèi)研究：

CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.

細(xì)胞實(shí)驗(yàn)：

Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.(Only for Reference)

動(dòng)物實(shí)驗(yàn)：

Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p.

參考文獻(xiàn)：

1. Ohashi K, et al. 2013

溶解性：

soluble in DMSO、DMF

保存條件：

-20°C

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.833 ml	9.165 ml	18.331 ml
5 mM	0.367 ml	1.833 ml	3.666 ml
10 mM	0.183 ml	0.917 ml	1.833 ml
50 mM	0.037 ml	0.183 ml	0.367 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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CNX-2006

N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-py