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CNX-2006

目录号: PL03802 纯度: ≥99%

CNX-2006是不可逆的 EGFR 突变体抑制剂；对 EGFR^T790M 的IC50 值小于20 nM。

CAS No. :1375465-09-0

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中文名称	CNX-2006
中文别名	CNX2006 抑制剂;N-[3-[[2-[[4-[[1-(2-氟乙基)-3-氮杂啶]氨基]-2-甲氧基苯基]氨基]-5-(三氟甲基)-4-嘧啶]氨基]苯基]-2-丙酰胺;N-[3-[[2-[[4-[[1-(2-氟乙基)-3-氮杂环丁基]氨基]-2-甲氧基苯基]氨基]-5-(三氟甲基)-4-嘧啶基]氨基]苯基]-2-丙烯酰胺
英文名称	CNX-2006
英文别名	N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide;AGN-PC-0BL9UN;KB-308457;N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-py;CNX2006;CNX-2006;N-?[3-?[[2-?[[4-?[[1-?(2-?fluoroethyl)?-?3-?azetidinyl]?amino]?-?2-?methoxyphenyl]?amino]?-?5-?(tr;N-[3-({2-[(4-{[1-(2-Fluoroethyl)-3-azetidinyl]amino}-2-methoxyphe nyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)phenyl]acrylam ide;N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phe...;N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2;N-[3-[[2-[[4-[[1-(2-Fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide;N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-e;N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide;C26H27F4N7O2;BDBM238270;HMS3653K17;BC
Cas No.	1375465-09-0
分子式	C₂₆H₂₇F₄N₇O₂
分子量	545.53
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	CNX-2006是不可逆的 EGFR 突变体抑制剂；对 EGFR^T790M 的IC50 值小于20 nM。

产品详情	CNX-2006是不可逆的 EGFR 突变体抑制剂；对 EGFR^T790M 的IC₅₀ 值小于20 nM。
生物活性	CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC 50 below 20 nM for EGFR.
性状	Solid
IC50 & Target[1][2]	EGFR 20 nM (IC50) EGFR
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 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
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Galvani E, et al. Abstract 3244: Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX-2006, a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC. CNX-2006, a novel mutant-selective EGFR inhib [2]. Ohashi K, et al. Abstract 2101A: CNX-2006, a novel irreversible epidermal growth factor receptor (EGFR) inhibitor, selectively inhibits EGFR T790M and fails to induce T790M-mediated resistance in vitro. [abstract]. In: Proceedings of the 104th Annual Meet

溶解度数据	In Vitro: DMSO : ≥ 52 mg/mL (95.32 mM)配制储备液

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[1]. Galvani E, et al. Abstract 3244: Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX-2006, a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC. CNX-2006, a novel mutant-selective EGFR inhib
[2]. Ohashi K, et al. Abstract 2101A: CNX-2006, a novel irreversible epidermal growth factor receptor (EGFR) inhibitor, selectively inhibits EGFR T790M and fails to induce T790M-mediated resistance in vitro. [abstract]. In: Proceedings of the 104th Annual Meet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

CNX-2006

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