CNX-2006
- CAS编号: 1375465-09-0
- 分子式: C26H27F4N7O2
- 分子量: 545.53
- PubChem编号: 56968072
库存信息
货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
---|---|---|---|---|
C421426-1ml |
1ml | 现货 | |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
---|---|---|---|---|
C421426-1ml |
1ml | 现货 | |
英文别名 | 2-Propenamide,N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- |
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规格或纯度 | 10mM in DMSO |
英文名称 | CNX-2006 |
生化机理 | CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
产品介绍 |
Information CNX-2006 is a novel irreversible mutant-selectiveEGFRinhibitor withIC50of < 20 nM, with very weak inhibition at wild-type EGFR. Targets mutant EGFR <20 nM In vitro CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9. In vivo CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. Cell Research(from reference) Cell lines:HEK293 Concentrations:~1000 nM Incubation Time:6 h |
IC50 | mutant EGFR, IC50: <20 nM |
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ALogP | 5.15 |
HBD Count | 4 |
Rotatable Bond | 12 |
IUPAC Name | N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide |
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INCHI | InChI=1S/C26H27F4N7O2/c1-3-23(38)33-16-5-4-6-17(11-16)34-24-20(26(28,29)30)13-31-25(36-24)35-21-8-7-18(12-22(21)39-2)32-19-14-37(15-19)10-9-27/h3-8,11-13,19,32H,1,9-10,14-15H2,2H3,(H,33,38)(H2,31,34,35,36) |
InChi Key | BFSRTTWIPACGMI-UHFFFAOYSA-N |
Canonical SMILES | COC1=C(C=CC(=C1)NC2CN(C2)CCF)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F |
Isomeric SMILES | COC1=C(C=CC(=C1)NC2CN(C2)CCF)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F |
PubChem CID | 56968072 |
分子量 | 545.53 |
DMSO(mg / mL) Max Solubility | 100 |
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DMSO(mM) Max Solubility | 183.3079757 |
Water(mg / mL) Max Solubility | <1 |
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