An irreversible inhibitor of mutant EGFRs
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CNX-2006

Item No. 30610

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
CAS Number
1375465-09-0
Molecular Formula
C26H27F4N7O2
Formula Weight
545.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 10 mg/ml
λmax
276 nm
SMILES
O=C(C=C)NC1=CC=CC(NC2=C(C(F)(F)F)C=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=N2)=C1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CNX-2006 is an irreversible inhibitor of mutant EGFRs.1 It inhibits EGFR phosphorylation in PC-9 and HCC827 cells (IC50s = 55-104 nM), which express the EGFRDel E746_A750 mutation, and NCI H1975 and PC-9/GR4 cells (IC50s = 46 and 61 nM, respectively), which express the EGFRL858R/T790M and EGFRDel E746_A750/T790M mutations, respectively. It is greater than 10-fold selective for cells expressing these mutants over A549 cells expressing wild-type EGFR. CNX-2006 inhibits growth in a panel of non-small cell lung cancer (NSCLC) cells expressing wild-type or mutant EGFRs (GI50s = 0.34-8 and 0.003-3.6 μM, respectively). It reduces tumor growth in an NCI H1975 mouse xenograft model when administered at doses of 25 and 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Galvani, E., Sun, J., Leon, L.G., et al. NF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitor. Oncotarget 6(40), 42717-42732 (2015).