An irreversible inhibitor of mutant EGFRs; inhibits EGFR phosphorylation in PC-9 and HCC827 cells (IC50s = 55-104 nM)

CNX-2006 – 10 mg

Brand:
Cayman
CAS:
1375465-09-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

CNX-2006 is an irreversible inhibitor of mutant EGFRs.{54404} 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.  

 

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SKU: 30610 - 10 mg Category:

Description

An irreversible inhibitor of mutant EGFRs; 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; >10-fold selective for cells expressing these mutants over A549 cells expressing wild-type EGFR; inhibits growth in a panel of NSCLC cells expressing wild-type or mutant EGFRs (GI50s = 0.34-8 and 0.003-3.6 μM, respectively); reduces tumor growth in an NCI H1975 mouse xenograft model at 25 and 50 mg/kg

Formal name: N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide

Synonyms: 

Molecular weight: 545.5

CAS: 1375465-09-0

Purity: ≥98%

Formulation: A crystalline solid

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