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Co1686

(CAS No:1374640-70-6)
Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.
CAS No:1374640-70-6
Molecular Weight(MW):555.55
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 1374640-70-6
Molecular formula(MF) C27H28F3N7O3
Molecular Weight(MW): 555.55
Alias
Solubility
In vitro DMSO 100 mg/mL (180.0 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
Biological Activity
Description Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.
Targets
EGFR (L858R/T790M) [1]
(Cell-free assay)		 EGFR (wt) [1]
(Cell-free assay)
21.5 nM(Ki) 303.3 nM(Ki)
In vitro

CO-1686 inhibits p-EGFR with IC50 ranging from 62 to 187 nM in the mutant EGFR–expressing cells, while inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. CO-1686 selectively inhibits growth of NSCLC cells expressing mutant EGFR with GI50 ranging from 7 to 32 nM, and induces apoptosis. CO-1686–resistant NSCLC cell lines exhibits signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1975 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 62 nM 24065731
HCC827 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 187 nM 24065731
HCC827-EPR Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 180 nM 24065731
PC9 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 211 nM 24065731
A431 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of >4331 nM 24065731
NCI-H1299 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of >2000 nM 24065731
NCI-H358 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of >2000 nM 24065731
NCI-H1975 Growth inhibitory assay ~5 μM DMSO GI50=32 nM 24065731
HCC827 Growth inhibitory assay ~5 μM DMSO GI50=7 nM 24065731
HCC827-EPR Growth inhibitory assay ~5 μM DMSO GI50=20 nM 24065731
PC9 Growth inhibitory assay ~5 μM DMSO GI50=26 nM 24065731
A431 Growth inhibitory assay ~5 μM DMSO GI50=547 nM 24065731
NCI-H1299 Growth inhibitory assay ~5 μM DMSO GI50=4275 nM 24065731
NCI-H358 Growth inhibitory assay ~5 μM DMSO GI50=1806 nM 24065731
PC-9 (exon 19del) Growth inhibitory assay ~10 μM DMSO IC50=84 nM 26515464
H3255 (L858R) Growth inhibitory assay ~10 μM DMSO IC50=35 nM 26515464
PC-9ER (exon 19del+T790M) Growth inhibitory assay ~10 μM DMSO IC50=37 nM 26515464
H1975 (L858R+T790M) Growth inhibitory assay ~10 μM DMSO IC50=23 nM 26515464
BID007 (A763_Y764insFQEA) Growth inhibitory assay ~10 μM DMSO IC50=1278 nM 26515464
Ba/F3 (FQEA) Growth inhibitory assay ~10 μM DMSO IC50=673 nM 26515464
Ba/F3 (HH) Growth inhibitory assay ~10 μM DMSO IC50=1730 nM 26515464
Ba/F3 (ASV) Growth inhibitory assay ~10 μM DMSO IC50=5290 nM 26515464
Ba/F3 (FQEA) Growth inhibitory assay ~10 μM DMSO IC50=262 nM 26515464

... Click to View More Cell Line Experimental Data
In vivo CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. [1]
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