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Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

28 publications

Rociletinib (CO-1686) Chemical Structure

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.

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Selleck's Rociletinib (CO-1686) has been cited by 28 publications

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Choose Selective EGFR Inhibitors

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.
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
HCC827 MkLyT4lv[XOnIHHzd4F6 M2P6WJ42KM7:TR?= Ml\ySG1UVw>? M2HSbolvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDdibl2= M1XybFI1ODZ3N{Ox
HCC827-EPR MlnOT4lv[XOnIHHzd4F6 M3;GbJ42KM7:TR?= NH;odoZFVVOR MX\pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVgxKG6P MYSyOFA3PTd|MR?=
PC9 MoHoT4lv[XOnIHHzd4F6 M3LXSJ42KM7:TR?= Ml7ZSG1UVw>? MVfpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNlEyKG6P NGLKTYQzPDB4NUezNS=>
A431 NF:xU|FMcW6jc3WgZZN{[Xl? NXu3bG5ohjVizszN MlzDSG1UVw>? M2flOYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,PDN|MTDuUS=> M1i2OVI1ODZ3N{Ox
NCI-H1299 NUXMNWFRU2mwYYPlJIF{e2G7 NIe3b4N,PSEQvF2= NVX6XY9tTE2VTx?= MWDpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= NI[3emQzPDB4NUezNS=>
NCI-H1975 NF7mNW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVn+OUDPxE1? NEiwU|FFVVOR NWC1OWJ[T0l3ME2zNkBvVQ>? MVGyOFA3PTd|MR?=
HCC827 NHrJUZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWr+OUDPxE1? M1XENmROW09? NUjHellZT0l3ME23JI5O MoP1NlQxPjV5M{G=
HCC827-EPR MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUL+OUDPxE1? NES3U2RFVVOR Mnu2S2k2OD1{MDDuUS=> MoHCNlQxPjV5M{G=
PC9 M{\q[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrYglUh|ryP M3rCZ2ROW09? NHG4cVFIUTVyPUK2JI5O M1XYO|I1ODZ3N{Ox
A431 NFftWlJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV6zcIVmhjVizszN NWS2Z2l2TE2VTx?= NW\Ge|RHT0l3ME21OFchdk1? MUWyOFA3PTd|MR?=
NCI-H1299 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWT+OUDPxE1? MmKzSG1UVw>? MmTqS2k2OD12Mke1JI5O NWr2XFZkOjRyNkW3N|E>
NCI-H358 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLNfY5QhjVizszN MYLEUXNQ NVvCZ4Y6T0l3ME2xPFA3KG6P NIDqZ4wzPDB4NUezNS=>
PC-9 (exon 19del) NEHVNoJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVj+NVAh|ryP NFLSSplFVVOR NYjUcZh3UUN3ME24OEBvVQ>? Mn7yNlY2OTV2NkS=
H3255 (L858R) MkPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7W[W95hjFyIN88US=> M3jPZmROW09? MWPJR|UxRTN3IH7N NFvFNZgzPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) Mk\SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml;pglExKM7:TR?= NHe0SZBFVVOR M{\TfWlEPTB;M{egcm0> Mn\HNlY2OTV2NkS=
H1975 (L858R+T790M) NHP4OmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4nsc54yOCEQvF2= M4DlVWROW09? MXHJR|UxRTJ|IH7N NHzjV3EzPjVzNUS2OC=>
BID007 (A763_Y764insFQEA) NX3lUGxnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{jQdp4yOCEQvF2= M1P2SGROW09? NVvOfYZvUUN3ME2xNlc5KG6P MYCyOlUyPTR4NB?=
Ba/F3 (FQEA) NV;2[2pMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGj2PGZ,OTBizszN MWLEUXNQ M17KdWlEPTB;NkezJI5O M2qyT|I3PTF3NE[0
Ba/F3 (ASV) MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVWwXopVhjFyIN88US=> MX\EUXNQ NF3i[o5KSzVyPUWyPVAhdk1? MUiyOlUyPTR4NB?=
Ba/F3 (FQEA) NHHPWGxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX3iNVdOhjFyIN88US=> NHm0ToRFVVOR M3j1dGlEPTB;Mk[yJI5O MVmyOlUyPTR4NB?=

... 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]


Kinase Assay:[1]
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Inhibition Kinetics Studies:

Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor.
Cell Research:[1]
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  • Cell lines: NSCLC cell lines expressing mutant EGFR (HCC827, PC9, HCC827-EPR, and NCI-H1975) and cell lines expressing WT EGFR (A431, NCI-H1299, and NCI-H358)
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
  • Dosages: ~50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.0 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 555.55


CAS No. 1374640-70-6
Storage powder
in solvent
Synonyms AVL-301
Smiles CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC

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% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID