Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

23 publications

Rociletinib (CO-1686) Chemical Structure

Molecular Weight(MW): 555.55

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 23 publications

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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
NCI-H1975 M3LhTmtqdmG|ZTDhd5NigQ>? NGjK[nF,PSEQvF2= M{PQT2ROW09? MWHpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gOlIhdk1? NGnwSoIzPDB4NUezNS=>
HCC827 NInkNodMcW6jc3WgZZN{[Xl? MVH+OUDPxE1? NWr1UpU{TE2VTx?= NHv6fmlqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOTh5IH7N MknUNlQxPjV5M{G=
HCC827-EPR NGfDTpBMcW6jc3WgZZN{[Xl? MmT5glUh|ryP M3ixRmROW09? MkTqbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5OCCwTR?= MkfCNlQxPjV5M{G=
PC9 MmjoT4lv[XOnIHHzd4F6 NHH2V|N,PSEQvF2= M1zJc2ROW09? NGC0dVdqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOjFzIH7N M1fBRVI1ODZ3N{Ox
A431 MmXiT4lv[XOnIHHzd4F6 NUXvVZoxhjVizszN NYSxV2FLTE2VTx?= NV\aXXhKcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD52M{OxJI5O MWqyOFA3PTd|MR?=
NCI-H1299 M4PQTWtqdmG|ZTDhd5NigQ>? NVe0NJpuhjVizszN NED4RlZFVVOR NFjMT|FqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> NGnpOnEzPDB4NUezNS=>
NCI-H1975 NVnKZVRzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{fOWp42KM7:TR?= MVjEUXNQ NXPneoo6T0l3ME2zNkBvVQ>? MkPGNlQxPjV5M{G=
HCC827 M{DUXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWj+OUDPxE1? NXvwRlZmTE2VTx?= NUO3V|ViT0l3ME23JI5O NInycGszPDB4NUezNS=>
PC9 M2DhS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXvHeI04hjVizszN MnPaSG1UVw>? Mkf6S2k2OD1{NjDuUS=> NUS0OllWOjRyNkW3N|E>
A431 NFTzXpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jXdZ42KM7:TR?= NUPhcmc5TE2VTx?= M3;Z[GdKPTB;NUS3JI5O NYPGOZZJOjRyNkW3N|E>
NCI-H1299 NVrkcmdDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVz+OUDPxE1? MoLCSG1UVw>? NWjWOHAzT0l3ME20Nlc2KG6P M{TvTFI1ODZ3N{Ox
NCI-H358 M2TFeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3LXeZ42KM7:TR?= NGrmXWZFVVOR NGXHWXhIUTVyPUG4NFYhdk1? MWeyOFA3PTd|MR?=
PC-9 (exon 19del) MmnOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVH+NVAh|ryP MV7EUXNQ NHXrV5BKSzVyPUi0JI5O NEizPJMzPjVzNUS2OC=>
H3255 (L858R) MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4TwUZ4yOCEQvF2= MXrEUXNQ M2\6SmlEPTB;M{Wgcm0> Mmm1NlY2OTV2NkS=
PC-9ER (exon 19del+T790M) NHnuZY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoG5glExKM7:TR?= MmrvSG1UVw>? NIfnUmdKSzVyPUO3JI5O NVTvfmtZOjZ3MUW0OlQ>
H1975 (L858R+T790M) NVnlXllbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVj+NVAh|ryP M1\PdmROW09? M1jwfmlEPTB;MkOgcm0> M1LmclI3PTF3NE[0
BID007 (A763_Y764insFQEA) MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWD+NVAh|ryP M1;DXWROW09? M4q1dGlEPTB;MUK3PEBvVQ>? NVjXZldVOjZ3MUW0OlQ>
Ba/F3 (FQEA) MoPsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGPUd2d,OTBizszN NEjh[4FFVVOR NGLwSoJKSzVyPU[3N{BvVQ>? MXuyOlUyPTR4NB?=
Ba/F3 (HH) M123NWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVn1eJRFhjFyIN88US=> NHnRPI1FVVOR MUHJR|UxRTF5M{Cgcm0> Mn;qNlY2OTV2NkS=
Ba/F3 (ASV) M3PITmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWjNfIV6hjFyIN88US=> NHXmdXpFVVOR MkS2TWM2OD13MkmwJI5O MYiyOlUyPTR4NB?=
Ba/F3 (FQEA) MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHHGbY1,OTBizszN M3L4fmROW09? M4\1[WlEPTB;Mk[yJI5O MVKyOlUyPTR4NB?=

... 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 COC1=C(NC2=NC=C(C(=N2)NC3=CC=CC(=C3)NC(=O)C=C)C(F)(F)F)C=CC(=C1)N4CCN(CC4)C(C)=O

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID