Rociletinib (CO-1686)

Catalog No.S7284 Synonyms: AVL-301

For research use only.

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.

Rociletinib (CO-1686) Chemical Structure

CAS No. 1374640-70-6

Selleck's Rociletinib (CO-1686) has been cited by 32 publications

Purity & Quality Control

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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.
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 MYnLbY5ie2ViYYPzZZk> MVL+OUDPxE1? M4P3RmROW09? MVLpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gOlIhdk1? NUjzOmhzOjRyNkW3N|E>
HCC827 MoPyT4lv[XOnIHHzd4F6 MUj+OUDPxE1? M3zNbmROW09? MYTpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVg4KG6P NFj6[VYzPDB4NUezNS=>
HCC827-EPR NEfoOI9McW6jc3WgZZN{[Xl? MlHuglUh|ryP MnrSSG1UVw>? M4LwcolvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDBibl2= NVzsfGs4OjRyNkW3N|E>
PC9 NFrjSnFMcW6jc3WgZZN{[Xl? MXL+OUDPxE1? M4L1SmROW09? NGi3fXlqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOjFzIH7N NVO3[XdIOjRyNkW3N|E>
A431 NHGwW3BMcW6jc3WgZZN{[Xl? M{DlSp42KM7:TR?= M4HFc2ROW09? M4jtZYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,PDN|MTDuUS=> NWLkOIdIOjRyNkW3N|E>
NCI-H1299 M4XUbGtqdmG|ZTDhd5NigQ>? M13Bep42KM7:TR?= MnW3SG1UVw>? Mnq3bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF4zODByIH7N NHvQO4EzPDB4NUezNS=>
NCI-H358 MYLLbY5ie2ViYYPzZZk> Ml3OglUh|ryP MWTEUXNQ NHHDTohqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> MWeyOFA3PTd|MR?=
NCI-H1975 MkTyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjpUJNKhjVizszN NF;WbIZFVVOR Mn6wS2k2OD1|MjDuUS=> NYG5PWlFOjRyNkW3N|E>
HCC827 NXzCO44xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{S3T542KM7:TR?= MojySG1UVw>? NVPoTohYT0l3ME23JI5O MYGyOFA3PTd|MR?=
HCC827-EPR NIPtTYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGnhfXR,PSEQvF2= MXzEUXNQ NFG0T4dIUTVyPUKwJI5O NX\mR4x4OjRyNkW3N|E>
PC9 M3zGT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIjUOol,PSEQvF2= NXLYcXg6TE2VTx?= NWq4dGdnT0l3ME2yOkBvVQ>? MVKyOFA3PTd|MR?=
A431 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2m5W542KM7:TR?= MkD6SG1UVw>? MXvHTVUxRTV2NzDuUS=> M1u2TlI1ODZ3N{Ox
NCI-H1299 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUDvXGo3hjVizszN NU\TZnRVTE2VTx?= MneyS2k2OD12Mke1JI5O NEDpTXUzPDB4NUezNS=>
NCI-H358 MlTxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NG\RNHd,PSEQvF2= M2W0eGROW09? Ml3WS2k2OD1zOEC2JI5O Mn;TNlQxPjV5M{G=
PC-9 (exon 19del) M2nE[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVPWUY1ihjFyIN88US=> NVrtPIk4TE2VTx?= MXrJR|UxRTh2IH7N Ml3UNlY2OTV2NkS=
H3255 (L858R) NH\1coVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjBVmJ,OTBizszN MmCxSG1UVw>? MWfJR|UxRTN3IH7N NEPNRlEzPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXf+NVAh|ryP MkDtSG1UVw>? MV;JR|UxRTN5IH7N MUGyOlUyPTR4NB?=
H1975 (L858R+T790M) M1HBRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mof0glExKM7:TR?= NVrVbJBqTE2VTx?= MWXJR|UxRTJ|IH7N M2fDb|I3PTF3NE[0
BID007 (A763_Y764insFQEA) MnvmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYr+NVAh|ryP Mn7mSG1UVw>? MWTJR|UxRTF{N{igcm0> M13Ld|I3PTF3NE[0
Ba/F3 (FQEA) M1W2[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH64enZ,OTBizszN NFXFR3dFVVOR NYD3do1lUUN3ME22O|Mhdk1? MWCyOlUyPTR4NB?=
Ba/F3 (HH) MkHZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVv5OW9ThjFyIN88US=> NYfoVmxrTE2VTx?= M1L1PWlEPTB;MUezNEBvVQ>? Mn3lNlY2OTV2NkS=
Ba/F3 (ASV) NEfUeI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFTUeGV,OTBizszN NYLRcI84TE2VTx?= M1rXS2lEPTB;NUK5NEBvVQ>? MmXRNlY2OTV2NkS=
Ba/F3 (FQEA) MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M16wRp4yOCEQvF2= MmPBSG1UVw>? MluyTWM2OD1{NkKgcm0> MWWyOlUyPTR4NB?=
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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
Formula

C27H28F3N7O3

CAS No. 1374640-70-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02630186 Terminated Drug: Rociletinib|Drug: MPDL3280A Non-small Cell Lung Cancer Clovis Oncology Inc.|Genentech Inc. February 24 2016 Phase 1|Phase 2
NCT02580708 Terminated Drug: Rociletinib|Drug: Trametinib Non-small Cell Lung Cancer Clovis Oncology Inc.|Novartis Pharmaceuticals September 30 2015 Phase 1|Phase 2
NCT02147990 Terminated Drug: Rociletinib Non-small Cell Lung Cancer Clovis Oncology Inc. June 16 2014 Phase 2
NCT01526928 Terminated Drug: Rociletinib Locally Advanced or Metastatic Non Small Cell Lung Cancer Clovis Oncology Inc. March 27 2012 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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