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 34 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 NWi5cI17U2mwYYPlJIF{e2G7 NEXIXZR,PSEQvF2= MX;EUXNQ NHTiXotqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhPjJibl2= MXiyOFA3PTd|MR?=
HCC827 MlHCT4lv[XOnIHHzd4F6 M{XpSp42KM7:TR?= NFXuZphFVVOR Mn7zbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5PyCwTR?= NITpWmkzPDB4NUezNS=>
HCC827-EPR NFfYNmpMcW6jc3WgZZN{[Xl? MofBglUh|ryP NUCyXXlVTE2VTx?= MkXwbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5OCCwTR?= NETUSowzPDB4NUezNS=>
PC9 MULLbY5ie2ViYYPzZZk> MYP+OUDPxE1? MVLEUXNQ MX;pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNlEyKG6P MUmyOFA3PTd|MR?=
A431 NGjhTplMcW6jc3WgZZN{[Xl? NIHv[JF,PSEQvF2= MmH4SG1UVw>? MWjpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlQ{OzFibl2= NXjUT2J2OjRyNkW3N|E>
NCI-H1299 NV7Gc2lKU2mwYYPlJIF{e2G7 NHvUcnl,PSEQvF2= NEXVd2ZFVVOR NG\LO4pqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> NF;RfpUzPDB4NUezNS=>
NCI-H358 NFXZe5ZMcW6jc3WgZZN{[Xl? MWf+OUDPxE1? M1LhWGROW09? NVX5O4s4cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O NVHpZ5hiOjRyNkW3N|E>
NCI-H1975 NIX5fGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NW\Q[WplhjVizszN NXTVU5FjTE2VTx?= NXjHTodMT0l3ME2zNkBvVQ>? NITORoIzPDB4NUezNS=>
HCC827 M4fWTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYD+OUDPxE1? NHL0VJVFVVOR NIn0UXRIUTVyPUegcm0> NHHNdpQzPDB4NUezNS=>
HCC827-EPR MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MofDglUh|ryP NID3eXBFVVOR M4nacGdKPTB;MkCgcm0> MUOyOFA3PTd|MR?=
PC9 MmnSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVvlNGgzhjVizszN Ml;3SG1UVw>? MmH4S2k2OD1{NjDuUS=> NGKzSFkzPDB4NUezNS=>
A431 NXPYWYV1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4Cyb542KM7:TR?= MkjKSG1UVw>? MUDHTVUxRTV2NzDuUS=> M3rKWFI1ODZ3N{Ox
NCI-H1299 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWf+OUDPxE1? MWTEUXNQ M3;v[2dKPTB;NEK3OUBvVQ>? MXuyOFA3PTd|MR?=
NCI-H358 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkTBglUh|ryP MYrEUXNQ MUTHTVUxRTF6ME[gcm0> MlPuNlQxPjV5M{G=
PC-9 (exon 19del) M3vIWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnjBglExKM7:TR?= MnvzSG1UVw>? NXT4S2VXUUN3ME24OEBvVQ>? M1fYclI3PTF3NE[0
H3255 (L858R) NIe1W4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX3+NVAh|ryP MVLEUXNQ NH\rSmFKSzVyPUO1JI5O NVyxc45VOjZ3MUW0OlQ>
PC-9ER (exon 19del+T790M) M4PnXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2qzPZ4yOCEQvF2= NILaO|dFVVOR NHjFXIdKSzVyPUO3JI5O NXj4R4Q{OjZ3MUW0OlQ>
H1975 (L858R+T790M) MoPkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknqglExKM7:TR?= M2\kSmROW09? M1;EWGlEPTB;MkOgcm0> NHvrdWEzPjVzNUS2OC=>
BID007 (A763_Y764insFQEA) MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHiglExKM7:TR?= MVXEUXNQ MonzTWM2OD1zMke4JI5O MUWyOlUyPTR4NB?=
Ba/F3 (FQEA) NWHPXY56T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYT+NVAh|ryP M2H4OGROW09? MYrJR|UxRTZ5MzDuUS=> MVSyOlUyPTR4NB?=
Ba/F3 (HH) MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmrIglExKM7:TR?= MYHEUXNQ M2DTZ2lEPTB;MUezNEBvVQ>? M33NdlI3PTF3NE[0
Ba/F3 (ASV) MoH2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1zGbZ4yOCEQvF2= MoPQSG1UVw>? NGCxfGFKSzVyPUWyPVAhdk1? MmjpNlY2OTV2NkS=
Ba/F3 (FQEA) NFrxVnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml:0glExKM7:TR?= MWTEUXNQ NWXwcIZbUUN3ME2yOlIhdk1? MXmyOlUyPTR4NB?=
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.
Animal Research:[1]
  • Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
  • Dosages: ~50 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

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

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.)

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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

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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 2022-08-01)

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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