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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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 M1zNXWtqdmG|ZTDhd5NigQ>? M3vTU542KM7:TR?= NUPtS2t4TE2VTx?= NInpZZJqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhPjJibl2= M1PPc|I1ODZ3N{Ox
HCC827 MlKyT4lv[XOnIHHzd4F6 NFiyT4t,PSEQvF2= NHq2e3VFVVOR MV;pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVg4KG6P NIe5dpozPDB4NUezNS=>
HCC827-EPR Mn3rT4lv[XOnIHHzd4F6 M4\tVJ42KM7:TR?= MmT1SG1UVw>? M4LsSYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDBibl2= NH;TR2QzPDB4NUezNS=>
PC9 NXjwW2NpU2mwYYPlJIF{e2G7 MkPEglUh|ryP NHTWNW9FVVOR Mn36bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFIyOSCwTR?= MXmyOFA3PTd|MR?=
A431 MnL1T4lv[XOnIHHzd4F6 NHTxPYV,PSEQvF2= MYLEUXNQ Mo[5bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF41OzNzIH7N NWHHU5RPOjRyNkW3N|E>
NCI-H1299 MnnFT4lv[XOnIHHzd4F6 M3LNdp42KM7:TR?= M4r2W2ROW09? M4HqfYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,OjByMDDuUS=> NEjKSYMzPDB4NUezNS=>
NCI-H358 MVjLbY5ie2ViYYPzZZk> MV3+OUDPxE1? NWDVZ5FITE2VTx?= MV\pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= M{exZVI1ODZ3N{Ox
NCI-H1975 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVX+OUDPxE1? MXfEUXNQ NEXZ[IdIUTVyPUOyJI5O NWTS[FBKOjRyNkW3N|E>
HCC827 Mkm5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVLqRnVyhjVizszN NFrmZXNFVVOR NXzoZpgxT0l3ME23JI5O NGHMflAzPDB4NUezNS=>
HCC827-EPR M{S3[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGTUOHB,PSEQvF2= M4Hvd2ROW09? MWDHTVUxRTJyIH7N M3XqR|I1ODZ3N{Ox
PC9 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHfZd3d,PSEQvF2= MWPEUXNQ MnrGS2k2OD1{NjDuUS=> M1P5dlI1ODZ3N{Ox
A431 Mne3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWn+OUDPxE1? M1\Pd2ROW09? NYnWTXFyT0l3ME21OFchdk1? MlnrNlQxPjV5M{G=
NCI-H1299 M{fyUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXW4[Wd1hjVizszN NFvjUYdFVVOR MVnHTVUxRTR{N{Wgcm0> MXGyOFA3PTd|MR?=
NCI-H358 MnfwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVHPXGZwhjVizszN M{DCbmROW09? NUfWXIsyT0l3ME2xPFA3KG6P NV7t[JBIOjRyNkW3N|E>
PC-9 (exon 19del) NV60ZYtNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{jyXJ4yOCEQvF2= MYfEUXNQ MW\JR|UxRTh2IH7N MYiyOlUyPTR4NB?=
H3255 (L858R) M2fqUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmDmglExKM7:TR?= NUnFS4tQTE2VTx?= NWm2dIJEUUN3ME2zOUBvVQ>? NWHnfGlMOjZ3MUW0OlQ>
PC-9ER (exon 19del+T790M) NIjFW21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXf+NVAh|ryP M13WSWROW09? NED6U3JKSzVyPUO3JI5O MVGyOlUyPTR4NB?=
H1975 (L858R+T790M) M{fmcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnuzglExKM7:TR?= MlLxSG1UVw>? MlTWTWM2OD1{MzDuUS=> Mme2NlY2OTV2NkS=
BID007 (A763_Y764insFQEA) NViwWZA1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vC[p4yOCEQvF2= Ml[0SG1UVw>? MWHJR|UxRTF{N{igcm0> Moj0NlY2OTV2NkS=
Ba/F3 (FQEA) MofyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXrDXZc{hjFyIN88US=> MXjEUXNQ M13HbGlEPTB;NkezJI5O NXP4THQxOjZ3MUW0OlQ>
Ba/F3 (HH) MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYH+NVAh|ryP MWPEUXNQ NYe0XINxUUN3ME2xO|MxKG6P NV\JXXppOjZ3MUW0OlQ>
Ba/F3 (ASV) MkPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHixe49,OTBizszN NF[5VXFFVVOR MXvJR|UxRTV{OUCgcm0> NYDZWlZDOjZ3MUW0OlQ>
Ba/F3 (FQEA) MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVfkXXZphjFyIN88US=> NV\ub5d2TE2VTx?= MkHhTWM2OD1{NkKgcm0> M3XoWlI3PTF3NE[0

... 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]

Protocol

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
Formula

C27H28F3N7O3
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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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID