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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID