Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

27 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 27 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 MlHyT4lv[XOnIHHzd4F6 MnPHglUh|ryP M1TOUGROW09? MkL1bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFYzKG6P M1\GNlI1ODZ3N{Ox
HCC827 NXv1UnJlU2mwYYPlJIF{e2G7 Mn3vglUh|ryP NY\VOGJxTE2VTx?= MnvYbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5PyCwTR?= NF30fpYzPDB4NUezNS=>
HCC827-EPR NHjZZ3ZMcW6jc3WgZZN{[Xl? MoHYglUh|ryP NIH5OGJFVVOR NF7afXhqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOThyIH7N MkP3NlQxPjV5M{G=
PC9 MmXTT4lv[XOnIHHzd4F6 NF64PWV,PSEQvF2= MkXLSG1UVw>? Ml73bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFIyOSCwTR?= MVGyOFA3PTd|MR?=
A431 M3H5TWtqdmG|ZTDhd5NigQ>? M3vDUp42KM7:TR?= M2XBeWROW09? MW\pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlQ{OzFibl2= M3uyPFI1ODZ3N{Ox
NCI-H1299 M3rpc2tqdmG|ZTDhd5NigQ>? NYjE[ZI4hjVizszN NGi3[olFVVOR M1;kSIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,OjByMDDuUS=> MXiyOFA3PTd|MR?=
NCI-H358 M{LO[WtqdmG|ZTDhd5NigQ>? MUL+OUDPxE1? M3XDZ2ROW09? NUfHR4ZFcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O NWjRbnVFOjRyNkW3N|E>
NCI-H1975 NEnoN5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGXIclN,PSEQvF2= M4rhSmROW09? MkDJS2k2OD1|MjDuUS=> NXnLWJo6OjRyNkW3N|E>
HCC827 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXnJUHY2hjVizszN NV3tXHNYTE2VTx?= Mk\wS2k2OD15IH7N NGX1e2UzPDB4NUezNS=>
HCC827-EPR MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWDTXY1khjVizszN NHPyO4dFVVOR MVHHTVUxRTJyIH7N NEK3TW0zPDB4NUezNS=>
PC9 M1vN[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;aTJ42KM7:TR?= NHvGPJJFVVOR MYHHTVUxRTJ4IH7N MmT2NlQxPjV5M{G=
A431 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLNcnhihjVizszN MoDOSG1UVw>? MVLHTVUxRTV2NzDuUS=> M1zVOVI1ODZ3N{Ox
NCI-H1299 NV:yUoV{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4jDPJ42KM7:TR?= MXvEUXNQ M3ywWWdKPTB;NEK3OUBvVQ>? M17rWFI1ODZ3N{Ox
NCI-H358 Ml3CS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\HeGl,PSEQvF2= MmTBSG1UVw>? NInKZYpIUTVyPUG4NFYhdk1? MVKyOFA3PTd|MR?=
PC-9 (exon 19del) M{PVPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUn+NVAh|ryP MU\EUXNQ MWDJR|UxRTh2IH7N NV63PFBoOjZ3MUW0OlQ>
H3255 (L858R) NFTxN2hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3HLPZ4yOCEQvF2= Mk\WSG1UVw>? M2rXTmlEPTB;M{Wgcm0> NHPQUIczPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkfQglExKM7:TR?= MXnEUXNQ NEnSPWVKSzVyPUO3JI5O NX;Td3d5OjZ3MUW0OlQ>
H1975 (L858R+T790M) NIPTcoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVj+NVAh|ryP MlXWSG1UVw>? MUDJR|UxRTJ|IH7N NEjie|UzPjVzNUS2OC=>
BID007 (A763_Y764insFQEA) NYLYXGZCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml;WglExKM7:TR?= NH\4ZZdFVVOR NUX3bIMyUUN3ME2xNlc5KG6P MUiyOlUyPTR4NB?=
Ba/F3 (FQEA) NYP3Z4tNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWT+NVAh|ryP MljsSG1UVw>? NYXRdXczUUN3ME22O|Mhdk1? MViyOlUyPTR4NB?=
Ba/F3 (HH) NU\qSG1kT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV3+NVAh|ryP MXPEUXNQ NFfaVmZKSzVyPUG3N|Ahdk1? MUGyOlUyPTR4NB?=
Ba/F3 (ASV) M{Lpdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkDDglExKM7:TR?= NIK2T3RFVVOR NXPCfZZFUUN3ME21NlkxKG6P NVnzZnBFOjZ3MUW0OlQ>
Ba/F3 (FQEA) M3S1N2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlvxglExKM7:TR?= NInldVRFVVOR NYTo[IFOUUN3ME2yOlIhdk1? MkP0NlY2OTV2NkS=

... 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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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID