Rociletinib (CO-1686, AVL-301)

Catalog No.S7284 Synonyms: CNX-419

Rociletinib (CO-1686, AVL-301) Chemical Structure

Molecular Weight(MW): 555.55

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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Cited by 8 Publications

5 Customer Reviews

  • Immunohistochemical studies reveal the tumor cells to be negative for chromogranin and synaptophysin pre-rociletinib and positive for both neuroendocrine markers in the post-rociletinib liver biopsy. The results, in conjunction with the morphology, are consistent with the diagnosis of small cell carcinoma in the rociletinib-resistant specimen. H&E, hematoxylin and eosin.

    Cancer Discov, 2015, 5(7): 713-22. Rociletinib (CO-1686, AVL-301) purchased from Selleck.

    Western blot analysis of H1975 mock and H1975 EGFR cells treated with the indicated concentrations of EGF and rociletinib for phosphorylated (p-) and total (t-) EGFR, AKT, ERK1/2, and b-actin.

    Cancer Res, 2017, 77(8):2078-2089. Rociletinib (CO-1686, AVL-301) purchased from Selleck.

  • Lysates from MGH700 cells treated with DMSO or 1 μmol/L of gefi tinib, afatinib, or rociletinib for 6 hours were probed with the indicated antibodies.

    Cancer Discov, 2015, 5(7): 713-22. Rociletinib (CO-1686, AVL-301) purchased from Selleck.

    Lysates from MGH121 parental cells treated with 1 μM of the indicated TKIs except for AZD9291 (160 nM) for 6 hours were probed with the indicated antibodies.

    Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 . Rociletinib (CO-1686, AVL-301) purchased from Selleck.

  • Inhibition of the phosphorylation of EGFR and downstream proteins by EGFR-TKIs in BaF3 cells harboring EGFR mutations. The results of immunoblotting for Ba/F3 cells with EGFR exon 19 deletion, L858R, exon 19 deletion+T790M, and L858R+T790M are shown. The cells were treated with the indicated concentrations of EGFR-TKIs for 4 h. Erlotinib, afatinib, osimertinib, and rociletinib were used as EGFR-TKIs. pEGFR, pAKT, and pERK indicate the phosphorylated form of EGFR, AKT, and ERK, respectively. Actin was used as a loading control.

    Oncotarget, 2015, 6(36):38789-803. . Rociletinib (CO-1686, AVL-301) purchased from Selleck.

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Choose Selective EGFR Inhibitors

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 MmHhT4lv[XOnIHHzd4F6 NIfSWZd,PSEQvF2= MknFSG1UVw>? NVj0RYc1cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKDZ{IH7N Mn6yNlQxPjV5M{G=
HCC827 MnrNT4lv[XOnIHHzd4F6 MVj+OUDPxE1? MXHEUXNQ MV\pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVg4KG6P MUmyOFA3PTd|MR?=
HCC827-EPR NIjFN2JMcW6jc3WgZZN{[Xl? MUX+OUDPxE1? NF\nSHZFVVOR M{XhSYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDBibl2= MkL2NlQxPjV5M{G=
PC9 MWXLbY5ie2ViYYPzZZk> NXzvc2JHhjVizszN NFnsW4JFVVOR M1\TTYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAzOTFibl2= MlfFNlQxPjV5M{G=
A431 MUHLbY5ie2ViYYPzZZk> MmDZglUh|ryP NHvSOpRFVVOR MVrpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlQ{OzFibl2= NW\BbI5iOjRyNkW3N|E>
NCI-H1299 NFy5S4dMcW6jc3WgZZN{[Xl? NI\VWoV,PSEQvF2= NGDSXW5FVVOR MVPpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= NFW3dGwzPDB4NUezNS=>
NCI-H358 NX;hR2xTU2mwYYPlJIF{e2G7 Mnj3glUh|ryP MVrEUXNQ NYPVcG5kcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O NUDVVXRrOjRyNkW3N|E>
NCI-H1975 NF\McY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1TPWJ42KM7:TR?= M2nD[WROW09? M33jUWdKPTB;M{Kgcm0> MlvrNlQxPjV5M{G=
HCC827 Mlf4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1:xSp42KM7:TR?= M2XkTWROW09? MmjjS2k2OD15IH7N M2HmNVI1ODZ3N{Ox
HCC827-EPR M{LEcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2rMd542KM7:TR?= NXvnRnFPTE2VTx?= Mn;YS2k2OD1{MDDuUS=> NX7xRVlsOjRyNkW3N|E>
PC9 NEXLbYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHrSPYd,PSEQvF2= M2\DVmROW09? NVTwdWU1T0l3ME2yOkBvVQ>? NI\CcIQzPDB4NUezNS=>
A431 M33jdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYX+OUDPxE1? NFrGeZZFVVOR NUjrNXoyT0l3ME21OFchdk1? NYjnUYpTOjRyNkW3N|E>
NCI-H1299 NHLFdYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWT+OUDPxE1? NFH1RZNFVVOR NWfLUo12T0l3ME20Nlc2KG6P MWqyOFA3PTd|MR?=
NCI-H358 M1vwfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUTNNFZjhjVizszN NH7R[XNFVVOR Mn31S2k2OD1zOEC2JI5O NYLl[2lbOjRyNkW3N|E>
PC-9 (exon 19del) M2HtdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFH0V4R,OTBizszN MmnYSG1UVw>? NUjiS5J1UUN3ME24OEBvVQ>? M{nCXVI3PTF3NE[0
H3255 (L858R) MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX\+NVAh|ryP NH7XNolFVVOR M4rkOWlEPTB;M{Wgcm0> MWeyOlUyPTR4NB?=
PC-9ER (exon 19del+T790M) M{jqeWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWrRb3FnhjFyIN88US=> M4G5cWROW09? NHPYbYdKSzVyPUO3JI5O M2LmfVI3PTF3NE[0
H1975 (L858R+T790M) NYTCfItkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVKyS4pQhjFyIN88US=> NVvvd5BmTE2VTx?= NH3VPW9KSzVyPUKzJI5O NVrMdlM3OjZ3MUW0OlQ>
BID007 (A763_Y764insFQEA) MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUf+NVAh|ryP Mom0SG1UVw>? MVzJR|UxRTF{N{igcm0> MUWyOlUyPTR4NB?=
Ba/F3 (FQEA) NF3nUY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWLJRnBnhjFyIN88US=> NEjET3BFVVOR MVHJR|UxRTZ5MzDuUS=> NXr4N2FOOjZ3MUW0OlQ>
Ba/F3 (HH) MkP2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX21cXVkhjFyIN88US=> MnPCSG1UVw>? NEm3fJlKSzVyPUG3N|Ahdk1? MX:yOlUyPTR4NB?=
Ba/F3 (ASV) NX;yR3dzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX;+NVAh|ryP NI\NTG5FVVOR NFO1fJBKSzVyPUWyPVAhdk1? NGfjfmszPjVzNUS2OC=>
Ba/F3 (FQEA) NVv3Z2lrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUDVcINqhjFyIN88US=> NV7Ze4U4TE2VTx?= MYnJR|UxRTJ4MjDuUS=> NVGwNlREOjZ3MUW0OlQ>

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
  • Formulation: DMSO: Solutol HS15: PBS (5:15:80; v:v:v)
  • 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 CNX-419

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02705339 Withdrawn Carcinoma Non-Small-Cell Lung|Non-Small Cell Lung Cancer|Nonsmall Cell Lung Cancer Washington University School of Medicine|Clovis Oncology Inc. May 2016 Phase 2
NCT02705339 Withdrawn Carcinoma Non-Small-Cell Lung|Non-Small Cell Lung Cancer|Nonsmall Cell Lung Cancer Washington University School of Medicine|Clovis Oncology Inc. May 2016 Phase 2
NCT02630186 Completed Non-small Cell Lung Cancer Clovis Oncology Inc.|Genentech Inc. January 2016 Phase 1|Phase 2
NCT02630186 Completed Non-small Cell Lung Cancer Clovis Oncology Inc.|Genentech Inc. January 2016 Phase 1|Phase 2
NCT02580708 Terminated Non-small Cell Lung Cancer Clovis Oncology Inc.|Novartis Pharmaceuticals September 30 2015 Phase 1|Phase 2
NCT02580708 Terminated Non-small Cell Lung Cancer Clovis Oncology Inc.|Novartis Pharmaceuticals September 30 2015 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID