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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4 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.

    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.

Purity & Quality Control

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 MnjtT4lv[XOnIHHzd4F6 NVz1[lRzhjVizszN MnrhSG1UVw>? MXvpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gOlIhdk1? M1;xVVI1ODZ3N{Ox
HCC827 NWHkVXdEU2mwYYPlJIF{e2G7 MnK2glUh|ryP MofNSG1UVw>? NVrFfXRrcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKDF6NzDuUS=> NE\OOnEzPDB4NUezNS=>
HCC827-EPR M1vB[WtqdmG|ZTDhd5NigQ>? MnnHglUh|ryP MVvEUXNQ NUXUZ4lUcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKDF6MDDuUS=> NXfjW4pbOjRyNkW3N|E>
PC9 MXvLbY5ie2ViYYPzZZk> MXX+OUDPxE1? M2rtZmROW09? MVTpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNlEyKG6P NVviNY9kOjRyNkW3N|E>
A431 M3TEfWtqdmG|ZTDhd5NigQ>? MXv+OUDPxE1? MWDEUXNQ NYLmVXVCcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD52M{OxJI5O NU\4UI1WOjRyNkW3N|E>
NCI-H1299 NYLrOXlMU2mwYYPlJIF{e2G7 MX3+OUDPxE1? NYrBSmVYTE2VTx?= MnXYbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF4zODByIH7N NIf2d44zPDB4NUezNS=>
NCI-H358 NWHTR|VYU2mwYYPlJIF{e2G7 M3TRXp42KM7:TR?= NVrwfm9zTE2VTx?= NYHFVIc3cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O MmDMNlQxPjV5M{G=
NCI-H1975 MoPvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEXRZ|V,PSEQvF2= NVr5U5BMTE2VTx?= Mm\qS2k2OD1|MjDuUS=> MW[yOFA3PTd|MR?=
HCC827 M4npb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLKglUh|ryP NFLkb2FFVVOR NGT6OYtIUTVyPUegcm0> MYWyOFA3PTd|MR?=
HCC827-EPR NYryXokxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYGwc5R3hjVizszN MXnEUXNQ MlOwS2k2OD1{MDDuUS=> NInKSmYzPDB4NUezNS=>
PC9 MonNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYX+OUDPxE1? MWTEUXNQ NYjuW5FKT0l3ME2yOkBvVQ>? M2HURVI1ODZ3N{Ox
A431 NHvrU5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MortglUh|ryP MYfEUXNQ M2Dkc2dKPTB;NUS3JI5O NWnXcmx1OjRyNkW3N|E>
NCI-H1299 NIPhUmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NW\nPWtThjVizszN MULEUXNQ MWnHTVUxRTR{N{Wgcm0> NYnuUIF1OjRyNkW3N|E>
NCI-H358 M3S1[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVr+OUDPxE1? NYS5RnhyTE2VTx?= NGW3PXRIUTVyPUG4NFYhdk1? NI\IOZMzPDB4NUezNS=>
PC-9 (exon 19del) NYDsUmFTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYL+NVAh|ryP MYrEUXNQ MX;JR|UxRTh2IH7N NELSWXgzPjVzNUS2OC=>
H3255 (L858R) NWGxfGlYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEXjV3J,OTBizszN NIjacY5FVVOR M3fLSGlEPTB;M{Wgcm0> MnyyNlY2OTV2NkS=
PC-9ER (exon 19del+T790M) Ml\PS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnfIglExKM7:TR?= M{XidmROW09? NIDQVXhKSzVyPUO3JI5O M136c|I3PTF3NE[0
H1975 (L858R+T790M) MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NW\kOopphjFyIN88US=> NVnudY1PTE2VTx?= M1PmRmlEPTB;MkOgcm0> M2PBWlI3PTF3NE[0
BID007 (A763_Y764insFQEA) MoG4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUj1WmF2hjFyIN88US=> MmTKSG1UVw>? M{mzUGlEPTB;MUK3PEBvVQ>? MYeyOlUyPTR4NB?=
Ba/F3 (FQEA) NIeybVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWX+NVAh|ryP Ml\3SG1UVw>? M{nhbWlEPTB;NkezJI5O NIDi[mszPjVzNUS2OC=>
Ba/F3 (HH) M4jCV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGHnb3h,OTBizszN NFe1Nm5FVVOR NFv2N3dKSzVyPUG3N|Ahdk1? NFnzbmMzPjVzNUS2OC=>
Ba/F3 (ASV) MkXkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX\2eFVDhjFyIN88US=> MontSG1UVw>? NXvP[Gl[UUN3ME21NlkxKG6P NWHhdVFQOjZ3MUW0OlQ>
Ba/F3 (FQEA) M174[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2HSWJ4yOCEQvF2= NUjZcZlqTE2VTx?= MWnJR|UxRTJ4MjDuUS=> M1\jU|I3PTF3NE[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]
+ 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT02630186 Active, not recruiting Non-small Cell Lung Cancer Clovis Oncology, Inc.|Genentech, Inc. January 2016 Phase 1|Phase 2
NCT02580708 Completed Non-small Cell Lung Cancer Clovis Oncology, Inc.|Novartis Pharmaceuticals September 2015 Phase 1|Phase 2
NCT02322281 Active, not recruiting Non-small Cell Lung Cancer Clovis Oncology, Inc. February 2015 Phase 3
NCT02186301 Active, not recruiting Non-Small Cell Lung Cancer Clovis Oncology, Inc. November 2014 Phase 2|Phase 3
NCT02147990 Active, not recruiting Non-small Cell Lung Cancer Clovis Oncology, Inc. April 2014 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID