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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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.

    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.

    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.. 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 NH7DPIJMcW6jc3WgZZN{[Xl? M{HSb542KM7:TR?= MYnEUXNQ MYfpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gOlIhdk1? Ml64NlQxPjV5M{G=
HCC827 NYDJbpNOU2mwYYPlJIF{e2G7 MnewglUh|ryP MYTEUXNQ NIPuN5pqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOTh5IH7N M4HYXVI1ODZ3N{Ox
HCC827-EPR M3PMWGtqdmG|ZTDhd5NigQ>? M3fZfZ42KM7:TR?= NV;jbWZ3TE2VTx?= MlTKbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5OCCwTR?= NVPCW2tiOjRyNkW3N|E>
PC9 MV\LbY5ie2ViYYPzZZk> MmHxglUh|ryP MlHRSG1UVw>? M4TtZYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAzOTFibl2= MkPDNlQxPjV5M{G=
A431 MXPLbY5ie2ViYYPzZZk> Mli0glUh|ryP MXnEUXNQ MYjpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlQ{OzFibl2= MWSyOFA3PTd|MR?=
NCI-H1299 NEDyfW9McW6jc3WgZZN{[Xl? NFywc|l,PSEQvF2= NGDEd2pFVVOR MXHpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= NVvwNmFtOjRyNkW3N|E>
NCI-H358 M4f5U2tqdmG|ZTDhd5NigQ>? M{nPb542KM7:TR?= MX3EUXNQ M2XtXYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,OjByMDDuUS=> NIC0VVMzPDB4NUezNS=>
NCI-H1975 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4HUWJ42KM7:TR?= MmjvSG1UVw>? Ml;OS2k2OD1|MjDuUS=> NF;S[VYzPDB4NUezNS=>
HCC827 NHXD[mRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXvReVY1hjVizszN NFn3bFVFVVOR NInkO2pIUTVyPUegcm0> M1m0W|I1ODZ3N{Ox
HCC827-EPR NX\VcmlkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWH+OUDPxE1? NIr1S|VFVVOR MVXHTVUxRTJyIH7N MlrXNlQxPjV5M{G=
PC9 NXe2b2lWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVT+OUDPxE1? NX:wXY4xTE2VTx?= NUS2Vm9ET0l3ME2yOkBvVQ>? Mn33NlQxPjV5M{G=
A431 NHeyOFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3vqTZ42KM7:TR?= MofySG1UVw>? MUHHTVUxRTV2NzDuUS=> NITPOVMzPDB4NUezNS=>
NCI-H1299 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYfQTo1{hjVizszN Ml\rSG1UVw>? NGjZPIVIUTVyPUSyO|Uhdk1? MlfsNlQxPjV5M{G=
NCI-H358 NYrvfJdQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX\+OUDPxE1? NVriUIZCTE2VTx?= Mki0S2k2OD1zOEC2JI5O MkK5NlQxPjV5M{G=
PC-9 (exon 19del) MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGHjZWl,OTBizszN MmPySG1UVw>? MnmzTWM2OD16NDDuUS=> MlHlNlY2OTV2NkS=
H3255 (L858R) Mk\HS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;EWpF,OTBizszN MWnEUXNQ MYfJR|UxRTN3IH7N NHHkWmgzPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) Ml25S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXKglExKM7:TR?= MWDEUXNQ M4L5[2lEPTB;M{egcm0> MVGyOlUyPTR4NB?=
H1975 (L858R+T790M) M{nqcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUHpfGk4hjFyIN88US=> MXjEUXNQ MXPJR|UxRTJ|IH7N MWeyOlUyPTR4NB?=
BID007 (A763_Y764insFQEA) M17QN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnLlglExKM7:TR?= NF\1d5NFVVOR NEWzc3pKSzVyPUGyO|ghdk1? NFXMUW8zPjVzNUS2OC=>
Ba/F3 (FQEA) NGHBPJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHrwS4Z,OTBizszN NGX0eXJFVVOR NIHERYhKSzVyPU[3N{BvVQ>? NVHPeHZ5OjZ3MUW0OlQ>
Ba/F3 (HH) MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLEOotIhjFyIN88US=> MlKySG1UVw>? MVrJR|UxRTF5M{Cgcm0> NYXTXY1POjZ3MUW0OlQ>
Ba/F3 (ASV) NEe0fYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2\3[54yOCEQvF2= MlTrSG1UVw>? M2fDPGlEPTB;NUK5NEBvVQ>? MV2yOlUyPTR4NB?=
Ba/F3 (FQEA) Mnu2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmLwglExKM7:TR?= MVjEUXNQ M3zrZmlEPTB;Mk[yJI5O MknTNlY2OTV2NkS=

... 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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
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