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.

    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, 77(8):2078-2089. 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 MkLhT4lv[XOnIHHzd4F6 NYi1WGdVhjVizszN NYD2[llRTE2VTx?= M2\kT4lvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA3OiCwTR?= MUKyOFA3PTd|MR?=
HCC827 NUj1flVOU2mwYYPlJIF{e2G7 MoXtglUh|ryP M4P5SmROW09? MWHpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVg4KG6P NIHpVmwzPDB4NUezNS=>
HCC827-EPR MneyT4lv[XOnIHHzd4F6 M2fvT542KM7:TR?= MV\EUXNQ M4S0V4lvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDBibl2= NVL4UZNOOjRyNkW3N|E>
PC9 NHjl[XNMcW6jc3WgZZN{[Xl? NVHZflBvhjVizszN NGr0RWZFVVOR Mn61bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFIyOSCwTR?= M1nhU|I1ODZ3N{Ox
A431 MWHLbY5ie2ViYYPzZZk> NX;VfGJxhjVizszN NXnRO3I6TE2VTx?= M1u3bIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,PDN|MTDuUS=> Mmq1NlQxPjV5M{G=
NCI-H1299 Ml7TT4lv[XOnIHHzd4F6 NVi3N2tThjVizszN NH3GUINFVVOR MWfpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= MnPXNlQxPjV5M{G=
NCI-H358 MmfaT4lv[XOnIHHzd4F6 M1i4WJ42KM7:TR?= NYLxRVc4TE2VTx?= MV7pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= MV[yOFA3PTd|MR?=
NCI-H1975 M2r2ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGnRbGV,PSEQvF2= Ml3rSG1UVw>? M4HuWWdKPTB;M{Kgcm0> NH:x[FczPDB4NUezNS=>
HCC827 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn\xglUh|ryP MWLEUXNQ M2Xpb2dKPTB;NzDuUS=> NHnETJMzPDB4NUezNS=>
HCC827-EPR NFfBVWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2PTXp42KM7:TR?= NVHwZWRNTE2VTx?= MlLsS2k2OD1{MDDuUS=> M2nNRVI1ODZ3N{Ox
PC9 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MofnglUh|ryP NX3hSpNJTE2VTx?= M{jNS2dKPTB;Mk[gcm0> Mn;aNlQxPjV5M{G=
A431 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX;rTpVYhjVizszN NGHCdJlFVVOR MWrHTVUxRTV2NzDuUS=> NEnlTJYzPDB4NUezNS=>
NCI-H1299 M4XPdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoP3glUh|ryP MnezSG1UVw>? M2XafGdKPTB;NEK3OUBvVQ>? M2nQeFI1ODZ3N{Ox
NCI-H358 M4LuOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWf+OUDPxE1? MXvEUXNQ M4\Ce2dKPTB;MUiwOkBvVQ>? MkCxNlQxPjV5M{G=
PC-9 (exon 19del) NHXoVIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml3vglExKM7:TR?= M3PuVGROW09? M2C1OmlEPTB;OESgcm0> M3\sUVI3PTF3NE[0
H3255 (L858R) MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVK2N29PhjFyIN88US=> MVnEUXNQ NEfBTJBKSzVyPUO1JI5O NIi2[nkzPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) NULNb4NyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFPyT|V,OTBizszN MojaSG1UVw>? NXLDcFdFUUN3ME2zO{BvVQ>? NHTab5gzPjVzNUS2OC=>
H1975 (L858R+T790M) MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoLsglExKM7:TR?= M4nPOGROW09? NWPNN2FGUUN3ME2yN{BvVQ>? MV:yOlUyPTR4NB?=
BID007 (A763_Y764insFQEA) NUmwWJluT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml3BglExKM7:TR?= NIrXXnZFVVOR MYnJR|UxRTF{N{igcm0> NYLXeHU3OjZ3MUW0OlQ>
Ba/F3 (FQEA) MoHvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHexNVJ,OTBizszN MVTEUXNQ NVzvWYNWUUN3ME22O|Mhdk1? NVTFNJN7OjZ3MUW0OlQ>
Ba/F3 (HH) M3X4TGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlrCglExKM7:TR?= NGPqNoxFVVOR M3TjeWlEPTB;MUezNEBvVQ>? MYGyOlUyPTR4NB?=
Ba/F3 (ASV) MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWTqcGV3hjFyIN88US=> MknvSG1UVw>? NXjDWYRPUUN3ME21NlkxKG6P MlriNlY2OTV2NkS=
Ba/F3 (FQEA) NIXzOWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX:zN2wyhjFyIN88US=> NV;y[5ViTE2VTx?= NELWcVNKSzVyPUK2NkBvVQ>? MXWyOlUyPTR4NB?=

... 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