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 13 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.

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 NU\zS2lwU2mwYYPlJIF{e2G7 NYD4RnlIhjVizszN MUfEUXNQ Mk\UbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFYzKG6P NGPYRVMzPDB4NUezNS=>
HCC827 NGXicldMcW6jc3WgZZN{[Xl? MmPUglUh|ryP NF7v[WxFVVOR M4j4dYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDdibl2= MX2yOFA3PTd|MR?=
HCC827-EPR MkDpT4lv[XOnIHHzd4F6 NX;Fb4lWhjVizszN NHL5W2NFVVOR MUjpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVgxKG6P MVWyOFA3PTd|MR?=
PC9 MlH5T4lv[XOnIHHzd4F6 M2W2WZ42KM7:TR?= NXniWY1UTE2VTx?= M2HEV4lvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAzOTFibl2= MkjWNlQxPjV5M{G=
A431 NH33VXpMcW6jc3WgZZN{[Xl? NVHmUmxRhjVizszN MUHEUXNQ NVu3Vm17cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD52M{OxJI5O MVGyOFA3PTd|MR?=
NCI-H1299 M2K3RWtqdmG|ZTDhd5NigQ>? NHXUbHZ,PSEQvF2= MmrlSG1UVw>? NV;RZoZwcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O NWnFb5I4OjRyNkW3N|E>
NCI-H358 M{PVWmtqdmG|ZTDhd5NigQ>? NITuSFB,PSEQvF2= M1f0WmROW09? NEftdnFqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> Ml24NlQxPjV5M{G=
NCI-H1975 M3rDO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEXFeGl,PSEQvF2= NXnTXpJHTE2VTx?= MWfHTVUxRTN{IH7N NU[wdGNzOjRyNkW3N|E>
HCC827 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{XXOp42KM7:TR?= M3rPW2ROW09? NIq3d29IUTVyPUegcm0> NHj5[HEzPDB4NUezNS=>
HCC827-EPR NIfaWYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHruU2t,PSEQvF2= MVTEUXNQ Mmj4S2k2OD1{MDDuUS=> Ml7PNlQxPjV5M{G=
PC9 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmK4glUh|ryP M17iRWROW09? MlLxS2k2OD1{NjDuUS=> NGX0RXczPDB4NUezNS=>
A431 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVj+OUDPxE1? NVnHRZkxTE2VTx?= M{X1ZmdKPTB;NUS3JI5O MWKyOFA3PTd|MR?=
NCI-H1299 NGP1ToVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{PDep42KM7:TR?= Mof3SG1UVw>? NV2wTWZTT0l3ME20Nlc2KG6P MUKyOFA3PTd|MR?=
NCI-H358 M3vVNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoG5glUh|ryP NHOydFBFVVOR MoqwS2k2OD1zOEC2JI5O NWrOT3F1OjRyNkW3N|E>
PC-9 (exon 19del) NHS2[2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVj4VmtFhjFyIN88US=> NFHZeZBFVVOR NH3vdmJKSzVyPUi0JI5O NFfVeFgzPjVzNUS2OC=>
H3255 (L858R) MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV7+NVAh|ryP NVHtOGJvTE2VTx?= NELXWlFKSzVyPUO1JI5O M1XXdVI3PTF3NE[0
PC-9ER (exon 19del+T790M) NISxc3RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmizglExKM7:TR?= MV;EUXNQ NFrUVZRKSzVyPUO3JI5O NHnEWVczPjVzNUS2OC=>
H1975 (L858R+T790M) M1Gzbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3PhTJ4yOCEQvF2= NFjkc4xFVVOR NVjwV4xoUUN3ME2yN{BvVQ>? M3T0OlI3PTF3NE[0
BID007 (A763_Y764insFQEA) MmftS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUm5XnlEhjFyIN88US=> NHe4[XRFVVOR NVjNXpN[UUN3ME2xNlc5KG6P MWeyOlUyPTR4NB?=
Ba/F3 (FQEA) M2XQbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVPWW3lthjFyIN88US=> MojSSG1UVw>? NFPOd3ZKSzVyPU[3N{BvVQ>? NVXBNoVCOjZ3MUW0OlQ>
Ba/F3 (HH) M4DL[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnzvglExKM7:TR?= NX\0dW9yTE2VTx?= Ml:4TWM2OD1zN{OwJI5O MlfwNlY2OTV2NkS=
Ba/F3 (ASV) MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXvaU4E2hjFyIN88US=> MmPqSG1UVw>? MnXpTWM2OD13MkmwJI5O NYLTTI5lOjZ3MUW0OlQ>
Ba/F3 (FQEA) NFfqWGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M37XRZ4yOCEQvF2= NFG1WHhFVVOR MYHJR|UxRTJ4MjDuUS=> NULiPHhJOjZ3MUW0OlQ>

... 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 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 Completed Drug: Rociletinib Locally Advanced or Metastatic Non Small Cell Lung Cancer Clovis Oncology Inc. March 27 2012 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID