Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

30 publications

Rociletinib (CO-1686) Chemical Structure

CAS No. 1374640-70-6

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.

Selleck's Rociletinib (CO-1686) has been cited by 30 publications

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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 NIXPWFlMcW6jc3WgZZN{[Xl? NFTC[Xl,PSEQvF2= M1zSOmROW09? M2\3XIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA3OiCwTR?= NU\BSVhjOjRyNkW3N|E>
HCC827 NYPJR4FbU2mwYYPlJIF{e2G7 MUP+OUDPxE1? MlzDSG1UVw>? Mon5bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5PyCwTR?= NFHIRYkzPDB4NUezNS=>
HCC827-EPR MYnLbY5ie2ViYYPzZZk> NXftN4pvhjVizszN M1rQeWROW09? NEjYfnFqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOThyIH7N M17DVFI1ODZ3N{Ox
PC9 M4XuOmtqdmG|ZTDhd5NigQ>? NIDBeZB,PSEQvF2= NUmzPHNmTE2VTx?= M1TtdIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAzOTFibl2= M{L3eFI1ODZ3N{Ox
A431 M{DwVmtqdmG|ZTDhd5NigQ>? NG\tU45,PSEQvF2= MnKzSG1UVw>? Mn3ibY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF41OzNzIH7N NF62eI8zPDB4NUezNS=>
NCI-H1299 MXzLbY5ie2ViYYPzZZk> NXPlO5cyhjVizszN Moq1SG1UVw>? MYjpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= MXuyOFA3PTd|MR?=
NCI-H358 NXnLTpd7U2mwYYPlJIF{e2G7 NIrZN3N,PSEQvF2= M2r2PWROW09? M4\EcYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,OjByMDDuUS=> NGnxZ4wzPDB4NUezNS=>
NCI-H1975 NGm2WFZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFvqVG9,PSEQvF2= Ml\2SG1UVw>? MWXHTVUxRTN{IH7N MXqyOFA3PTd|MR?=
HCC827 Mo\kS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MojkglUh|ryP M2HYT2ROW09? MlvXS2k2OD15IH7N MXOyOFA3PTd|MR?=
HCC827-EPR NYnqZVdZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXj+OUDPxE1? M3jmdGROW09? NFfiZ49IUTVyPUKwJI5O NYPKeVRtOjRyNkW3N|E>
PC9 NEjy[ohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXT+OUDPxE1? NFntcmZFVVOR MoizS2k2OD1{NjDuUS=> MnvHNlQxPjV5M{G=
A431 NVuyOm9NT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXPseWl{hjVizszN NEiyWGxFVVOR M2j3XmdKPTB;NUS3JI5O NVj4XYlTOjRyNkW3N|E>
NCI-H1299 MnXoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLBdZpZhjVizszN M{TpNmROW09? Mm\uS2k2OD12Mke1JI5O MYeyOFA3PTd|MR?=
NCI-H358 NILVRnhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmfMglUh|ryP MmXrSG1UVw>? MYPHTVUxRTF6ME[gcm0> Mlm3NlQxPjV5M{G=
PC-9 (exon 19del) MoHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVTrXnhQhjFyIN88US=> MkS3SG1UVw>? NWX2OG5SUUN3ME24OEBvVQ>? NFzRdGgzPjVzNUS2OC=>
H3255 (L858R) Mke0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWn+NVAh|ryP MUDEUXNQ M2DSNWlEPTB;M{Wgcm0> NWD6Z4RHOjZ3MUW0OlQ>
PC-9ER (exon 19del+T790M) NHi3dm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEPDTXp,OTBizszN NWPZWmdETE2VTx?= MYLJR|UxRTN5IH7N MnP6NlY2OTV2NkS=
H1975 (L858R+T790M) Mmr5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnzWglExKM7:TR?= MmO5SG1UVw>? MV3JR|UxRTJ|IH7N NUD4U5dEOjZ3MUW0OlQ>
BID007 (A763_Y764insFQEA) NGOxe2VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUL+NVAh|ryP MYHEUXNQ NIHrVHhKSzVyPUGyO|ghdk1? Mn34NlY2OTV2NkS=
Ba/F3 (FQEA) NFv4XlhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4TzU54yOCEQvF2= MXrEUXNQ NV\rVGt6UUN3ME22O|Mhdk1? M2TTSVI3PTF3NE[0
Ba/F3 (HH) MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWT+NVAh|ryP NYn2UWtFTE2VTx?= MkDuTWM2OD1zN{OwJI5O MX:yOlUyPTR4NB?=
Ba/F3 (ASV) MkfvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY\+NVAh|ryP MkjBSG1UVw>? Ml3YTWM2OD13MkmwJI5O Ml;tNlY2OTV2NkS=
Ba/F3 (FQEA) MmPRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3pV4d,OTBizszN MW\EUXNQ M1SzUGlEPTB;Mk[yJI5O NGLQOWczPjVzNUS2OC=>

... 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]
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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]
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  • 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]
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  • Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
  • 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 AVL-301
Smiles CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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 Terminated Drug: Rociletinib Locally Advanced or Metastatic Non Small Cell Lung Cancer Clovis Oncology Inc. March 27 2012 Phase 1|Phase 2

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID