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 ()
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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

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID