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Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

28 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.

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Selleck's Rociletinib (CO-1686) has been cited by 28 publications

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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 NHrpSJFMcW6jc3WgZZN{[Xl? NFy2eY5,PSEQvF2= MXTEUXNQ M4TFWYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA3OiCwTR?= M{e3eFI1ODZ3N{Ox
HCC827 MkLyT4lv[XOnIHHzd4F6 M2P6WJ42KM7:TR?= Ml\ySG1UVw>? M2HSbolvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDdibl2= M1XybFI1ODZ3N{Ox
HCC827-EPR MlnOT4lv[XOnIHHzd4F6 M3;GbJ42KM7:TR?= NH;odoZFVVOR MX\pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVgxKG6P MYSyOFA3PTd|MR?=
PC9 MoHoT4lv[XOnIHHzd4F6 M3LXSJ42KM7:TR?= Ml7ZSG1UVw>? MVfpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNlEyKG6P NGLKTYQzPDB4NUezNS=>
A431 NF:xU|FMcW6jc3WgZZN{[Xl? NXu3bG5ohjVizszN MlzDSG1UVw>? M2flOYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,PDN|MTDuUS=> M1i2OVI1ODZ3N{Ox
NCI-H1299 NUXMNWFRU2mwYYPlJIF{e2G7 NIe3b4N,PSEQvF2= NVX6XY9tTE2VTx?= MWDpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlIxODBibl2= NI[3emQzPDB4NUezNS=>
NCI-H358 MUjLbY5ie2ViYYPzZZk> MV;+OUDPxE1? NF:4XmJFVVOR M1j1bIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,OjByMDDuUS=> MXKyOFA3PTd|MR?=
NCI-H1975 NF7mNW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVn+OUDPxE1? NEiwU|FFVVOR NWC1OWJ[T0l3ME2zNkBvVQ>? MVGyOFA3PTd|MR?=
HCC827 NHrJUZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWr+OUDPxE1? M1XENmROW09? NUjHellZT0l3ME23JI5O MoP1NlQxPjV5M{G=
HCC827-EPR MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUL+OUDPxE1? NES3U2RFVVOR Mnu2S2k2OD1{MDDuUS=> MoHCNlQxPjV5M{G=
PC9 M{\q[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrYglUh|ryP M3rCZ2ROW09? NHG4cVFIUTVyPUK2JI5O M1XYO|I1ODZ3N{Ox
A431 NFftWlJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV6zcIVmhjVizszN NWS2Z2l2TE2VTx?= NW\Ge|RHT0l3ME21OFchdk1? MUWyOFA3PTd|MR?=
NCI-H1299 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWT+OUDPxE1? MmKzSG1UVw>? MmTqS2k2OD12Mke1JI5O NWr2XFZkOjRyNkW3N|E>
NCI-H358 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLNfY5QhjVizszN MYLEUXNQ NVvCZ4Y6T0l3ME2xPFA3KG6P NIDqZ4wzPDB4NUezNS=>
PC-9 (exon 19del) NEHVNoJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVj+NVAh|ryP NFLSSplFVVOR NYjUcZh3UUN3ME24OEBvVQ>? Mn7yNlY2OTV2NkS=
H3255 (L858R) MkPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7W[W95hjFyIN88US=> M3jPZmROW09? MWPJR|UxRTN3IH7N NFvFNZgzPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) Mk\SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml;pglExKM7:TR?= NHe0SZBFVVOR M{\TfWlEPTB;M{egcm0> Mn\HNlY2OTV2NkS=
H1975 (L858R+T790M) NHP4OmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4nsc54yOCEQvF2= M4DlVWROW09? MXHJR|UxRTJ|IH7N NHzjV3EzPjVzNUS2OC=>
BID007 (A763_Y764insFQEA) NX3lUGxnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{jQdp4yOCEQvF2= M1P2SGROW09? NVvOfYZvUUN3ME2xNlc5KG6P MYCyOlUyPTR4NB?=
Ba/F3 (FQEA) NV;2[2pMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGj2PGZ,OTBizszN MWLEUXNQ M17KdWlEPTB;NkezJI5O M2qyT|I3PTF3NE[0
Ba/F3 (HH) MnjYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLXNllbhjFyIN88US=> NGDPSZRFVVOR NGnKVVVKSzVyPUG3N|Ahdk1? NYfxWJZUOjZ3MUW0OlQ>
Ba/F3 (ASV) MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVWwXopVhjFyIN88US=> MX\EUXNQ NF3i[o5KSzVyPUWyPVAhdk1? MUiyOlUyPTR4NB?=
Ba/F3 (FQEA) NHHPWGxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX3iNVdOhjFyIN88US=> NHm0ToRFVVOR M3j1dGlEPTB;Mk[yJI5O MVmyOlUyPTR4NB?=

... 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]
- Collapse
  • 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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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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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