Rociletinib (CO-1686)

For research use only. Not for use in humans.

Catalog No.S7284 Synonyms: AVL-301

20 publications

Rociletinib (CO-1686) 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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Selleck's Rociletinib (CO-1686) has been cited by 20 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 Mn3ET4lv[XOnIHHzd4F6 M17KZZ42KM7:TR?= M2fBfmROW09? Ml\sbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFYzKG6P MVmyOFA3PTd|MR?=
HCC827 MYPLbY5ie2ViYYPzZZk> MVn+OUDPxE1? MYLEUXNQ NH7VdpdqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOTh5IH7N NHe3enozPDB4NUezNS=>
HCC827-EPR MYTLbY5ie2ViYYPzZZk> MWL+OUDPxE1? M{X2ZWROW09? MkLzbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5OCCwTR?= MnewNlQxPjV5M{G=
PC9 MnvsT4lv[XOnIHHzd4F6 MonjglUh|ryP NV7VOHhHTE2VTx?= NUPUbJBUcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKDJzMTDuUS=> MknxNlQxPjV5M{G=
A431 MYjLbY5ie2ViYYPzZZk> MV;+OUDPxE1? Mn;FSG1UVw>? MWfpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlQ{OzFibl2= MkL5NlQxPjV5M{G=
NCI-H1299 MmrIT4lv[XOnIHHzd4F6 M1iyWJ42KM7:TR?= MYnEUXNQ NEn2UG5qdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> M2TwUlI1ODZ3N{Ox
NCI-H358 MWXLbY5ie2ViYYPzZZk> NGP2O3Z,PSEQvF2= MYHEUXNQ MmjrbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF4zODByIH7N MmPXNlQxPjV5M{G=
NCI-H1975 M{K4ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHjyXnp,PSEQvF2= M2ThTGROW09? NUW3UJp6T0l3ME2zNkBvVQ>? MXSyOFA3PTd|MR?=
HCC827 M{jjcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVH+OUDPxE1? MYHEUXNQ NH:5doFIUTVyPUegcm0> Ml3PNlQxPjV5M{G=
HCC827-EPR MmPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXTVWm1ThjVizszN M2LHVWROW09? MmXHS2k2OD1{MDDuUS=> MmPzNlQxPjV5M{G=
PC9 NVrPU3BbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmLuglUh|ryP NY[wSnpNTE2VTx?= M3iz[GdKPTB;Mk[gcm0> M{PCUFI1ODZ3N{Ox
A431 NV[x[|BDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrpUohbhjVizszN NViyepUzTE2VTx?= MXrHTVUxRTV2NzDuUS=> MYeyOFA3PTd|MR?=
NCI-H1299 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWfHbIFVhjVizszN M{TCU2ROW09? MkfaS2k2OD12Mke1JI5O NGXMbGszPDB4NUezNS=>
NCI-H358 MmHwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVuwbGpOhjVizszN MYHEUXNQ MkPvS2k2OD1zOEC2JI5O NGDZZWgzPDB4NUezNS=>
PC-9 (exon 19del) NXP6PHRnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV7+NVAh|ryP MkHySG1UVw>? MVjJR|UxRTh2IH7N MnzyNlY2OTV2NkS=
H3255 (L858R) MmPjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlywglExKM7:TR?= NXjNVm5MTE2VTx?= MXjJR|UxRTN3IH7N MofTNlY2OTV2NkS=
PC-9ER (exon 19del+T790M) M1fT[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXL+NVAh|ryP NIXUdYtFVVOR M2ThNWlEPTB;M{egcm0> Mo\WNlY2OTV2NkS=
H1975 (L858R+T790M) MnS0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHafFB,OTBizszN M{PYVmROW09? NYrjW|Q3UUN3ME2yN{BvVQ>? M{m0fVI3PTF3NE[0
BID007 (A763_Y764insFQEA) NEn2UYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFLC[IZ,OTBizszN Ml3QSG1UVw>? NUO3U3U6UUN3ME2xNlc5KG6P NWHXVVhrOjZ3MUW0OlQ>
Ba/F3 (FQEA) MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml3NglExKM7:TR?= NHG0blhFVVOR M4H3OWlEPTB;NkezJI5O NGXyemUzPjVzNUS2OC=>
Ba/F3 (HH) MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnWwglExKM7:TR?= MnfrSG1UVw>? MX7JR|UxRTF5M{Cgcm0> MYWyOlUyPTR4NB?=
Ba/F3 (ASV) NV\odVNZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mnv5glExKM7:TR?= NEn1SHdFVVOR MVHJR|UxRTV{OUCgcm0> MXyyOlUyPTR4NB?=
Ba/F3 (FQEA) MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX7GVJhwhjFyIN88US=> M13O[mROW09? Ml\yTWM2OD1{NkKgcm0> NXznUJI{OjZ3MUW0OlQ>

... 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.
  • 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 AVL-301
Smiles COC1=C(NC2=NC=C(C(=N2)NC3=CC=CC(=C3)NC(=O)C=C)C(F)(F)F)C=CC(=C1)N4CCN(CC4)C(C)=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID