Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

24 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 24 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 MmC1T4lv[XOnIHHzd4F6 M3fnZ542KM7:TR?= MXLEUXNQ NHH4emRqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhPjJibl2= NIXXPIIzPDB4NUezNS=>
HCC827 M4TVeWtqdmG|ZTDhd5NigQ>? M3H0NZ42KM7:TR?= NX\XWpN6TE2VTx?= M4m0bIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDdibl2= M3fURlI1ODZ3N{Ox
HCC827-EPR MlHjT4lv[XOnIHHzd4F6 NX7jXJV1hjVizszN M{fFUmROW09? MmezbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5OCCwTR?= NHLCdVgzPDB4NUezNS=>
PC9 NIDCfXJMcW6jc3WgZZN{[Xl? M{fy[p42KM7:TR?= MoqzSG1UVw>? Mn6xbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFIyOSCwTR?= M{fpV|I1ODZ3N{Ox
A431 NELTZopMcW6jc3WgZZN{[Xl? NEXlOIN,PSEQvF2= NV\M[5NlTE2VTx?= NYPjSFU{cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD52M{OxJI5O NFf6S5ozPDB4NUezNS=>
NCI-H1299 NUCwdmNvU2mwYYPlJIF{e2G7 Mo\XglUh|ryP NFjDVmtFVVOR NUHBTGF[cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O MmXoNlQxPjV5M{G=
NCI-H358 MYPLbY5ie2ViYYPzZZk> NG\KPGh,PSEQvF2= NYXEOIx3TE2VTx?= NWrSNmsxcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O M3vpWFI1ODZ3N{Ox
NCI-H1975 MofwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHvkNmx,PSEQvF2= MlG4SG1UVw>? NGf5UldIUTVyPUOyJI5O MYGyOFA3PTd|MR?=
HCC827 NUjkU5I3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4LXbJ42KM7:TR?= MofiSG1UVw>? M1vNSGdKPTB;NzDuUS=> M3q0TFI1ODZ3N{Ox
HCC827-EPR NHnISWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWLHRpJHhjVizszN MkW2SG1UVw>? MmXIS2k2OD1{MDDuUS=> MoLONlQxPjV5M{G=
PC9 M4DURmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX3+OUDPxE1? NH;pRlVFVVOR NGLF[mFIUTVyPUK2JI5O MYqyOFA3PTd|MR?=
A431 NHHhWWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXf+OUDPxE1? MYHEUXNQ NUTqUIVDT0l3ME21OFchdk1? NE\JTYgzPDB4NUezNS=>
NCI-H1299 NFu5TIlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3Ttd542KM7:TR?= NX3rT3cyTE2VTx?= NHzLc4hIUTVyPUSyO|Uhdk1? NEjhZ5UzPDB4NUezNS=>
NCI-H358 NX7lZZZDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVHNWpFuhjVizszN NHzOe4ZFVVOR M1n0cmdKPTB;MUiwOkBvVQ>? NYTTTm5COjRyNkW3N|E>
PC-9 (exon 19del) MoXxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPBglExKM7:TR?= M3PJbGROW09? MXXJR|UxRTh2IH7N M1nPVlI3PTF3NE[0
H3255 (L858R) NGnMdI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVntPGRShjFyIN88US=> M{X1UmROW09? NHnJd|NKSzVyPUO1JI5O NHLYUmczPjVzNUS2OC=>
PC-9ER (exon 19del+T790M) NXjKT2ZZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVj+NVAh|ryP MmHTSG1UVw>? NVy4VVBOUUN3ME2zO{BvVQ>? M1jiTVI3PTF3NE[0
H1975 (L858R+T790M) NGPxZZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoO5glExKM7:TR?= NH24O5VFVVOR M1zpO2lEPTB;MkOgcm0> NFvDTFczPjVzNUS2OC=>
BID007 (A763_Y764insFQEA) NUnjVVRmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIDhfG5,OTBizszN M1ntWWROW09? NFrZUINKSzVyPUGyO|ghdk1? M2THdlI3PTF3NE[0
Ba/F3 (FQEA) MknCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2L2Z54yOCEQvF2= NYfDSJRqTE2VTx?= MYLJR|UxRTZ5MzDuUS=> MV2yOlUyPTR4NB?=
Ba/F3 (HH) NFK0eWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NITa[Jd,OTBizszN Mne2SG1UVw>? MW\JR|UxRTF5M{Cgcm0> NXqwNmhKOjZ3MUW0OlQ>
Ba/F3 (ASV) M37lRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX7+NVAh|ryP MYLEUXNQ NWi5cJhYUUN3ME21NlkxKG6P MnrGNlY2OTV2NkS=
Ba/F3 (FQEA) MoLQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXj6OZZ3hjFyIN88US=> MmHZSG1UVw>? NXntco5LUUN3ME2yOlIhdk1? MUSyOlUyPTR4NB?=

... 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

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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