Rociletinib (CO-1686, AVL-301)

Catalog No.S7284 Synonyms: CNX-419

Rociletinib (CO-1686, AVL-301) 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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Cited by 19 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 NIe0U2FMcW6jc3WgZZN{[Xl? NEfXTXZ,PSEQvF2= NIrWVXZFVVOR NEDXfldqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhPjJibl2= MUiyOFA3PTd|MR?=
HCC827 M3XrXGtqdmG|ZTDhd5NigQ>? MV7+OUDPxE1? MX3EUXNQ M{j0VIlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDdibl2= NEDTcG8zPDB4NUezNS=>
HCC827-EPR NFmxW|ZMcW6jc3WgZZN{[Xl? MXL+OUDPxE1? MX3EUXNQ NVjLTZBycW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKDF6MDDuUS=> NEj5XpczPDB4NUezNS=>
PC9 NVvETlFrU2mwYYPlJIF{e2G7 NIH1c2h,PSEQvF2= Mm[5SG1UVw>? NHLt[nZqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOjFzIH7N MYiyOFA3PTd|MR?=
A431 NHzHO3BMcW6jc3WgZZN{[Xl? MVH+OUDPxE1? NVfuZWlQTE2VTx?= NVzhcWIxcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD52M{OxJI5O M{\BPFI1ODZ3N{Ox
NCI-H1299 NGjNcIVMcW6jc3WgZZN{[Xl? MUn+OUDPxE1? MVnEUXNQ NHXiWpFqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> MmXhNlQxPjV5M{G=
NCI-H358 Mm\hT4lv[XOnIHHzd4F6 NGO4cph,PSEQvF2= NYToOJpHTE2VTx?= NYjCWINucW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O M4r6dFI1ODZ3N{Ox
NCI-H1975 NImzPIxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mkf6glUh|ryP NYTRZXljTE2VTx?= M2LCWGdKPTB;M{Kgcm0> M3vhelI1ODZ3N{Ox
HCC827 M2jyVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4r6Op42KM7:TR?= Mn;QSG1UVw>? MV7HTVUxRTdibl2= MlLiNlQxPjV5M{G=
HCC827-EPR MmPNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn\oglUh|ryP NWr1[JpWTE2VTx?= NVfZWZlqT0l3ME2yNEBvVQ>? NIL2[4kzPDB4NUezNS=>
PC9 MmHzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NI\NdW5,PSEQvF2= MXvEUXNQ MlLYS2k2OD1{NjDuUS=> M3HDWFI1ODZ3N{Ox
A431 NFHLW3ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYn+OUDPxE1? NGr0SlRFVVOR MUnHTVUxRTV2NzDuUS=> MmnoNlQxPjV5M{G=
NCI-H1299 MnfQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkTvglUh|ryP MnnUSG1UVw>? NGLpeZlIUTVyPUSyO|Uhdk1? MYiyOFA3PTd|MR?=
NCI-H358 NIrFc2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1zET542KM7:TR?= NH;XNGdFVVOR M1X5[GdKPTB;MUiwOkBvVQ>? MnjMNlQxPjV5M{G=
PC-9 (exon 19del) MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWL+NVAh|ryP NYHwWoRYTE2VTx?= NGi4SXZKSzVyPUi0JI5O NXvQWIFWOjZ3MUW0OlQ>
H3255 (L858R) M{jpUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2T6RZ4yOCEQvF2= M1XTT2ROW09? NIHGSZpKSzVyPUO1JI5O MmXJNlY2OTV2NkS=
PC-9ER (exon 19del+T790M) NGnSWVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWHFfmU3hjFyIN88US=> MlL3SG1UVw>? NIjTbHpKSzVyPUO3JI5O M4W2W|I3PTF3NE[0
H1975 (L858R+T790M) NUnyZXBFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3\uOZ4yOCEQvF2= MljTSG1UVw>? NGLIW5BKSzVyPUKzJI5O M4jRXVI3PTF3NE[0
BID007 (A763_Y764insFQEA) M4r6PWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoPuglExKM7:TR?= NWTvVlk3TE2VTx?= MkXXTWM2OD1zMke4JI5O M3TrTlI3PTF3NE[0
Ba/F3 (FQEA) Mny4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGjONVN,OTBizszN M{K0R2ROW09? MVPJR|UxRTZ5MzDuUS=> MYmyOlUyPTR4NB?=
Ba/F3 (HH) MlzLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{nqNZ4yOCEQvF2= MUnEUXNQ MWXJR|UxRTF5M{Cgcm0> MkjoNlY2OTV2NkS=
Ba/F3 (ASV) NVP1dHlXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{O1c54yOCEQvF2= NGT5NFZFVVOR NWKxVXl7UUN3ME21NlkxKG6P NGr2V3YzPjVzNUS2OC=>
Ba/F3 (FQEA) Mn;rS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3PFN54yOCEQvF2= Mnu4SG1UVw>? MXLJR|UxRTJ4MjDuUS=> NV\McZhnOjZ3MUW0OlQ>

... 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 CNX-419

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID