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Rociletinib (CO-1686)

Name: Rociletinib (CO-1686)
Brand: Selleck Chemicals
SKU: S7284
Rating: 5 (32 reviews)

Catalog No.S7284 Synonyms: AVL-301

For research use only.

Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with K_i of 21.5 nM and 303.3 nM for EGFR^L858R/T790M and EGFR^WT in cell-free assays, respectively. Phase 2.

Rociletinib (CO-1686) Chemical Structure

CAS No. 1374640-70-6

Selleck's Rociletinib (CO-1686) has been cited by 32 publications

Purity & Quality Control

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EGFR Signaling Pathway Map

Biological Activity

Description

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	MYnLbY5ie2ViYYPzZZk>	MVL+OUDPxE1?	M4P3RmROW09?	MVLpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gOlIhdk1?	NUjzOmhzOjRyNkW3N\|E>
HCC827	MoPyT4lv[XOnIHHzd4F6	MUj+OUDPxE1?	M3zNbmROW09?	MYTpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVg4KG6P	NFj6[VYzPDB4NUezNS=>
HCC827-EPR	NEfoOI9McW6jc3WgZZN{[Xl?	MlHuglUh\|ryP	MnrSSG1UVw>?	M4LwcolvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDBibl2=	NVzsfGs4OjRyNkW3N\|E>
PC9	NFrjSnFMcW6jc3WgZZN{[Xl?	MXL+OUDPxE1?	M4L1SmROW09?	NGi3fXlqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhOjFzIH7N	NVO3[XdIOjRyNkW3N\|E>
A431	NHGwW3BMcW6jc3WgZZN{[Xl?	M{DlSp42KM7:TR?=	M4HFc2ROW09?	M4jtZYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,PDN\|MTDuUS=>	NWLkOIdIOjRyNkW3N\|E>
NCI-H1299	M4XUbGtqdmG\|ZTDhd5NigQ>?	M13Bep42KM7:TR?=	MnW3SG1UVw>?	Mnq3bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF4zODByIH7N	NHvQO4EzPDB4NUezNS=>
NCI-H358	MYLLbY5ie2ViYYPzZZk>	Ml3OglUh\|ryP	MWTEUXNQ	NHHDTohqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0>	MWeyOFA3PTd\|MR?=
NCI-H1975	MkTyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NVjpUJNKhjVizszN	NF;WbIZFVVOR	Mn6wS2k2OD1\|MjDuUS=>	NYG5PWlFOjRyNkW3N\|E>
HCC827	NXzCO44xT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M{S3T542KM7:TR?=	MojySG1UVw>?	NVPoTohYT0l3ME23JI5O	MYGyOFA3PTd\|MR?=
HCC827-EPR	NIPtTYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NGnhfXR,PSEQvF2=	MXzEUXNQ	NFG0T4dIUTVyPUKwJI5O	NX\mR4x4OjRyNkW3N\|E>
PC9	M3zGT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NIjUOol,PSEQvF2=	NXLYcXg6TE2VTx?=	NWq4dGdnT0l3ME2yOkBvVQ>?	MVKyOFA3PTd\|MR?=
A431	MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M2m5W542KM7:TR?=	MkD6SG1UVw>?	MXvHTVUxRTV2NzDuUS=>	M1u2TlI1ODZ3N{Ox
NCI-H1299	MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NUDvXGo3hjVizszN	NU\TZnRVTE2VTx?=	MneyS2k2OD12Mke1JI5O	NEDpTXUzPDB4NUezNS=>
NCI-H358	MlTxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NG\RNHd,PSEQvF2=	M2W0eGROW09?	Ml3WS2k2OD1zOEC2JI5O	Mn;TNlQxPjV5M{G=
PC-9 (exon 19del)	M2nE[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NVPWUY1ihjFyIN88US=>	NVrtPIk4TE2VTx?=	MXrJR\|UxRTh2IH7N	Ml3UNlY2OTV2NkS=
H3255 (L858R)	NH\1coVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NIjBVmJ,OTBizszN	MmCxSG1UVw>?	MWfJR\|UxRTN3IH7N	NEPNRlEzPjVzNUS2OC=>
PC-9ER (exon 19del+T790M)	MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MXf+NVAh\|ryP	MkDtSG1UVw>?	MV;JR\|UxRTN5IH7N	MUGyOlUyPTR4NB?=
H1975 (L858R+T790M)	M1HBRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Mof0glExKM7:TR?=	NVrVbJBqTE2VTx?=	MWXJR\|UxRTJ\|IH7N	M2fDb\|I3PTF3NE[0
BID007 (A763_Y764insFQEA)	MnvmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MYr+NVAh\|ryP	Mn7mSG1UVw>?	MWTJR\|UxRTF{N{igcm0>	M13Ld\|I3PTF3NE[0
Ba/F3 (FQEA)	M1W2[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NH64enZ,OTBizszN	NFXFR3dFVVOR	NYD3do1lUUN3ME22O\|Mhdk1?	MWCyOlUyPTR4NB?=
Ba/F3 (HH)	MkHZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NVv5OW9ThjFyIN88US=>	NYfoVmxrTE2VTx?=	M1L1PWlEPTB;MUezNEBvVQ>?	Mn3lNlY2OTV2NkS=
Ba/F3 (ASV)	NEfUeI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NFTUeGV,OTBizszN	NYLRcI84TE2VTx?=	M1rXS2lEPTB;NUK5NEBvVQ>?	MmXRNlY2OTV2NkS=
Ba/F3 (FQEA)	MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M16wRp4yOCEQvF2=	MmPBSG1UVw>?	MluyTWM2OD1{NkKgcm0>	MWWyOlUyPTR4NB?=

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 (from reference)

Kinase Assay:^[1]	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]	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]	Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. Dosages: ~50 mg/kg Administration: Oral gavage (Only for Reference)

References

[1] Walter AO, et al. Cancer Discov. 2013. doi:10.1158/2159-8290.CD-13-0314

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. Click to purchase: Tween 80	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	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
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

Download Rociletinib (CO-1686) SDF

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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