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Rociletinib (CO-1686)

Name: Rociletinib (CO-1686)
Brand: Selleck Chemicals
SKU: S7284
Rating: 5 (34 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 34 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	NWH1NWJJU2mwYYPlJIF{e2G7	M{HiW542KM7:TR?=	NETjNI5FVVOR	NYDndmRRcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKDZ{IH7N	NV[3dII{OjRyNkW3N\|E>
HCC827	NUK4S3F7U2mwYYPlJIF{e2G7	NInOVFF,PSEQvF2=	MX3EUXNQ	MnnjbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5PyCwTR?=	MlP2NlQxPjV5M{G=
HCC827-EPR	Mn61T4lv[XOnIHHzd4F6	NWjidJBKhjVizszN	Mn[2SG1UVw>?	MXzpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNVgxKG6P	MX[yOFA3PTd\|MR?=
PC9	NVf3[nY6U2mwYYPlJIF{e2G7	NVqwd25qhjVizszN	MX\EUXNQ	Mne4bY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFIyOSCwTR?=	MX6yOFA3PTd\|MR?=
A431	NX6yfnBOU2mwYYPlJIF{e2G7	NECwfmV,PSEQvF2=	NYjIVWZqTE2VTx?=	NIXQXndqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjR\|M{Ggcm0>	NEHEXYUzPDB4NUezNS=>
NCI-H1299	NYD0cnpMU2mwYYPlJIF{e2G7	NUewVXFJhjVizszN	NVz4UVdxTE2VTx?=	NWOxVm9kcW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O	NFTWZZYzPDB4NUezNS=>
NCI-H358	NITxXJVMcW6jc3WgZZN{[Xl?	NV7zOlg3hjVizszN	NYrQfmhxTE2VTx?=	M2TweolvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kA,OjByMDDuUS=>	M4LiXVI1ODZ3N{Ox
NCI-H1975	NVXwTnBQT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MV\+OUDPxE1?	NFfUe5ZFVVOR	Mk\yS2k2OD1\|MjDuUS=>	M2jhb\|I1ODZ3N{Ox
HCC827	NIXHfY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MnjGglUh\|ryP	MWDEUXNQ	MVnHTVUxRTdibl2=	NYfCcWprOjRyNkW3N\|E>
HCC827-EPR	MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MXj+OUDPxE1?	MUXEUXNQ	MXfHTVUxRTJyIH7N	NG\5TZkzPDB4NUezNS=>
PC9	MlTQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MnHkglUh\|ryP	NGLxOmRFVVOR	NFHXeZVIUTVyPUK2JI5O	NGfZfFIzPDB4NUezNS=>
A431	M{n4WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MofpglUh\|ryP	NILZXWRFVVOR	NE[1SW1IUTVyPUW0O{BvVQ>?	NIHqfmIzPDB4NUezNS=>
NCI-H1299	NGKweXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M3j5SJ42KM7:TR?=	NYfjPHZjTE2VTx?=	NGDPR4xIUTVyPUSyO\|Uhdk1?	NXnzRlJ3OjRyNkW3N\|E>
NCI-H358	MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MVX+OUDPxE1?	NGe5U\|NFVVOR	MlTRS2k2OD1zOEC2JI5O	NETGb2ozPDB4NUezNS=>
PC-9 (exon 19del)	MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4SzO54yOCEQvF2=	NX\Z[FFDTE2VTx?=	NITJ[ZBKSzVyPUi0JI5O	NUC0OXBoOjZ3MUW0OlQ>
H3255 (L858R)	NX7pZVVQT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MUT+NVAh\|ryP	MnvESG1UVw>?	M1TG[2lEPTB;M{Wgcm0>	MlHwNlY2OTV2NkS=
PC-9ER (exon 19del+T790M)	MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NWnkSlJPhjFyIN88US=>	NWXLNoRTTE2VTx?=	NW\IdpdUUUN3ME2zO{BvVQ>?	NWC2UndXOjZ3MUW0OlQ>
H1975 (L858R+T790M)	NFHjOm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MlPwglExKM7:TR?=	NGDmXlZFVVOR	MVPJR\|UxRTJ\|IH7N	NUXSPHVyOjZ3MUW0OlQ>
BID007 (A763_Y764insFQEA)	NVPITolyT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M{jxbZ4yOCEQvF2=	MVzEUXNQ	NG\oWI5KSzVyPUGyO\|ghdk1?	MWWyOlUyPTR4NB?=
Ba/F3 (FQEA)	M1TDPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MlOwglExKM7:TR?=	NFfNVnJFVVOR	NHKz[YxKSzVyPU[3N{BvVQ>?	MVqyOlUyPTR4NB?=
Ba/F3 (HH)	M1XYUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXzmSoQ1hjFyIN88US=>	MY\EUXNQ	Mn3iTWM2OD1zN{OwJI5O	MVuyOlUyPTR4NB?=
Ba/F3 (ASV)	M2HXPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MkXuglExKM7:TR?=	MnToSG1UVw>?	M3fT[GlEPTB;NUK5NEBvVQ>?	NYKzdYhXOjZ3MUW0OlQ>
Ba/F3 (FQEA)	M2XiWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NX\vWoczhjFyIN88US=>	M4OyemROW09?	M{nLZ2lEPTB;Mk[yJI5O	NYH6Rm5WOjZ3MUW0OlQ>

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.
Animal Research:^[1]	Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. Dosages: ~50 mg/kg Administration: Oral gavage

References

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

Solubility (25°C)

In vitro


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

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

In vivo Formulation Calculator (Clear solution)

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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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