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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	NWi5cI17U2mwYYPlJIF{e2G7	NEXIXZR,PSEQvF2=	MX;EUXNQ	NHTiXotqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhPjJibl2=	MXiyOFA3PTd\|MR?=
HCC827	MlHCT4lv[XOnIHHzd4F6	M{XpSp42KM7:TR?=	NFXuZphFVVOR	Mn7zbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5PyCwTR?=	NITpWmkzPDB4NUezNS=>
HCC827-EPR	NFfYNmpMcW6jc3WgZZN{[Xl?	MofBglUh\|ryP	NUCyXXlVTE2VTx?=	MkXwbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFE5OCCwTR?=	NETUSowzPDB4NUezNS=>
PC9	MULLbY5ie2ViYYPzZZk>	MYP+OUDPxE1?	MVLEUXNQ	MX;pcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gNlEyKG6P	MUmyOFA3PTd\|MR?=
A431	NGjhTplMcW6jc3WgZZN{[Xl?	NIHv[JF,PSEQvF2=	MmH4SG1UVw>?	MWjpcohq[mm2czDwSWdHWiC5aYToJGlEPTBib3[gQlQ{OzFibl2=	NXjUT2J2OjRyNkW3N\|E>
NCI-H1299	NV7Gc2lKU2mwYYPlJIF{e2G7	NHvUcnl,PSEQvF2=	NEXVd2ZFVVOR	NG\LO4pqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0>	NF;RfpUzPDB4NUezNS=>
NCI-H358	NFXZe5ZMcW6jc3WgZZN{[Xl?	MWf+OUDPxE1?	M1LhWGROW09?	NVX5O4s4cW6qaXLpeJMheEWJRmKge4l1cCCLQ{WwJI9nKD5{MECwJI5O	NVHpZ5hiOjRyNkW3N\|E>
NCI-H1975	NIX5fGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NW\Q[WplhjVizszN	NXTVU5FjTE2VTx?=	NXjHTodMT0l3ME2zNkBvVQ>?	NITORoIzPDB4NUezNS=>
HCC827	M4fWTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MYD+OUDPxE1?	NHL0VJVFVVOR	NIn0UXRIUTVyPUegcm0>	NHHNdpQzPDB4NUezNS=>
HCC827-EPR	MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MofDglUh\|ryP	NID3eXBFVVOR	M4nacGdKPTB;MkCgcm0>	MUOyOFA3PTd\|MR?=
PC9	MmnSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NVvlNGgzhjVizszN	Ml;3SG1UVw>?	MmH4S2k2OD1{NjDuUS=>	NGKzSFkzPDB4NUezNS=>
A431	NXPYWYV1T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M4Cyb542KM7:TR?=	MkjKSG1UVw>?	MUDHTVUxRTV2NzDuUS=>	M3rKWFI1ODZ3N{Ox
NCI-H1299	MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWf+OUDPxE1?	MWTEUXNQ	M3;v[2dKPTB;NEK3OUBvVQ>?	MXuyOFA3PTd\|MR?=
NCI-H358	MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MkTBglUh\|ryP	MYrEUXNQ	MUTHTVUxRTF6ME[gcm0>	MlPuNlQxPjV5M{G=
PC-9 (exon 19del)	M3vIWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MnjBglExKM7:TR?=	MnvzSG1UVw>?	NXT4S2VXUUN3ME24OEBvVQ>?	M1fYclI3PTF3NE[0
H3255 (L858R)	NIe1W4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MX3+NVAh\|ryP	MVLEUXNQ	NH\rSmFKSzVyPUO1JI5O	NVyxc45VOjZ3MUW0OlQ>
PC-9ER (exon 19del+T790M)	M4PnXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M2qzPZ4yOCEQvF2=	NILaO\|dFVVOR	NHjFXIdKSzVyPUO3JI5O	NXj4R4Q{OjZ3MUW0OlQ>
H1975 (L858R+T790M)	MoPkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MknqglExKM7:TR?=	M2\kSmROW09?	M1;EWGlEPTB;MkOgcm0>	NHvrdWEzPjVzNUS2OC=>
BID007 (A763_Y764insFQEA)	MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MkHiglExKM7:TR?=	MVXEUXNQ	MonzTWM2OD1zMke4JI5O	MUWyOlUyPTR4NB?=
Ba/F3 (FQEA)	NWHPXY56T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MYT+NVAh\|ryP	M2H4OGROW09?	MYrJR\|UxRTZ5MzDuUS=>	MVSyOlUyPTR4NB?=
Ba/F3 (HH)	MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MmrIglExKM7:TR?=	MYHEUXNQ	M2DTZ2lEPTB;MUezNEBvVQ>?	M33NdlI3PTF3NE[0
Ba/F3 (ASV)	MoH2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1zGbZ4yOCEQvF2=	MoPQSG1UVw>?	NGCxfGFKSzVyPUWyPVAhdk1?	MmjpNlY2OTV2NkS=
Ba/F3 (FQEA)	NFrxVnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	Ml:0glExKM7:TR?=	MWTEUXNQ	NWXwcIZbUUN3ME2yOlIhdk1?	MXmyOlUyPTR4NB?=

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 2022-08-01)

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