Home Protein Tyrosine Kinase EGFR inhibitor Rociletinib (CO-1686)

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Rociletinib (CO-1686) EGFR inhibitor

Cat.No.S7284

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. This compound is in Phase 2.
Rociletinib (CO-1686) EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 555.55

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Quality Control

Batch: Purity: 99.97%
99.97

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1975 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 62 nM
HCC827 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 187 nM
HCC827-EPR Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 180 nM
PC9 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of 211 nM
A431 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of >4331 nM
NCI-H1299 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of >2000 nM
NCI-H358 Kinase assay ~5 μM DMSO inhibits pEGFR with IC50 of >2000 nM
NCI-H1975 Growth inhibitory assay ~5 μM DMSO GI50=32 nM
HCC827 Growth inhibitory assay ~5 μM DMSO GI50=7 nM
HCC827-EPR Growth inhibitory assay ~5 μM DMSO GI50=20 nM
PC9 Growth inhibitory assay ~5 μM DMSO GI50=26 nM
A431 Growth inhibitory assay ~5 μM DMSO GI50=547 nM
NCI-H1299 Growth inhibitory assay ~5 μM DMSO GI50=4275 nM
NCI-H358 Growth inhibitory assay ~5 μM DMSO GI50=1806 nM
PC-9 (exon 19del) Growth inhibitory assay ~10 μM DMSO IC50=84 nM
H3255 (L858R) Growth inhibitory assay ~10 μM DMSO IC50=35 nM
PC-9ER (exon 19del+T790M) Growth inhibitory assay ~10 μM DMSO IC50=37 nM
H1975 (L858R+T790M) Growth inhibitory assay ~10 μM DMSO IC50=23 nM
BID007 (A763_Y764insFQEA) Growth inhibitory assay ~10 μM DMSO IC50=1278 nM
Ba/F3 (FQEA) Growth inhibitory assay ~10 μM DMSO IC50=673 nM
Ba/F3 (HH) Growth inhibitory assay ~10 μM DMSO IC50=1730 nM
Ba/F3 (ASV) Growth inhibitory assay ~10 μM DMSO IC50=5290 nM
Ba/F3 (FQEA) Growth inhibitory assay ~10 μM DMSO IC50=262 nM
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Solubility

In vitro
Batch:

DMSO : 100 mg/mL (180.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 555.55 Formula

C27H28F3N7O3

 Storage (From the date of receipt)
CAS No. 1374640-70-6 Download SDF Storage of Stock Solutions

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

Mechanism of Action

Targets/IC50/Ki
EGFR (L858R/T790M)
(Cell-free assay)
21.5 nM(Ki)
EGFR (wt)
(Cell-free assay)
303.3 nM(Ki)
In vitro
Rociletinib (CO-1686) inhibits p-EGFR with IC50 ranging from 62 to 187 nM in mutant EGFR–expressing cells, while it inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. This compound 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 exhibit signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors.
Kinase Assay
Inhibition Kinetics Studies
Recombinant human wild-type and T790M/L858R double mutant EGFR, both N-terminal GST-tagged, are used in the assay for Rociletinib (CO-1686). The Omnia continuous read assay is performed as described by the vendor.
In vivo
Rociletinib (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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02630186 Terminated
Non-small Cell Lung Cancer
Clovis Oncology Inc.|Genentech Inc.
 February 24 2016 Phase 1|Phase 2
NCT02580708 Terminated
Non-small Cell Lung Cancer
Clovis Oncology Inc.|Novartis Pharmaceuticals
 September 30 2015 Phase 1|Phase 2
NCT02147990 Terminated
Non-small Cell Lung Cancer
Clovis Oncology Inc.
 June 16 2014 Phase 2
NCT01526928 Terminated
Locally Advanced or Metastatic Non Small Cell Lung Cancer
Clovis Oncology Inc.
 March 27 2012 Phase 1|Phase 2

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