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1374640-70-6 (CO-1686)



CO-1686 CO-1686
Name CO-1686
Formula C27H28F3N7O3
MW 555.55
CAS No. 1374640-70-6
Smiles C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
Synonyms AVL-301;CNX-419; N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide
InChI InChI=1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35)


CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM).

Background Information

An orally bioavailable irreversible EGFR inhibitor ......by AOBIOUS INC
Rociletinib, also known as CO-1686, is an irreversible tyrosine kinase inhibitor with a Ki of 21.5 nM for the EGFR L858R/T790M mutant and a Ki of 303.3 nM for wt EGFR. It inhibited the growth of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR, and it induced apoptosis. It also demonstrated in vivo anti-tumor activity in mice bearing NSCLC tumors with activating EGFR mutations. Walter A.O., et al. "Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC." Cancer Discov. 3: 1404-1415 (2013). The T790M mutation is the most common reason for acquired resistance to existing EGFR inhibitors in NSCLC. Rociletinib potently inhibited mutant EGFR L858R/T790M with an IC50 < 0.51nM. Rociletinib blocked the growth of T790M-positive NSCLC cells in vitro and in vivo. Walter A.O., et al. "CO-1686, a novel mutant-selective EGFR inhibitor, overcomes T790M mediated resistance in non-small cell lung cancer (NSCLC)." http://www.clovisoncology.com/assets/pdf/CO-1686/Clovis-Avila_AACR_2012_CO-1686_Poster_ClovisFINAL_27MAR12.pdf A phase I clinical trial in patients with EGFR mutated NSCLC demonstrated that rociletinib was well tolerated, and activity was observed in dose escalation cohorts. Sequist L.V., et al. "First-in-human evaluation of CO-1686, an irreversible, selective, and potent tyrosine kinase inhibitor of EGFR T790M." http://www.clovisoncology.com/files/CLVS_ASCO_2013_poster_CO1686_P1monotx_abstract2524.pdf ......by LC Laboratoies
CO-1686 is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. ......by MedChemexpress Co., Ltd.
CO-1686, also know as AVL-301, is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. EGFR inhibitor CO-1686 binds to and inhibits mutant forms of EGFR, including T790M, thereby leading to cell death of resistant tumor cells. Compared to other EGFR inhibitors, CO-1686 inhibits T790M, a secondary acquired resistance mutation, as well as other mutant EGFRs and may have therapeutic benefits in tumors with T790M-mediated resistance to other EGFR tyrosine kinase inhibitors. This agent shows minimal activity against wild-type EGFR, hence does not cause certain dose-limiting toxicities. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). Shelf life: >2 years if stored properly Drug formulation: This drug may be formulated in DMSO ......by MedKoo Biosciences, Inc.
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. ......by Selleck Chemicals LLC
CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM). ......by Target Molecule Corp.

Protocol(Only for Reference)

Cell Experiment

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)
Conditions ~10 μM; 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.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
Dosage ~50 mg/kg
Formulation DMSO: Solutol HS15: PBS (5:15:80; v:v:v)
Administration Oral gavage
Source Selleck Chemicals LLC

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000014043

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.


DMSO by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 100 mg/mL (180.0 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 1% DMSO+30% polyethylene glycol+1% Tween 8030 mg/mL by Selleck Chemicals LLC

Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area Cancer
Indications Non-small-cell lung cancer

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
CO-1686 Clovis Oncology Inc Non-small-cell lung cancer 2012/3/31 2015/9/30 Phase 2 Clinical
CO-1686 - Phase 3

Safety Data of CO-1686


Spectral Information


Suppliers List

Company Price and Availability Country/Region
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD60();10mg/USD96() USA
LC Laboratoies 10mg/USD82(In stock);25mg/USD119(In stock);50mg/USD169(In stock);100mg/USD259(In stock);200mg/USD435(In stock);500mg/USD815(In stock) USA
MedChemexpress Co., Ltd. 5mg/USD60();10mg/USD96() USA
MedKoo Biosciences, Inc. USA
Pure Chemistry Scientific Inc. 10mg/USD98(In stock) USA
Selleck Chemicals LLC 10mg/USD297(In stock);50mg/USD970(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD60();10mg/USD96() China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD800(In stock) CHINA
Target Molecule Corp. 10mg/USD77();50mg/USD156();100mg/USD247() USA

Related Products

Other Forms of 1374640-70-6

Name CAS No Formula MW
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46

Recommended Compounds in EGFR

Name CAS No Formula MW
Ginsenoside Rh2 78214-33-2 C36H62O8 622.87
Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 445.56
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 595.71
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 520.03
AZD-9291 1421373-65-0 C28H33N7O2 499.61
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
WHI-P180 211555-08-7 C16H15N3O3 297.31
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 483.36
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 489.54
BGB-102 807640-87-5 C22H25BrN4O2 457.36
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 491.34
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD168393 194423-15-9 C17H13BrN4O 369.2153
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanol 481-74-3 C15H10O4 254.2375
AG-1478 153436-53-4 C16H14ClN3O2 315.75
Mubritinib 366017-09-6 C25H23F3N4O2 468.47
AST-1306 (TsOH) 1050500-29-2 C31H26ClFN4O5S 621.08

Recommended Compounds in Same Indication

Name CAS No Formula MW
Crizotinib 877399-52-5 C21H22Cl2FN5O 450.34
AT-101 90141-22-3 C30H30O8 518.55
Dovitinib 405169-16-6 C21H21FN6O 392.43
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
Anamorelin (hydrochloride) 861998-00-7 C31H43ClN6O3 583.16
LY2603618 911222-45-2 C18H22BrN5O3 436.3
AT13387 912999-49-6 C24H31N3O3 409.52
Carboplatin 41575-94-4 C6H12N2O4Pt 371.25
Vandetanib (hydrochloride) 524722-52-9 C22H25BrClFN4O2 511.81
Dinaciclib 779353-01-4 C21H28N6O2 396.49
XL-647 781613-23-8 C24H25Cl2FN4O2 491.39
YM-155 781661-94-7 C20H19BrN4O3 443.29
Crenolanib 670220-88-9 C26H29N5O2 443.54
Ezatiostat 168682-53-9 C27H35N3O6S 529.65
Roscovitine 186692-46-6 C19H26N6O 354.45
Vandetanib (trifluoroacetate) 338992-53-3 C24H25BrF4N4O4 589.38
Anamorelin (Fumarate) 339539-92-3 C35H46N6O7 662.78
Vinorelbine 71486-22-1 C45H54N4O8 778.93

Route of Synthesis




More Information


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