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1446700-26-0 (CO-1686 (hydrobromide))

1

Identification

CO-1686 (hydrobromide) CO-1686 (hydrobromide)
Name CO-1686 (hydrobromide)
Formula C27H29BrF3N7O3
MW 636.46
CAS No. 1446700-26-0
EINECS
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.[H]Br
Synonyms AVL-301 hydrobromide;CNX-419 hydrobromide; N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide hydrobromide
InChI InChI=1S/C27H28F3N7O3.BrH/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);1H
2

Introduction

Background Information

CO-1686 hydrobromide is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M (IC50=21 nM). IC50 value: 21.5±1.7 nM (EGFRL858R/T790M), 303.3 ± 26.7 nM (EGFRWT) in vitro: CO-1686 is a potent inhibitor of EGFR L858R/T790M kinase (kinact/Ki = (2.41 ± 0.30) x 105 M-1s-1) and is approximately 22-fold selective over WT EGFR (kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1). CO-1686 potently inhibited proliferation in the mutant-EGFR NSCLC cellswith GI50 values ranging from 7 - 32 nM. In comparison, the GI50 value for A431 cells, an epidermoid cell line that is driven by amplified WT EGFR(19), was 547 nM. Two cell lines expressing WT EGFR in the presence of an N- or KRAS mutation (NCI-H1299 and NCI-H358,respectively) were inhibited by CO-1686 at a concentration of 4275 and 1806 nM, respectively. in vivo: CO-1686 displays high oral bioavailability (65%) and a relatively long half-life of 2.6 hours when dosed at 20 mg/kg. Tumor-bearing mice were dosed orally once daily with CO-1686 as single agent and its effect on tumor growth was determined in several EGFR dependent xenograft models. Continuous oral dosing of CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models examined. At 100 mg/kg/day CO-1686 causs tumor regressions in two Erlotinib-resistant models expressing the L858R/T790M EGFR mutation, the NCI-H1975 cell line xenograft and the patient-derived lung tumor xenograft (PDX) LUM1868, while Erlotinib had no inhibitory effect on tumor growth. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000014042

Storage condition

Store in a tightly closed container, in a cool and dry place. by MedChemexpress Co., Ltd.

Solubility

DMSO:59mg/mL by CHEMSCENE, LLC
DMSO:59mg/mL by MedChemexpress Co., Ltd.
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Mechanism and Indication

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

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
CO-1686 (hydrobromide) Clovis Oncology Inc Non-small-cell lung cancer 2012/3/31 2015/9/30 Phase 2 Clinical
CO-1686 (hydrobromide) - No Development Reported
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Safety Data of CO-1686 (hydrobromide)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 10mg/USD150();50mg/USD400() USA
Aladdin 10mg/RMB1518();50mg/RMB4890() China
Apexbio Technology LLC 10mg/USD125();50mg/USD200();100mg/USD325() USA
BioVision, Inc., 5mg/USD145();25mg/USD575() USA
CHEMSCENE, LLC USA
Cayman Chemical Company 1mg/USD55();5mg/USD165();10mg/USD275() USA
MedChemexpress Co., Ltd. 5mg/USD50(In stock);10mg/USD80(In stock);50mg/USD165(In stock);100mg/USD255(In stock) USA
MedKoo Biosciences, Inc. 10mg/USD120();50mg/USD250();100mg/USD350();200mg/USD450();500mg/USD550();1g/USD850();2g/USD1450();5g/USD2850();10g/USD3650() USA
Selleck Chemicals LLC 10mg/USD297();50mg/USD970() USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
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Related Products

Other Forms of 1446700-26-0

Name CAS No Formula MW
CO-1686 1374640-70-6 C27H28F3N7O3 555.55

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 1374640-70-6 C27H28F3N7O3 555.55
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD 168393 194423-15-9 C17H13BrN4O 369.22
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanic acid 481-74-3 C15H10O4 254.24
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
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Route of Synthesis

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References

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More Information

CO-1686 (hydrobromide)

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