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1375465-09-0 (CNX-2006)

1

Identification

CNX-2006 CNX-2006
Name CNX-2006
Formula C26H27F4N7O2
MW 545.53
CAS No. 1375465-09-0
EINECS
Smiles C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
Synonyms CNX2006;CNX 2006; N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide
InChI InChI=1S/C26H27F4N7O2/c1-3-23(38)33-16-5-4-6-17(11-16)34-24-20(26(28,29)30)13-31-25(36-24)35-21-8-7-18(12-22(21)39-2)32-19-14-37(15-19)10-9-27/h3-8,11-13,19,32H,1,9-10,14-15H2,2H3,(H,33,38)(H2,31,34,35,36)
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Introduction

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. IC50 value: <20 nM Target: Mutant EGFR CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR.

Background Information

A novel irreversible mutant-selective EGFR inhibitor ......by AOBIOUS INC
CNX-2006 is a novel irreversible epidermal growth factor receptor (EGFR) inhibitor. CNX-2006 exhibited specificity and potent in vitro and in vivo activity against T790M. In an in vitro resistance model, CNX-2006 significantly inhibited the emergence of resistant cells compared with erlotinib (1/24 vs 11/24, p = 0.0013). CNX-2006 selectively targets T790M, shows activity against other common and uncommon EGFR mutations, and does not select for resistance mediated by T790M. Additional studies are ongoing to elucidate mechanisms of acquired resistance to CNX-2006. ......by AbMole BioScience
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. ......by AdooQ BioScience, LLC
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clini ......by BOC Sciences
CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M. ......by MedChemexpress Co., Ltd.
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. ......by MedKoo Biosciences, Inc.
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. ......by Selleck Chemicals LLC
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Cell lines HEK293
Conditions ~1000 nM; 6 h
Method Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Nude mice
Dosage 25 mg/kg
Formulation 5% DMSO:15% Solutol HS15 in PBS
Administration i.p.
Source Selleck Chemicals LLC
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Physical and Chemical Properties

Appearance:White to gray Solid EBNumber:EB000014208

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.

Solubility

DMSO 100mg/ml; Water <1 mg/ml by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 100 mg/mL (183.3 mM); Ethanol29 mg/mL (53.15 mM); Water<1 mg/mL (<1 mM) by Selleck Chemicals LLC
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Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
CNX-2006 - No Development Reported
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Safety Data of CNX-2006

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
AdooQ BioScience, LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD126();10mg/USD228() USA
MedChemexpress Co., Ltd. 5mg/USD126();10mg/USD228() USA
MedKoo Biosciences, Inc. USA
Santa Cruz Biotechnology, Inc. 5mg/USD260() USA
Selleck Chemicals LLC 5mg/USD185(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD126();10mg/USD228() China
Target Molecule Corp. 2mg/USD66();5mg/USD99();10mg/USD172();25mg/USD333();50mg/USD441() USA
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Related Products

Other Forms of 1375465-09-0

Name CAS No Formula MW

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
CO-1686 1374640-70-6 C27H28F3N7O3 555.55
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
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Route of Synthesis

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References

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More Information

CNX-2006

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