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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

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. (03/14/2014) Shelf life: >2 years if stored properly Drug formulation: This drug may be formulated in DMSO ......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
AbMole BioScience 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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