ETC-206 (AUM 001) - 98%, high purity , CAS No.1464151-33-4, Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2

Item Number
E413572
Grouped product items
SKUSizeAvailabilityPrice Qty
E413572-5mg
5mg
In stock
$98.90
E413572-10mg
10mg
In stock
$177.90
E413572-25mg
25mg
In stock
$400.90
E413572-50mg
50mg
In stock
$474.90
E413572-100mg
100mg
In stock
$771.90

MNK Inhibitors

Basic Description

SynonymsHY-112424 | F88611 | AUM001 | AUM-001 | s6658 | MND3WX2R7I | MS-27017 | 4-{6-[4-(morpholine-4-carbonyl)phenyl]imidazo[1,2- a]pyridin-3-yl}benzonitrile | UNII-MND3WX2R7I | tinodasertib [INN] | compound 48 [PMID: 29683667] | ETC-206 (AUM 001) | M03858 | AKO
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsETC-206 (AUM 001, ETC-1907206) is an orally available highly selective small-molecule MNK 1/2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2

Product Properties

ALogP3.016
Rotatable Bond3

Associated Targets(Human)

MKNK2 Tchem MAP kinase-interacting serine/threonine-protein kinase 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MKNK1 Tchem MAP kinase-interacting serine/threonine-protein kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MKNK2 Tchem MAP kinase signal-integrating kinase 2 (3518 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
K562 (73714 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
P3HR-1 (52 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PBMC (10003 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MKNK1 Tchem MAP kinase-interacting serine/threonine-protein kinase MNK1 (2071 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase; MEK1/2 (426 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DOHH-2 (352 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MKNK2 Tchem MAP kinase-interacting serine/threonine-protein kinase 1/2 (155 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TMD8 (415 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[6-[4-(morpholine-4-carbonyl)phenyl]imidazo[1,2-a]pyridin-3-yl]benzonitrile
INCHI InChI=1S/C25H20N4O2/c26-15-18-1-3-20(4-2-18)23-16-27-24-10-9-22(17-29(23)24)19-5-7-21(8-6-19)25(30)28-11-13-31-14-12-28/h1-10,16-17H,11-14H2
InChi Key FWRFPHJSGLYXTD-UHFFFAOYSA-N
Canonical SMILES C1COCCN1C(=O)C2=CC=C(C=C2)C3=CN4C(=NC=C4C5=CC=C(C=C5)C#N)C=C3
Isomeric SMILES C1COCCN1C(=O)C2=CC=C(C=C2)C3=CN4C(=NC=C4C5=CC=C(C=C5)C#N)C=C3
PubChem CID 71766360
Molecular Weight 408.45

Certificates

Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
K2229046Certificate of AnalysisOct 09, 2022 E413572
K2229047Certificate of AnalysisOct 09, 2022 E413572
K2229048Certificate of AnalysisOct 09, 2022 E413572
K2229054Certificate of AnalysisOct 09, 2022 E413572
K2229055Certificate of AnalysisOct 09, 2022 E413572

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 82 mg/mL (200.75 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility82
DMSO(mM) Max Solubility200.758966825805
Water(mg / mL) Max Solubility<1

Related Documents

References

1. Jin X, Yu R, Wang X, Proud CG, Jiang T.  (2021)  Progress in developing MNK inhibitors..  Eur J Med Chem,  219  (13): (113420).  [PMID:33892273] [10.1021/op500134e]
2. Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK et al..  (2018)  Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia..  J Med Chem,  61  (10): (4348-4369).  [PMID:29683667] [10.1021/op500134e]
3. Teneggi V, Novotny-Diermayr V, Lee LH, Yasin M, Yeo P, Ethirajulu K, Gan SBH, Blanchard SE, Nellore R, Umrani DN et al..  (2020)  First-in-Human, Healthy Volunteers Integrated Protocol of ETC-206, an Oral Mnk 1/2 Kinase Inhibitor Oncology Drug..  Clin Transl Sci,  13  (1): (57-66).  [PMID:31343094] [10.1021/op500134e]

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