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MK-2206 2HCl - ≥98%, high purity , CAS No.1032350-13-2, Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3

Moligand™
≥98%

CAS#: 1032350-13-2
Formula: C₂₅H₂₁N₅O·2HCl
Molecular Weight: 480.39
PubChem CID: 46930998

Item Number

M129684

Grouped product items
SKU	Size	Availability	Price
M129684-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$160.90
M129684-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$532.90
M129684-100mg	100mg	In stock	$959.90

View related series

AKT serine/threonine kinase 1 Allosteric modulator AKT serine/threonine kinase 2 Allosteric modulator AKT serine/threonine kinase 3 Allosteric modulator

Basic Description

Synonyms	1032350-13-2\|MK-2206 dihydrochloride\|MK-2206 2HCl\|MK2206\|8-(4-(1-Aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride\|8-[4-(1-AMINOCYCLOBUTYL)PHENYL]-9-PHENYL-1,2,4-TRIAZOLO[3,4-F][1,6]NAPHTHYRIDIN-3(2H)-ONE D
Specifications & Purity	≥98%
Storage Temp	Store at -20°C,Argon charged
Shipped In	Dry ice
Grade	Moligand™
Action Type	ALLOSTERIC MODULATOR
Mechanism of action	Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3
Product Description	MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain

Associated Targets

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 1 Activities

Discover Target: AKT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 1 Activities

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 1 Activities

Discover Target: AKT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride
INCHI	InChI=1S/C25H21N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31;;/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31);2*1H
InChi Key	HWUHTJIKQZZBRA-UHFFFAOYSA-N
Canonical SMILES	C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
Isomeric SMILES	C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
PubChem CID	46930998
Molecular Weight	480.39

PubChem CID

ChEBI

CAS Registry No.

ChEMBL Ligand

Reactome Reaction

Reactome Drug

Certificates

Certificate of Analysis(COA)

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2 results found

Lot Number	Certificate Type	Date	Item
H2203478	Certificate of Analysis	May 13, 2024	M129684
H1504074	Certificate of Analysis	Mar 16, 2023	M129684

Solubility

Soluble in DMSO (≥92 mg/ml), water (≥92 mg/ml), ethanol (≥1.8 mg/ml), and methanol.

Sensitivity

moisture sensitive

Melt Point(°C)

>225°C

References

1. Hirai H, Sootome H, Nakatsuru Y, Miyama K, Taguchi S, Tsujioka K, Ueno Y, Hatch H, Majumder PK, Pan BS et al.. (2010) MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo.. Mol Cancer Ther, 9 (7): (1956-67). [PMID:20571069]
2. Liu R, Liu D, Trink E, Bojdani E, Ning G, Xing M. (2011) The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathway.. J Clin Endocrinol Metab, 96 (4): (E577-85). [PMID:21289267]
3. Lin YH, Chen BY, Lai WT, Wu SF, Guh JH, Cheng AL, Hsu LC. (2015) The Akt inhibitor MK-2206 enhances the cytotoxicity of paclitaxel (Taxol) and cisplatin in ovarian cancer cells.. Naunyn Schmiedebergs Arch Pharmacol, 388 (1): (19-31). [PMID:25164962]
4. Holland WS, Chinn DC, Lara Jr PN, Gandara DR, Mack PC. (2015) Effects of AKT inhibition on HGF-mediated erlotinib resistance in non-small cell lung cancer cell lines.. J Cancer Res Clin Oncol, 141 (4): (615-26). [PMID:25323938]

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