General
Preferred name
MK-2206
Synonyms
MK2206 ()
MK-2206 2HCl ()
MK-2206 dihydrochloride ()
MK 2206 dihydrochloride ()
MK-2206 (dihydrochloride) ()
MK-2206 (2HCl) ()
MK-2206 hydrochloride ()
MK-2206 (hydrochloride) ()
P&D ID
PD003288
CAS
1032349-93-1
1032350-13-2
1032349-77-1
Tags
available
drug candidate
Drug indication
Rectal adenocarcinoma
Nasopharyngeal carcinoma
Drug Status
investigational
Max Phase
Phase 2
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
MK-2206 is an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity .
(GtoPdb)
DESCRIPTION
inhibitor of AKT1
(Informer Set)
DESCRIPTION
MK-2206 is an allosteric inhibitor of Akt that prevents translocation of Akt to membranes. It is also an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B). It binds to and inhibits the activity of Akt in a non-ATP competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. It has potential antineoplastic activity. It exhibits anticancer chemotherapeutic activity in a variety of in vitro cancer models. It induces G1-phase cell cycle arrest in hepatocellular carcinoma cells, inhibits cell proliferation in non-small cell lung cancer cells, and inhibits proliferation in medullary thyroid cancer cells. It also inhibits tumor growth in animal models of nasopharyngeal cancer. It was developed by Merck Sharp & Dohme and in clinic phase 2 trials.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
MK-2206 hydrochloride is the hydrochloride form of MK-2206, which is an allosteric inhibitor of Akt and an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B). It has potential antineoplastic activity. It exhibits anticancer chemotherapeutic activity in a variety of in vitro cancer models. It inhibits tumor growth in animal models of nasopharyngeal cancer.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
440
Organisms
1
Compound Sets
22
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
Informer Set
Kinase Inhibitors (best-in-class)
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
38
Molecular Weight
407.17
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
3
Ring Count
6
Aromatic Ring Count
5
cLogP
4.24
TPSA
89.07
Fraction CSP3
0.16
Chiral centers
0.0
Largest ring
6.0
QED
0.47
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
AKT1
AKT1, AKT2
Akt
AKT2
AKT3
AKT1, AKT2, AKT3
Akt,Apoptosis related,Autophagy
Compound status
clinical
Pathway
PI3K signaling
Cytoskeletal Signaling
PI3K/Akt/mTOR signaling
Apoptosis
Autophagy
PI3K/Akt/mTOR
Kinase group
AGC
Targets
AKT1,AKT2,AKT3
Member status
member
MOA
Protein Kinase B (PKB/Akt) Inhibitors
Akt inhibitor
Solubility
10 mM in DMSO
Soluble in DMSO, water with 1 eq. of acid
Source data
