DGIdb - MK-2206 Drug Record

MK-2206 chembl:CHEMBL1079175 Antineoplastic

Alternate Names:

MK-2206
MK2206
MK 2206
MK-2206 FREE BASE
pubchem.compound:24964624
chembl:CHEMBL1079175
chemidplus:1032349-93-1

Drug Info:

Pharmaceutical Developer	Merck
Source Reported Drug Name(s)	MK2206
Drug Class	AKT Allosteric Inhibitor
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
Notes	allosteric inhibitor
Drug Class	Kinase Inhibitors

(8 More Sources)

Publications:

Papadimitrakopoulou et al., 2016, The BATTLE-2 Study: A Biomarker-Integrated Targeted Therapy Study in Previously Treated Patients With Advanced Non-Small-Cell Lung Cancer., J. Clin. Oncol.
Hu et al., 2015, Combined Inhibition of Cyclin-Dependent Kinases (Dinaciclib) and AKT (MK-2206) Blocks Pancreatic Tumor Growth and Metastases in Patient-Derived Xenograft Models., Mol. Cancer Ther.
Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
Yap et al., 2011, First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors., J. Clin. Oncol.
Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.
Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
Vivanco et al., 2014, A kinase-independent function of AKT promotes cancer cell survival., Elife
Lara et al., 2015, Phase II Study of the AKT Inhibitor MK-2206 plus Erlotinib in Patients with Advanced Non-Small Cell Lung Cancer Who Previously Progressed on Erlotinib., Clin. Cancer Res.
Liu et al., 2011, The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathway., J. Clin. Endocrinol. Metab.
Khan et al., 2013, AKT is a therapeutic target in myeloproliferative neoplasms., Leukemia
Zook et al., 2017, Combination of Imatinib Mesylate and AKT Inhibitor Provides Synergistic Effects in Preclinical Study of Gastrointestinal Stromal Tumor., Clin. Cancer Res.
Doi et al., 2015, Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors., Cancer Chemother. Pharmacol.
Chlebowski et al., 1976, Metallophosphoryl and Apophosphoryl Alkaline Phosphatases., J. Biol. Chem.
Bland et al., 1976, Rapid infusion of sodium bicarbonate and albumin into high-risk premature infants soon after birth: a controlled, prospective trial., Am. J. Obstet. Gynecol.
Wisinski et al., 2016, Phase I Study of an AKT Inhibitor (MK-2206) Combined with Lapatinib in Adult Solid Tumors Followed by Dose Expansion in Advanced HER2+ Breast Cancer., Clin. Cancer Res.
Yahiaoui et al., 2017, PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors., PLoS ONE
Gupta et al., 2015, A Phase I Trial of Combined Ridaforolimus and MK-2206 in Patients with Advanced Malignancies., Clin. Cancer Res.
Ma et al., 2015, Multicenter phase II study of the AKT inhibitor MK-2206 in recurrent or metastatic nasopharyngeal carcinoma from patients in the mayo phase II consortium and the cancer therapeutics research group (MC1079)., Invest New Drugs
Sangai et al., 2012, Biomarkers of response to Akt inhibitor MK-2206 in breast cancer., Clin. Cancer Res.
Dogruluk et al., 2015, Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations., Cancer Res.

MK-2206 UBE2T

Interaction Score: 3.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MK-2206 EZH2

Interaction Score: 1.04

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Indication/Tumor Type colon cancer

Indication/Tumor Type pancreatic cancer

PMIDs:
26676756

Sources:
JAX-CKB
MK-2206 AKT3

Interaction Score: 0.83

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

Trial Name MK-2206

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial TTD
MK-2206 MPL

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type myelofibrosis

Response Type sensitive

Approval Status Preclinical

PMIDs:
23748344

Sources:
JAX-CKB
MK-2206 AKT2

Interaction Score: 0.66

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Trial Name MK-2206

Novel drug target Novel Target

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial
MK-2206 AKT1

Interaction Score: 0.56

Interaction Types & Directionality:

allosteric modulator

inhibitory allosteric modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

combination therapy MK2206 + Vemurafenib

Indication/Tumor Type melanoma

PMIDs:
25551293 24265152

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial
MK-2206 PTEN

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type follicular thyroid carcinoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
28178345 26187616 22025163 24265152 21289267

Sources:
JAX-CKB
MK-2206 HRAS

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
21289267

Sources:
JAX-CKB
MK-2206 KRAS

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy DZNep + MK2206

Indication/Tumor Type pancreatic cancer

Response Type sensitive

PMIDs:
27480147 25931518 26725216 22025163 26676756

Sources:
JAX-CKB
MK-2206 PIK3CA

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
26084990 22932669 26187616 21289267 26627007

Sources:
JAX-CKB
MK-2206 NRAS

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
21289267

Sources:
JAX-CKB
MK-2206 ERBB2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy KRIBB11 + MK2206

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type predicted – sensitive

PMIDs:
26104654 2605 2013 27026198

Sources:
JAX-CKB
MK-2206 KIT

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Imatinib + MK2206

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

PMIDs:
27370604

Sources:
JAX-CKB
MK-2206 BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MK2206 + Trametinib

Indication/Tumor Type melanoma

PMIDs:
24265152

Sources:
JAX-CKB
MK-2206 EGFR

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + MK2206

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
26106072

Sources:
JAX-CKB
MK-2206 SMAD3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MK-2206 AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

CancerCommons: MK2206
- Version: 25-July-2013
Alternate Names:

MK2206 PubChem Drug Name

46930998 PubChem Drug ID

MK2206 Drug Trade Name

Drug Info:

Drug Class AKT Allosteric Inhibitor

Source Reported Drug Name(s) MK2206

Pharmaceutical Developer Merck

Publications:
MyCancerGenome: MK-2206
- Version: 20-Jun-2017
Alternate Names:

MK-2206 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Publications:
TdgClinicalTrial: MK-2206
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: MK2206

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Lara et al., 2015, Phase II Study of the AKT Inhibitor MK-2206 plus Erlotinib in Patients with Advanced Non-Small Cell Lung Cancer Who Previously Progressed on Erlotinib., Clin. Cancer Res.

Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.

Yahiaoui et al., 2017, PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors., PLoS ONE

TALC: MK2206
- Version: 12-May-2016
Alternate Names:

MK2206 Primary Drug Name

MK2206 Drug Synonym

Drug Info:

Publications:
TTD: MK-2206
- Version: 2020.06.01
Alternate Names:

D0W3RW TTD Drug ID

Drug Info:

Publications:
DTC: MK-2206
- Version: 02-September-2020
Alternate Names:

CHEMBL1079175 ChEMBL Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1079175
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: MK2206
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: MK2206
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: MK2206
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1079175
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Approval Status	Preclinical - Cell line xenograft
Indication/Tumor Type	colon cancer
Indication/Tumor Type	pancreatic cancer

Mechanism of Interaction	Serine/threonine-protein kinase AKT inhibitor
Direct Interaction	yes
Trial Name	MK-2206

Indication/Tumor Type	myelofibrosis
Response Type	sensitive
Approval Status	Preclinical

Trial Name	MK-2206
Novel drug target	Novel Target
Mechanism of Interaction	Serine/threonine-protein kinase AKT inhibitor

Notes
combination therapy	MK2206 + Vemurafenib
Indication/Tumor Type	melanoma

Indication/Tumor Type	follicular thyroid carcinoma
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

combination therapy	DZNep + MK2206
Indication/Tumor Type	pancreatic cancer
Response Type	sensitive

Indication/Tumor Type	breast cancer
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	thyroid cancer
Response Type	sensitive
Approval Status	Preclinical - Cell culture

allosteric modulator
inhibitor (inhibitory)

allosteric modulator
inhibitor (inhibitory)

allosteric modulator
inhibitory allosteric modulator (inhibitory)
inhibitor (inhibitory)

combination therapy	KRIBB11 + MK2206
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	predicted – sensitive

combination therapy	Imatinib + MK2206
Indication/Tumor Type	gastrointestinal stromal tumor
Response Type	sensitive

combination therapy	Erlotinib + MK2206
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

MK2206	PubChem Drug Name
46930998	PubChem Drug ID
MK2206	Drug Trade Name

MK-2206 Drug Record

MK-2206 chembl:CHEMBL1079175 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info: Approval Status Preclinical - Cell line xenograft Indication/Tumor Type colon cancer Indication/Tumor Type pancreatic cancer

PMIDs: 26676756

Sources: JAX-CKB

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor Direct Interaction yes Trial Name MK-2206

PMIDs: None found

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type myelofibrosis Response Type sensitive Approval Status Preclinical

PMIDs: 23748344

Sources: JAX-CKB

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Trial Name MK-2206 Novel drug target Novel Target Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs: None found

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: allosteric modulator inhibitory allosteric modulator (inhibitory) inhibitor (inhibitory)

Interaction Info: Notes combination therapy MK2206 + Vemurafenib Indication/Tumor Type melanoma

PMIDs: 25551293 24265152

Sources: TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type follicular thyroid carcinoma Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 28178345 26187616 22025163 24265152 21289267

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell culture Response Type sensitive

PMIDs: 21289267

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy DZNep + MK2206 Indication/Tumor Type pancreatic cancer Response Type sensitive

PMIDs: 27480147 25931518 26725216 22025163 26676756

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type breast cancer Response Type sensitive Approval Status Preclinical

PMIDs: 26084990 22932669 26187616 21289267 26627007

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type thyroid cancer Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 21289267

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy KRIBB11 + MK2206 Indication/Tumor Type Her2-receptor positive breast cancer Response Type predicted – sensitive

PMIDs: 26104654 2605 2013 27026198

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Imatinib + MK2206 Indication/Tumor Type gastrointestinal stromal tumor Response Type sensitive

PMIDs: 27370604

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable combination therapy MK2206 + Trametinib Indication/Tumor Type melanoma

PMIDs: 24265152

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Erlotinib + MK2206 Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive

PMIDs: 26106072

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

CancerCommons: MK2206

Alternate Names: MK2206 PubChem Drug Name 46930998 PubChem Drug ID MK2206 Drug Trade Name

Drug Info: Drug Class AKT Allosteric Inhibitor Source Reported Drug Name(s) MK2206 Pharmaceutical Developer Merck

Publications:

MyCancerGenome: MK-2206

Alternate Names: MK-2206 Development Name

Drug Info: Drug Class Kinase Inhibitors Notes allosteric inhibitor

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Indication/Tumor Type colon cancer

Indication/Tumor Type pancreatic cancer

PMIDs:
26676756

Sources:
JAX-CKB

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

Direct Interaction yes

Trial Name MK-2206

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type myelofibrosis

Response Type sensitive

Approval Status Preclinical

PMIDs:
23748344

Sources:
JAX-CKB

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Trial Name MK-2206

Novel drug target Novel Target

Mechanism of Interaction Serine/threonine-protein kinase AKT inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

allosteric modulator

inhibitory allosteric modulator (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

combination therapy MK2206 + Vemurafenib

Indication/Tumor Type melanoma

PMIDs:
25551293 24265152

Sources:
TALC ClearityFoundationBiomarkers MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type follicular thyroid carcinoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
28178345 26187616 22025163 24265152 21289267

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
21289267

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy DZNep + MK2206

Indication/Tumor Type pancreatic cancer

Response Type sensitive

PMIDs:
27480147 25931518 26725216 22025163 26676756

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
26084990 22932669 26187616 21289267 26627007

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
21289267

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy KRIBB11 + MK2206

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type predicted – sensitive

PMIDs:
26104654 2605 2013 27026198

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Imatinib + MK2206

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

PMIDs:
27370604

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MK2206 + Trametinib

Indication/Tumor Type melanoma

PMIDs:
24265152

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + MK2206

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
26106072

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

MK2206 PubChem Drug Name

46930998 PubChem Drug ID

MK2206 Drug Trade Name

Drug Info:

Drug Class AKT Allosteric Inhibitor

Source Reported Drug Name(s) MK2206

Pharmaceutical Developer Merck

Alternate Names:

MK-2206 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

MK2206 Primary Drug Name

MK2206 Drug Synonym

Alternate Names:

D0W3RW TTD Drug ID

Alternate Names:

CHEMBL1079175 ChEMBL Drug ID