DGIdb - PD-0325901 Drug Record

PD-0325901 chembl:CHEMBL507361 Antineoplastic

Alternate Names:

PD-0325901

Drug Info:

Drug Class	Kinase Inhibitors

(2 More Sources)

Publications:

García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
Wang et al., 2016, KIT Exon 11 Codons 557-558 Deletion Mutation Promotes Liver Metastasis Through the CXCL12/CXCR4 Axis in Gastrointestinal Stromal Tumors., Clin. Cancer Res.
Teh et al., 2016, An In Vivo Reporter to Quantitatively and Temporally Analyze the Effects of CDK4/6 Inhibitor-Based Therapies in Melanoma., Cancer Res.
Gannon et al., 2016, Identification of an "Exceptional Responder" Cell Line to MEK1 Inhibition: Clinical Implications for MEK-Targeted Therapy., Mol. Cancer Res.
Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
Van Dort ME et al., 2015, Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor., Bioorg Med Chem
Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
Solit et al., 2006, BRAF mutation predicts sensitivity to MEK inhibition., Nature
Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
Haagensen et al., 2013, The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice., PLoS ONE
Kaufman et al., 2017, A Transcriptional Signature Identifies LKB1 Functional Status as a Novel Determinant of MEK Sensitivity in Lung Adenocarcinoma., Cancer Res.
Janakiraman et al., 2010, Genomic and biological characterization of exon 4 KRAS mutations in human cancer., Cancer Res.
Dhawan et al., 2016, Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling., Nature
Hunter et al., 2015, Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations., Mol. Cancer Res.
Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
Boasberg et al., 2011, Pilot study of PD-0325901 in previously treated patients with advanced melanoma, breast cancer, and colon cancer., Cancer Chemother. Pharmacol.
Soares et al., 2015, Dual PI3K/mTOR Inhibitors Induce Rapid Overactivation of the MEK/ERK Pathway in Human Pancreatic Cancer Cells through Suppression of mTORC2., Mol. Cancer Ther.
Simmons et al., 2012, Combination of a MEK inhibitor at sub-MTD with a PI3K/mTOR inhibitor significantly suppresses growth of lung adenocarcinoma tumors in Kras(G12D-LSL) mice., Cancer Chemother. Pharmacol.
Chen et al., 2014, Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations., Oncogene

PD-0325901 MAP2K1

Interaction Score: 1.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical

PMIDs:
26582713 26267534 25766633 23398453 10592235

Sources:
DTC MyCancerGenome JAX-CKB ChemblInteractions
PD-0325901 GNAQ

Interaction Score: 0.89

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AEB071 + PD-0325901

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
24141786

Sources:
JAX-CKB
PD-0325901 MAP2K2

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Direct Interaction yes

PMIDs:
23398453

Sources:
DTC MyCancerGenome ChemblInteractions
PD-0325901 KRAS

Interaction Score: 0.52

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
21325073 20570890 26582713 27556948 26037647 23934108 26267534 21516509 25673820 22684718 26272063

Sources:
JAX-CKB
PD-0325901 STK11

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
27821489

Sources:
JAX-CKB
PD-0325901 BRAF

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26272063 27488531 26573800 16273091 26267534

Sources:
JAX-CKB
PD-0325901 NRAS

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type no benefit

Approval Status Preclinical - Cell line xenograft

PMIDs:
27488531

Sources:
JAX-CKB
PD-0325901 KIT

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26936919

Sources:
JAX-CKB
PD-0325901 PIK3CA

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

PMIDs:
21325073 24339963 26272063

Sources:
JAX-CKB
PD-0325901 PTEN

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

PMIDs:
26272063

Sources:
JAX-CKB
PD-0325901 TP53

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Pdx & cell culture

Response Type predicted – sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
26272063

Sources:
JAX-CKB

MyCancerGenome: PD0325901
- Version: 20-Jun-2017
Alternate Names:

PD-0325901 Development Name

PD0325901 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
TTD: PD-0325901
- Version: 2020.06.01
Alternate Names:

D0K0YC TTD Drug ID

Drug Info:

Publications:

Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

DTC: PD-0325901

Version: 02-September-2020

Alternate Names:

CHEMBL507361 ChEMBL Drug ID

Drug Info:

Publications:

Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem

Van Dort ME et al., 2015, Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor., Bioorg Med Chem

JAX-CKB: PD-0325901

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Teh et al., 2016, An In Vivo Reporter to Quantitatively and Temporally Analyze the Effects of CDK4/6 Inhibitor-Based Therapies in Melanoma., Cancer Res.

García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.

Haagensen et al., 2013, The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice., PLoS ONE

ChemblInteractions: CHEMBL507361
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL507361
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	melanoma
Response Type	resistant
Approval Status	Preclinical

combination therapy	AEB071 + PD-0325901
Indication/Tumor Type	uveal melanoma
Response Type	sensitive

Mechanism of Interaction	Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
Direct Interaction	yes

combination therapy	MLN0128 + PD-0325901
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Indication/Tumor Type	gastrointestinal stromal tumor
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Evidence Type	Actionable
combination therapy	MLN0128 + PD-0325901
Indication/Tumor Type	colorectal cancer

Response Type	no benefit
combination therapy	MLN0128 + PD-0325901
Indication/Tumor Type	colorectal cancer

Approval Status	Preclinical - Pdx & cell culture
Response Type	predicted – sensitive
Approval Status	Preclinical - Cell line xenograft

PD-0325901	Development Name
PD0325901	Development Name

PD-0325901 Drug Record

PD-0325901 chembl:CHEMBL507361 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type melanoma Response Type resistant Approval Status Preclinical

PMIDs: 26582713 26267534 25766633 23398453 10592235

Sources: DTC MyCancerGenome JAX-CKB ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: combination therapy AEB071 + PD-0325901 Indication/Tumor Type uveal melanoma Response Type sensitive

PMIDs: 24141786

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor Direct Interaction yes

PMIDs: 23398453

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: combination therapy MLN0128 + PD-0325901 Indication/Tumor Type colorectal cancer Response Type sensitive

PMIDs: 21325073 20570890 26582713 27556948 26037647 23934108 26267534 21516509 25673820 22684718 26272063

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 27821489

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type resistant Approval Status Preclinical

PMIDs: 26272063 27488531 26573800 16273091 26267534

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type no benefit Approval Status Preclinical - Cell line xenograft

PMIDs: 27488531

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type gastrointestinal stromal tumor Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 26936919

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable combination therapy MLN0128 + PD-0325901 Indication/Tumor Type colorectal cancer

PMIDs: 21325073 24339963 26272063

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Response Type no benefit combination therapy MLN0128 + PD-0325901 Indication/Tumor Type colorectal cancer

PMIDs: 26272063

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Approval Status Preclinical - Pdx & cell culture Response Type predicted – sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 26272063

Sources: JAX-CKB

MyCancerGenome: PD0325901

Alternate Names: PD-0325901 Development Name PD0325901 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

TTD: PD-0325901

Alternate Names: D0K0YC TTD Drug ID

Drug Info:

Publications: Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

DTC: PD-0325901

Alternate Names: CHEMBL507361 ChEMBL Drug ID

Drug Info:

JAX-CKB: PD-0325901

Alternate Names:

Drug Info:

ChemblInteractions: CHEMBL507361

Alternate Names:

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL507361

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical

PMIDs:
26582713 26267534 25766633 23398453 10592235

Sources:
DTC MyCancerGenome JAX-CKB ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AEB071 + PD-0325901

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
24141786

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Direct Interaction yes

PMIDs:
23398453

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
21325073 20570890 26582713 27556948 26037647 23934108 26267534 21516509 25673820 22684718 26272063

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
27821489

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26272063 27488531 26573800 16273091 26267534

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type no benefit

Approval Status Preclinical - Cell line xenograft

PMIDs:
27488531

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26936919

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

PMIDs:
21325073 24339963 26272063

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

PMIDs:
26272063

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Pdx & cell culture

Response Type predicted – sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
26272063

Sources:
JAX-CKB

Alternate Names:

PD-0325901 Development Name

PD0325901 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

D0K0YC TTD Drug ID

Publications:

Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

Alternate Names:

CHEMBL507361 ChEMBL Drug ID