DGIdb - GEDATOLISIB Drug Record

GEDATOLISIB chembl:CHEMBL592445 Antineoplastic

Alternate Names:

PKI-587
PF-05212384
GEDATOLISIB

Drug Info:

Notes	pan-PI3K inhibitor, catalytic, dual PI3K/mTOR inhibitor
Drug Class	Kinase Inhibitors

(6 More Sources)

Publications:

Venkatesan et al., 2010, Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor., J. Med. Chem.
Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
Tang et al., 2008, Dual MET-EGFR combinatorial inhibition against T790M-EGFR-mediated erlotinib-resistant lung cancer., Br. J. Cancer
Van Schaeybroeck et al., 2006, Chemotherapy-induced epidermal growth factor receptor activation determines response to combined gefitinib/chemotherapy treatment in non-small cell lung cancer cells., Mol. Cancer Ther.
Mohan et al., 2015, MEK Inhibitor PD-0325901 Overcomes Resistance to PI3K/mTOR Inhibitor PF-5212384 and Potentiates Antitumor Effects in Human Head and Neck Squamous Cell Carcinoma., Clin. Cancer Res.
D'Amato et al., 2014, The dual PI3K/mTOR inhibitor PKI-587 enhances sensitivity to cetuximab in EGFR-resistant human head and neck cancer models., Br. J. Cancer
Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis
Hollestelle et al., 2007, Phosphatidylinositol-3-OH kinase or RAS pathway mutations in human breast cancer cell lines., Mol. Cancer Res.
Song et al., 2015, Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1-Rearranged Non-Small Cell Lung Cancer., Clin. Cancer Res.
Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
Zhao et al., 2004, PTEN inhibits cell proliferation and induces apoptosis by downregulating cell surface IGF-IR expression in prostate cancer cells., Oncogene
Abazeed et al., 2013, Integrative radiogenomic profiling of squamous cell lung cancer., Cancer Res.
Acquaviva et al., 2012, Targeting KRAS-mutant non-small cell lung cancer with the Hsp90 inhibitor ganetespib., Mol. Cancer Ther.
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.

GEDATOLISIB AKT1S1

Interaction Score: 1.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20166697

Sources:
DTC
GEDATOLISIB CRTC1

Interaction Score: 0.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
GEDATOLISIB CRTC2

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
GEDATOLISIB VHL

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal carcinoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
21325073

Sources:
JAX-CKB
GEDATOLISIB PIK3R4

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome MyCancerGenomeClinicalTrial
GEDATOLISIB PIK3R6

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome MyCancerGenomeClinicalTrial
GEDATOLISIB PIK3R1

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB PIK3R3

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB PIK3R5

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB NOS3

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20166697

Sources:
DTC
GEDATOLISIB STK11

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
21325073

Sources:
JAX-CKB
GEDATOLISIB PIK3R2

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB PIK3CA

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25977343 24823695 24042735 21325073 17314276 25688157

Sources:
ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB PIK3C2G

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
GEDATOLISIB PIK3C2A

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
GEDATOLISIB PIK3C2B

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
GEDATOLISIB PIK3C3

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
GEDATOLISIB NRAS

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
12068308 21325073

Sources:
JAX-CKB
GEDATOLISIB PIK3CD

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB KRAS

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical - Cell culture

PMIDs:
17314276 24042735 23012248 12068308 21325073 25688157 25673820

Sources:
JAX-CKB
GEDATOLISIB PIK3CB

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial
GEDATOLISIB PTEN

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
14737113 21325073 17314276

Sources:
ClearityFoundationBiomarkers JAX-CKB
GEDATOLISIB MTOR

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor

PMIDs:
20166697

Sources:
DTC MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial TTD
GEDATOLISIB PIK3CG

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial TTD
GEDATOLISIB BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colon cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
17314276 21325073 24042735

Sources:
JAX-CKB
GEDATOLISIB AKT1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20166697

Sources:
DTC
GEDATOLISIB EGFR

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gedatolisib + Neratinib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
21325073 19238632 16731747

Sources:
JAX-CKB
GEDATOLISIB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
17314276 21325073

Sources:
JAX-CKB
GEDATOLISIB TP53

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
23980093 21325073

Sources:
JAX-CKB

MyCancerGenome: PKI-587
- Version: 20-Jun-2017
Alternate Names:

PKI-587 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes pan-PI3K inhibitor, catalytic, dual PI3K/mTOR inhibitor

Publications:

DTC: GEDATOLISIB

Version: 02-September-2020

Alternate Names:

CHEMBL592445 ChEMBL Drug ID

Drug Info:

Publications:

Venkatesan et al., 2010, Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor., J. Med. Chem.

JAX-CKB: PF-05212384

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.

Abazeed et al., 2013, Integrative radiogenomic profiling of squamous cell lung cancer., Cancer Res.

Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis

JAX-CKB: Gedatolisib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.

Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis

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.

TTD: PF-05212384
- Version: 2020.06.01
Alternate Names:

D0D8JB TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL592445
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: PKI-587
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: PKI-587
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: PF-05212384
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL592445
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	renal carcinoma
Response Type	decreased response
Approval Status	Preclinical

Mechanism of Interaction	PI3-kinase class I inhibitor
Direct Interaction	yes

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

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

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

Direct Interaction	yes
Mechanism of Interaction	Serine/threonine-protein kinase mTOR inhibitor

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

combination therapy	Gedatolisib + Neratinib
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

GEDATOLISIB Drug Record

GEDATOLISIB chembl:CHEMBL592445 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20166697

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type renal carcinoma Response Type decreased response Approval Status Preclinical

PMIDs: 21325073

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20166697

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive Approval Status Preclinical

PMIDs: 21325073

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Her2-receptor positive breast cancer Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 25977343 24823695 24042735 21325073 17314276 25688157

Sources: ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type decreased response Approval Status Preclinical

PMIDs: 12068308 21325073

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PI3-kinase class I inhibitor Direct Interaction yes

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
20166697

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal carcinoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
21325073

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PI3-kinase class I inhibitor

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
20166697

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
21325073

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25977343 24823695 24042735 21325073 17314276 25688157

Sources:
ClearityFoundationBiomarkers MyCancerGenome JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
12068308 21325073

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical - Cell culture

PMIDs:
17314276 24042735 23012248 12068308 21325073 25688157 25673820

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PI3-kinase class I inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
14737113 21325073 17314276

Sources:
ClearityFoundationBiomarkers JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase mTOR inhibitor