DGIdb - TANESPIMYCIN Drug Record

TANESPIMYCIN chembl:CHEMBL109480 Antineoplastic

Alternate Names:

CNF1010
TANESPIMYCIN
CNF-1010
KOS-953
NSC-330507
BMS-722782
17-AAG

Drug Info:

Drug Class	Small molecule inhibitor
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
Drug Categories	protein-serine-threonine kinases, antagonists & inhibitors
Drug Categories	hsp90 heat-shock proteins, antagonists & inhibitors

(8 More Sources)

Publications:

Li Z et al., 2014, Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors., Eur J Med Chem
Lauria A et al., 2013, Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening., J Med Chem
Ramsey DM et al., 2012, An Hsp90 modulator that exhibits a unique mechanistic profile., Bioorg Med Chem Lett
Li Z et al., 2014, Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors., Eur J Med Chem
Rodina A et al., 2007, Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer., Nat Chem Biol
Kunicki JB et al., 2011, Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90., Bioorg Med Chem Lett
O'Boyle NM et al., 2011, Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90., Bioorg Med Chem
Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature
Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.
Marsee et al., 2004, Inhibition of heat shock protein 90, a novel RET/PTC1-associated protein, increases radioiodide accumulation in thyroid cells., J. Biol. Chem.
Premkumar et al., 2006, Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells., Mol. Carcinog.
Naik R et al., 2012, Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors., J Med Chem
Jia et al., 2003, Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways., Blood

TANESPIMYCIN HSP90AB1

Interaction Score: 1.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Heat shock protein HSP90 inhibitor

Direct Interaction yes

Trial Name CNF1010

PMIDs:
25277067 23520985 22480433 25105924 17603540 21764310

Sources:
DTC TdgClinicalTrial DrugBank MyCancerGenome ChemblInteractions
TANESPIMYCIN HSP90AA2P

Interaction Score: 1.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
TANESPIMYCIN XIAP

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12738674

Sources:
NCI
TANESPIMYCIN HSP90AA1

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name CNF1010

Mechanism of Interaction Heat shock protein HSP90 inhibitor

PMIDs:
25277067 23520985 22480433 21920765 21764310

Sources:
DTC TdgClinicalTrial TTD DrugBank MyCancerGenome ChemblInteractions
TANESPIMYCIN CDK4

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16203796

Sources:
NCI
TANESPIMYCIN RET

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15302866

Sources:
NCI
TANESPIMYCIN HIF1A

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23153200

Sources:
DTC
TANESPIMYCIN PIK3CA

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16267832

Sources:
NCI
TANESPIMYCIN MET

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measuring downstream uPA-plasmin inhibition.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
TANESPIMYCIN MTOR

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TANESPIMYCIN TP53

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
26009011

Sources:
JAX-CKB
TANESPIMYCIN GMNN

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TANESPIMYCIN AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

KOS-953 Development Name

TANESPIMYCIN Generic Name

Drug Info:

Drug Class Small molecule inhibitor

Publications:
DrugBank: DB05134
- Version: 5.1.7
Alternate Names:

TANESPIMYCIN DrugBank Drug Name

75747-14-7 CAS Number

CHEMBL109480 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Categories amides

Publications:
TdgClinicalTrial: TANESPIMYCIN
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:
TdgClinicalTrial: CNF1010
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

NCI: 17-AAG

Version: 14-September-2017

Alternate Names:

C37899 NCI drug code

Drug Info:

Publications:

Premkumar et al., 2006, Synergistic interaction between 17-AAG and phosphatidylinositol 3-kinase inhibition in human malignant glioma cells., Mol. Carcinog.

Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.

Marsee et al., 2004, Inhibition of heat shock protein 90, a novel RET/PTC1-associated protein, increases radioiodide accumulation in thyroid cells., J. Biol. Chem.

DTC: TANESPIMYCIN

Version: 02-September-2020

Alternate Names:

CHEMBL109480 ChEMBL Drug ID

Drug Info:

Publications:

Li Z et al., 2014, Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors., Eur J Med Chem

Lauria A et al., 2013, Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening., J Med Chem

Ramsey DM et al., 2012, An Hsp90 modulator that exhibits a unique mechanistic profile., Bioorg Med Chem Lett

JAX-CKB: Tanespimycin
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature
TALC: TANESPIMYCIN
- Version: 12-May-2016
Alternate Names:

TANESPIMYCIN Primary Drug Name

TANESPIMYCIN Drug Generic Name

KOS-953 Drug Synonym

Drug Info:

Publications:
GuideToPharmacology: 223366084
- Version: 29-September-2020
Alternate Names:

TANESPIMYCIN GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Tanespimycin
- Version: 2020.06.01
Alternate Names:

D0SC2J TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL109480
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL109480
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Heat shock protein HSP90 inhibitor
Direct Interaction	yes
Trial Name	CNF1010

Novel drug target	Novel Target
Trial Name	CNF1010
Mechanism of Interaction	Heat shock protein HSP90 inhibitor

Details of the Assay for Interaction	Measuring downstream uPA-plasmin inhibition.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

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

TANESPIMYCIN	DrugBank Drug Name
75747-14-7	CAS Number
CHEMBL109480	ChEMBL ID

Drug Type	small molecule
Drug Groups	investigational
Drug Categories	amides

TANESPIMYCIN	Primary Drug Name
TANESPIMYCIN	Drug Generic Name
KOS-953	Drug Synonym

TANESPIMYCIN Drug Record

TANESPIMYCIN chembl:CHEMBL109480 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Heat shock protein HSP90 inhibitor Direct Interaction yes Trial Name CNF1010

PMIDs: 25277067 23520985 22480433 25105924 17603540 21764310

Sources: DTC TdgClinicalTrial DrugBank MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenome

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12738674

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Novel Target Trial Name CNF1010 Mechanism of Interaction Heat shock protein HSP90 inhibitor

PMIDs: 25277067 23520985 22480433 21920765 21764310

Sources: DTC TdgClinicalTrial TTD DrugBank MyCancerGenome ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16203796

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15302866

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23153200

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16267832

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Measuring downstream uPA-plasmin inhibition. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

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

PMIDs: 26009011

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

MyCancerGenome: TANESPIMYCIN

Alternate Names: KOS-953 Development Name TANESPIMYCIN Generic Name

Drug Info: Drug Class Small molecule inhibitor

Publications:

DrugBank: DB05134

Alternate Names: TANESPIMYCIN DrugBank Drug Name 75747-14-7 CAS Number CHEMBL109480 ChEMBL ID

Drug Info: Drug Type small molecule Drug Groups investigational Drug Categories amides

Publications:

TdgClinicalTrial: TANESPIMYCIN

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class small molecule FDA Approval not approved

Publications:

TdgClinicalTrial: CNF1010

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small molecule FDA Approval not approved

Publications:

NCI: 17-AAG

Alternate Names: C37899 NCI drug code

Drug Info:

DTC: TANESPIMYCIN

Alternate Names: CHEMBL109480 ChEMBL Drug ID

Drug Info:

JAX-CKB: Tanespimycin

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Heat shock protein HSP90 inhibitor

Direct Interaction yes

Trial Name CNF1010

PMIDs:
25277067 23520985 22480433 25105924 17603540 21764310

Sources:
DTC TdgClinicalTrial DrugBank MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenome

Interaction Types & Directionality:

n/a

PMIDs:
12738674

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name CNF1010

Mechanism of Interaction Heat shock protein HSP90 inhibitor

PMIDs:
25277067 23520985 22480433 21920765 21764310

Sources:
DTC TdgClinicalTrial TTD DrugBank MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
16203796

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15302866

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
23153200

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
16267832

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measuring downstream uPA-plasmin inhibition.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
26009011

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:

KOS-953 Development Name

TANESPIMYCIN Generic Name

Drug Info:

Drug Class Small molecule inhibitor

Alternate Names:

TANESPIMYCIN DrugBank Drug Name

75747-14-7 CAS Number

CHEMBL109480 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Categories amides

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

C37899 NCI drug code

Alternate Names:

CHEMBL109480 ChEMBL Drug ID

Publications:

Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature

Alternate Names:

TANESPIMYCIN Primary Drug Name

TANESPIMYCIN Drug Generic Name

KOS-953 Drug Synonym

Alternate Names:

TANESPIMYCIN GuideToPharmacology Ligand Name

Alternate Names:

D0SC2J TTD Drug ID