U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C26H30N6O3
Molecular Weight 474.5548
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DANUSERTIB

SMILES

CO[C@@H](C(=O)N1CC2=C(C1)C(NC(=O)C3=CC=C(C=C3)N4CCN(C)CC4)=NN2)C5=CC=CC=C5

InChI

InChIKey=XKFTZKGMDDZMJI-HSZRJFAPSA-N
InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1

HIDE SMILES / InChI
Molecular Formula C26H30N6O3
Molecular Weight 474.5548
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including: https://repository.library.northeastern.edu/files/neu:657/fulltext.pdf | http://adisinsight.springer.com/drugs/800025382 | https://www.ncbi.nlm.nih.gov/pubmed/19770380

Danusertib is a serine/threonine kinase inhibitor of multiple kinases, including aurora-A, B, and C. It also inhibits several cancer related tyrosine kinases as well as Abl, Trk-a, fibroblast growth receptor-1 and Ret. Danusertib is in phase II trials for the treatment of solid tumours, prostate cancer and chronic myeloid leukemia (CML). The most frequently reported side effects were neutropenia, nausea, anorexia, fatigue, and diarrhea.

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 13.0 nM [IC50]
Inhibitor
8297
 79.0 nM [IC50]
Inhibitor
8297
 61.0 nM [IC50]
Inhibitor
8297
 47.0 nM [IC50]
Inhibitor
8297
 25.0 nM [IC50]
Inhibitor
8297
 31.0 nM [IC50]
Inhibitor
8297
 31.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Doses

Doses

DosePopulationAdverse events​
1000 mg/m2 1 times / 2 weeks multiple, intravenous
Highest studied dose
Dose: 1000 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 1000 mg/m2, 1 times / 2 weeks
Co-administed with::
Filgrastim(Treatment with G-CSF (5μg/kg/daily) was started 24 h after the end of danusertib infusion and continued for 10 days (from Day 3 to Day 12) ending 48 h before the next infusion.)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
DLT: Febrile neutropenia, Nausea...
Disc. AE: Azotemia...
Dose limiting toxicities:
Febrile neutropenia (14.3%)
Nausea (14.3%)
AEs leading to
discontinuation/dose reduction:
Azotemia (grade 1-2, 28.6%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
330 mg/m2 1 times / week multiple, intravenous
MTD
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
DLT: Fatigue, Febrile neutropenia...
Disc. AE: Hypertension...
Dose limiting toxicities:
Fatigue (grade 3, 12.5%)
Febrile neutropenia (grade 3-4, 12.5%)
AEs leading to
discontinuation/dose reduction:
Hypertension (grade 1, 12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
500 mg/m2 1 times / 2 weeks multiple, intravenous
MTD
Dose: 500 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 500 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 12
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
DLT: Febrile neutropenia, Mucositis...
Dose limiting toxicities:
Febrile neutropenia (8.3%)
Mucositis (8.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
750 mg/m2 1 times / 2 weeks multiple, intravenous
MTD
Dose: 750 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 750 mg/m2, 1 times / 2 weeks
Co-administed with::
Filgrastim(Treatment with G-CSF (5μg/kg/daily) was started 24 h after the end of danusertib infusion and continued for 10 days (from Day 3 to Day 12) ending 48 h before the next infusion.)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 6
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
330 mg/m2 1 times / week multiple, intravenous
Studied dose
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
DLT: Neutropenia, Fatigue...
Dose limiting toxicities:
Neutropenia (grade 4, 14.3%)
Fatigue (grade 3, 14.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
400 mg/m2 1 times / week multiple, intravenous
Studied dose
Dose: 400 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 400 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 50%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
580 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 580 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 580 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 6
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
DLT: Mucositis, Liver function test abnormal...
Dose limiting toxicities:
Mucositis (grade 3, 16.7%)
Liver function test abnormal (grade 3, 16.7%)
Febrile neutropenia (33.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
650 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 650 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 650 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
DLT: Neutropenia, Febrile neutropenia...
Dose limiting toxicities:
Neutropenia (14.3%)
Febrile neutropenia (14.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
AEs

AEs

AESignificanceDosePopulation
Febrile neutropenia 14.3%
DLT
1000 mg/m2 1 times / 2 weeks multiple, intravenous
Highest studied dose
Dose: 1000 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 1000 mg/m2, 1 times / 2 weeks
Co-administed with::
Filgrastim(Treatment with G-CSF (5μg/kg/daily) was started 24 h after the end of danusertib infusion and continued for 10 days (from Day 3 to Day 12) ending 48 h before the next infusion.)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Nausea 14.3%
DLT
1000 mg/m2 1 times / 2 weeks multiple, intravenous
Highest studied dose
Dose: 1000 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 1000 mg/m2, 1 times / 2 weeks
Co-administed with::
Filgrastim(Treatment with G-CSF (5μg/kg/daily) was started 24 h after the end of danusertib infusion and continued for 10 days (from Day 3 to Day 12) ending 48 h before the next infusion.)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Azotemia grade 1-2, 28.6%
Disc. AE
1000 mg/m2 1 times / 2 weeks multiple, intravenous
Highest studied dose
Dose: 1000 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 1000 mg/m2, 1 times / 2 weeks
Co-administed with::
Filgrastim(Treatment with G-CSF (5μg/kg/daily) was started 24 h after the end of danusertib infusion and continued for 10 days (from Day 3 to Day 12) ending 48 h before the next infusion.)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Hypertension grade 1, 12.5%
Disc. AE
330 mg/m2 1 times / week multiple, intravenous
MTD
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
Fatigue grade 3, 12.5%
DLT
330 mg/m2 1 times / week multiple, intravenous
MTD
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
Febrile neutropenia grade 3-4, 12.5%
DLT
330 mg/m2 1 times / week multiple, intravenous
MTD
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096, 5097
Febrile neutropenia 8.3%
DLT
500 mg/m2 1 times / 2 weeks multiple, intravenous
MTD
Dose: 500 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 500 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 12
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Mucositis 8.3%
DLT
500 mg/m2 1 times / 2 weeks multiple, intravenous
MTD
Dose: 500 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 500 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 12
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Fatigue grade 3, 14.3%
DLT, Disc. AE
330 mg/m2 1 times / week multiple, intravenous
Studied dose
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
Neutropenia grade 4, 14.3%
DLT, Disc. AE
330 mg/m2 1 times / week multiple, intravenous
Studied dose
Dose: 330 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 330 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
Neutropenia grade 4, 50%
DLT, Disc. AE
400 mg/m2 1 times / week multiple, intravenous
Studied dose
Dose: 400 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 400 mg/m2, 1 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
Page: p.5096
Febrile neutropenia 33.3%
DLT
580 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 580 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 580 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 6
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Liver function test abnormal grade 3, 16.7%
DLT
580 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 580 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 580 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 6
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Mucositis grade 3, 16.7%
DLT
580 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 580 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 580 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 6
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Febrile neutropenia 14.3%
DLT
650 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 650 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 650 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Neutropenia 14.3%
DLT
650 mg/m2 1 times / 2 weeks multiple, intravenous
Studied dose
Dose: 650 mg/m2, 1 times / 2 weeks
Route: intravenous
Route: multiple
Dose: 650 mg/m2, 1 times / 2 weeks
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
unhealthy, ADULT
n = 7
Health Status: unhealthy
Condition: cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 7
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Page: p.5, 6, 16
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP
111

P-gp
1461

BCRP
699

MRP4
204
BCRP
561

FMO3
67

P-gp
1537
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP
147
 no
P-gp
1650
 no
BCRP
773
 yes [IC50 7.49 uM]
MRP4
238
 yes [IC50 8.7 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
FMO3
67
 major
BCRP
561
 yes [Km 57.3 uM]
P-gp
1537
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY103127
https://www.001chemical.com/chem/search?q=DY103127
1PlusChem LLC
1P003PPD
https://www.1pchem.com/search?query=1P003PPD
AK Scientific
SYN1095
https://aksci.com/item_detail.php?cat=SYN1095
AK Scientific
X7370
https://aksci.com/item_detail.php?cat=X7370
ApexBio Technology
A4116
https://www.apexbt.com/catalogsearch/result/?q=A4116
AstaTech
A11611
http://astatechinc.com/CPSResult.php?CRNO=A11611
BLD Pharm
BD167193
http://www.bldpharm.com/search/Search.html?keyword=BD167193
BOC Sciences
827318-97-8
http://www.bocsci.com/description.asp?cas=827318-97-8
BioSynth
J-502504
https://www.biosynth.com/en/products/life-science/other-biochemicals/products/J-502504
Capot Chemical
16771
https://www.capotchem.com/search.do?q=16771
Cayman Chemical
18387
http://www.caymanchem.com/app/template/Product.vm/catalog/18387
Chem Scene
CS-0152
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0152
ChemShuttle
104825
https://www.chemshuttle.com/catalogsearch/result/?q=104825
Excenen
EX-A1599
http://www.excenen.com/searchresultlist.php?id=EX-A1599
Exclusive Chemistry
2352
http://www.exchemistry.com/chem-catalog/product-2352.html
KeyOrganics
AS-16243
http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-16243
Lab Seeker
SC-27938
http://www.labseeker.com/search.php?keywords=SC-27938&category=0
LabSeeker
SC-27938
http://www.labseeker.com/search.php?keywords=SC-27938&category=0
Matrix Scientific
120848
http://www.matrixscientific.com/120848.html
MedChem Express
HY-10179
https://www.medchemexpress.com/search.html?q=HY-10179&ft=&fa=&fp=
MolPort
MolPort-009-679-390
https://www.molport.com/shop/molecule-link/MolPort-009-679-390
Molcore
MC103127
http://www.molcore.com/CatMC103127.html
Molnova
M16072
https://www.molnova.com/en/serch-list.html?keywords=M16072
MuseChem
I004992
https://www.musechem.com/product/I004992.html
ShangHai Biochempartner
BCP01750
http://www.biochempartner.com/search_BCP01750
Toronto Research Chemicals
D185070
https://www.trc-canada.com/product-detail/?CatNum=D185070
Toronto Research Chemicals
D462135
https://www.trc-canada.com/product-detail/?CatNum=D462135
Wonderchem
WD045Y8
http://www.wonder-chem.com/search.html?text=WD045Y8
eMolecules
108761839
https://orderbb.emolecules.com/search/#?query=108761839
eMolecules
300421563
https://orderbb.emolecules.com/search/#?query=300421563
eMolecules
31229903
https://orderbb.emolecules.com/search/#?query=31229903
eMolecules
48860153
https://orderbb.emolecules.com/search/#?query=48860153
eMolecules
72977010
https://orderbb.emolecules.com/search/#?query=72977010
eNovation Chemicals
D395247
https://www.enovationchem.com/Products.asp?SEARCHTEXT=D395247&searchbtn.x=0&searchbtn.y=0
mcule
MCULE-1841941964
https://mcule.com/MCULE-1841941964/
mcule
MCULE-4216266063
https://mcule.com/MCULE-4216266063/
PubMed

PubMed

TitleDatePubMed
Inhibitors of ABL and the ABL-T315I mutation.
2008
A phase I dose-escalation study of danusertib (PHA-739358) administered as a 24-hour infusion with and without granulocyte colony-stimulating factor in a 14-day cycle in patients with advanced solid tumors.
2009 Nov 1
Identification of Myb-binding protein 1A (MYBBP1A) as a novel substrate for aurora B kinase.
2010 Apr 16
Optimizing combination therapies with existing and future CML drugs.
2010 Aug 23
Abcg2 overexpression represents a novel mechanism for acquired resistance to the multi-kinase inhibitor Danusertib in BCR-ABL-positive cells in vitro.
2011 Apr 26
Patents

Patents

07582628
1
20050032839
1
20060276471
1

Sample Use Guides

In Vivo Use Guide
330 mg/m(2) over 6 h on days 1, 8 and 15 or 500 mg/m(2) over 24 h on days 1 and 15, every 4 weeks.
Route of Administration: Intravenous
In Vitro Use Guide
PHA-739358 strongly inhibited proliferation of all human and murine leukemic and nonleukemic cell lines (BCR-ABL-positive and BCR-ABL-negative) tested, with IC50 values ranging from 0.05 μM to 3.06 μM
Substance Class Chemical
Created
by admin
on Sat Dec 16 17:51:49 UTC 2023
Edited
by admin
on Sat Dec 16 17:51:49 UTC 2023
Record UNII
M3X659D0FY
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DANUSERTIB
INN   WHO-DD  
INN  
Official Name English
N-(5-((2R)-2-METHOXY-2-PHENYLACETYL)-1,4,5,6-TETRAHYDROPYRROLO(3,4-C)PYRAZOL-3-YL)-4-(4-METHYLPIPERAZIN-1-YL)BENZAMIDE
Systematic Name English
PHA-739358
Code English
Danusertib [WHO-DD]
Common Name English
danusertib [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C62556
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
Code System Code Type Description
EPA CompTox
DTXSID301002864
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
FDA UNII
M3X659D0FY
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
INN
8993
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
EVMPD
SUB96034
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
DRUG BANK
DB11778
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
SMS_ID
100000141656
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
PUBCHEM
11442891
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
ChEMBL
CHEMBL402548
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
CAS
827318-97-8
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
MESH
C523797
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
NCI_THESAURUS
C61587
Created by admin on Sat Dec 16 17:51:50 UTC 2023 , Edited by admin on Sat Dec 16 17:51:50 UTC 2023
PRIMARY
Related Record Type Details
AURORA KINASE B
TARGET -> INHIBITOR
AURORA KINASE C
TARGET -> INHIBITOR
HIGH AFFINITY NERVE GROWTH FACTOR RECEPTOR
TARGET -> INHIBITOR
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET
TARGET -> INHIBITOR
TYROSINE-PROTEIN KINASE ABL1
TARGET -> INHIBITOR
FIBROBLAST GROWTH FACTOR RECEPTOR 1
TARGET -> INHIBITOR
AURORA KINASE A
TARGET -> INHIBITOR
Related Record Type Details
Structure of DANUSERTIB
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HHS VULNERABILITY DISCLOSURE
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