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
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 13.0 nM [IC50]
Inhibitor
8504
 79.0 nM [IC50]
Inhibitor
8504
 61.0 nM [IC50]
Inhibitor
8504
 47.0 nM [IC50]
Inhibitor
8504
 25.0 nM [IC50]
Inhibitor
8504
 31.0 nM [IC50]
Inhibitor
8504
 31.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
5.62 μM
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19770380
330 mg/m² single, intravenous
dose: 330 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DANUSERTIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.31 μM
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19770380
400 mg/m² single, intravenous
dose: 400 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DANUSERTIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
38.5 μM × h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19770380
330 mg/m² single, intravenous
dose: 330 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DANUSERTIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
49.3 μM × h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19770380
400 mg/m² single, intravenous
dose: 400 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DANUSERTIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
33.3 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19770380
330 mg/m² single, intravenous
dose: 330 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DANUSERTIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
37.7 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/19770380
400 mg/m² single, intravenous
dose: 400 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
DANUSERTIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: 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
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
DLT: Febrile neutropenia, Fatigue...
Disc. AE: Hypertension...
Dose limiting toxicities:
Febrile neutropenia (grade 3-4, 12.5%)
Fatigue (grade 3, 12.5%)
AEs leading to
discontinuation/dose reduction:
Hypertension (grade 1, 12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
DLT: Febrile neutropenia, Mucositis...
Dose limiting toxicities:
Febrile neutropenia (8.3%)
Mucositis (8.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
DLT: Neutropenia, Fatigue...
Dose limiting toxicities:
Neutropenia (grade 4, 14.3%)
Fatigue (grade 3, 14.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 50%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
DLT: Febrile neutropenia, Mucositis...
Dose limiting toxicities:
Febrile neutropenia (33.3%)
Mucositis (grade 3, 16.7%)
Liver function test abnormal (grade 3, 16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
DLT: Neutropenia, Febrile neutropenia...
Dose limiting toxicities:
Neutropenia (14.3%)
Febrile neutropenia (14.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19770380
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
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
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/19825950
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP
110

P-gp
1741

BCRP
910

MRP4
290
BCRP
697

FMO3
77

P-gp
2052
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP
150
 no
P-gp
1932
 no
BCRP
985
 yes [IC50 7.49 uM]
MRP4
345
 yes [IC50 8.7 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
FMO3
77
 major
BCRP
697
 yes [Km 57.3 uM]
P-gp
2052
 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
BioSynth
J-502504
https://www.biosynth.com/en/products/life-science/other-biochemicals/products/J-502504
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
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
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
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
mcule
MCULE-1841941964
https://mcule.com/MCULE-1841941964/
mcule
MCULE-4216266063
https://mcule.com/MCULE-4216266063/
MedChem Express
HY-10179
https://www.medchemexpress.com/search.html?q=HY-10179&ft=&fa=&fp=
Molcore
MC103127
http://www.molcore.com/CatMC103127.html
Molnova
M16072
https://www.molnova.com/en/serch-list.html?keywords=M16072
MolPort
MolPort-009-679-390
https://www.molport.com/shop/molecule-link/MolPort-009-679-390
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
PubMed

PubMed

TitleDatePubMed
Abcg2 overexpression represents a novel mechanism for acquired resistance to the multi-kinase inhibitor Danusertib in BCR-ABL-positive cells in vitro.
2011-04-26
Optimizing combination therapies with existing and future CML drugs.
2010-08-23
Identification of Myb-binding protein 1A (MYBBP1A) as a novel substrate for aurora B kinase.
2010-04-16
Danusertib (formerly PHA-739358)--a novel combined pan-Aurora kinases and third generation Bcr-Abl tyrosine kinase inhibitor.
2010
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.
2009-11-01
Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors.
2009-10-20
Inhibitors of ABL and the ABL-T315I mutation.
2008
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.
2006-11-30
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 Wed Apr 02 09:42:23 GMT 2025
Edited
by admin
on Wed Apr 02 09:42:23 GMT 2025
Record UNII
M3X659D0FY
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
danusertib [INN]
Preferred Name English
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
Classification Tree Code System Code
NCI_THESAURUS C62556
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
NCI_THESAURUS C129825
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
Code System Code Type Description
EPA CompTox
DTXSID301002864
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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FDA UNII
M3X659D0FY
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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INN
8993
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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EVMPD
SUB96034
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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DRUG BANK
DB11778
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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SMS_ID
100000141656
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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PUBCHEM
11442891
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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ChEMBL
CHEMBL402548
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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CAS
827318-97-8
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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MESH
C523797
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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NCI_THESAURUS
C61587
Created by admin on Wed Apr 02 09:42:23 GMT 2025 , Edited by admin on Wed Apr 02 09:42:23 GMT 2025
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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
ACTIVE MOIETY
NIH
NCATS
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DISCLAIMER
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