General
Preferred name
AZD-4877
Synonyms
AZD4877 ()
Azd 4877 ()
P&D ID
PD046643
CAS
1176760-49-8
758722-49-5
Tags
available
drug candidate
Drug indication
Acute myeloid leukaemia
Acute myeloid leukemia
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity[1][2][3][4][5].
PRICE 955
DESCRIPTION AZD4877 was developed as an inhibitor of the kinesin spindle protein KIF11 (aka Eg5) and was investigated as a potential treatment for haematopoietic and solid malignancies. This compound is now included in AstaZeneca's Open Innovation Pharmacology Toolbox. (GtoPdb)
DESCRIPTION AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly. (BOC Sciences Bioactive Compounds)
DESCRIPTION AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC). (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
8
BOC Sciences Bioactive Compounds
azd4877-cas-1176760-49-8-item-84-457290
ChEMBL Drugs
CHEMBL1829433
DrugBank
DB11671
DrugMAP
DMFVL5J
Guide to Pharmacology
7708
MedChem Express Bioactive Compound Library
HY-13224
ReFrame library
TargetMol Bioactive Compound Library
T9682
External IDs
19
Properties
(calculated by RDKit )
Molecular Weight
503.24
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
9
Ring Count
4
Aromatic Ring Count
4
cLogP
4.71
TPSA
94.11
Fraction CSP3
0.36
Chiral centers
1.0
Largest ring
6.0
QED
0.36
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Apoptosis
Eg5
Kinesin
Pathway
Cell Cycle/DNA Damage
cytoskeleton
Cytoskeletal Signaling
Source data