AZD-4877

Investigational

Details

Stereochemistry	UNKNOWN
Molecular Formula	C28H33N5O2S
Molecular Weight	503.659
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)C(N(CCCN)C(=O)C1=CC=C(C)C=C1)C2=NC3=C(C(C)=NS3)C(=O)N2CC4=CC=CC=C4

InChI

InChIKey=SMFXSYMLJDHGIE-UHFFFAOYSA-N

InChI=1S/C28H33N5O2S/c1-18(2)24(32(16-8-15-29)27(34)22-13-11-19(3)12-14-22)25-30-26-23(20(4)31-36-26)28(35)33(25)17-21-9-6-5-7-10-21/h5-7,9-14,18,24H,8,15-17,29H2,1-4H3

HIDE SMILES / InChI

Molecular Formula	C28H33N5O2S
Molecular Weight	503.659
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23329066 | https://www.ncbi.nlm.nih.gov/pubmed/21494838

AZD4877 was developed by AstraZeneca as a potent inhibitor of the mitotic spindle kinesin, Eg5. AZD4877 participated in clinical trials phase I/II for patients with acute myeloid leukemia, the study was terminated due to lack of efficacy. In addition, the drug was studied in Phase II in patients with previously treated advanced urothelial cancer. However, limited clinical efficacy stops the further development of AZD4877 in urothelial cancer.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Kinesin-like protein KIF11 5 Target ID: P52732 Gene ID: 3832.0 Gene Symbol: KIF11 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21494838	Inhibitor 8297

PubMed

Title	Date	PubMed
Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.	2011 Oct 13	21899292
Phase I/II multicenter study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of AZD4877 in patients with refractory acute myeloid leukemia.	2012 Jun	21494838
Phase II study to assess the efficacy, safety and tolerability of the mitotic spindle kinesin inhibitor AZD4877 in patients with recurrent advanced urothelial cancer.	2013 Aug	23329066

Patents

Sample Use Guides

In Vivo Use Guide

AZD4877 25 mg was administered once-weekly for 3 weeks of each 4-week cycle

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 00:36:45 GMT 2023` Edited by `admin` on `Sat Dec 16 00:36:45 GMT 2023`
Record UNII	19ORU63E06
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

AZD-4877

Common Name

English

N-(3-AMINOPROPYL)-N-(1-(5-BENZYL-3-METHYL-4-OXO-4,5-DIHYDROISOTHIAZOLO(5,4-D)PYRIMIDIN-6-YL)-2-METHYLPROPYL)-4-METHYLBENZAMIDE

Systematic Name

English

AZD 4877 [WHO-DD]

Common Name

English

AZD4877

Code

English

Code System Code Type Description

FDA UNII

19ORU63E06