AS-605240

Details

Stereochemistry	ACHIRAL
Molecular Formula	C12H7N3O2S
Molecular Weight	257.268
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=C1NC(=O)\C(S1)=C/C2=CC3=NC=CN=C3C=C2

InChI

InChIKey=SQWZFLMPDUSYGV-UXBLZVDNSA-N

InChI=1S/C12H7N3O2S/c16-11-10(18-12(17)15-11)6-7-1-2-8-9(5-7)14-4-3-13-8/h1-6H,(H,15,16,17)/b10-6+

HIDE SMILES / InChI

Molecular Formula	C12H7N3O2S
Molecular Weight	257.268
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22017414 | https://www.ncbi.nlm.nih.gov/pubmed/16127437

AS-605240 is a potent and selective phosphoinositide 3-kinase (PI3K) gamma inhibitor. It selectively inhibits PI3Kgamma enzymatic activity as well as PI3Kgamma-mediated signaling and chemotaxis in vitro and in vivo. It also has peripheral activity versus other PI3K isoforms. AS-605240 did not progress to clinical development although it had been described as a development candidate.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
PI3-kinase p110-alpha subunit 41 Target ID: CHEMBL4005 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16127437	Inhibitor 8504	0.06 µM [IC50]
PI3-kinase p110-delta subunit 43 Target ID: CHEMBL3130 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16127437	Inhibitor 8504	0.3 µM [IC50]
PI3-kinase p110-gamma subunit 32 Target ID: CHEMBL3267 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16127437	Inhibitor 8504	0.008 µM [IC50]
PI3-kinase p110-beta subunit 31 Target ID: CHEMBL3145 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16127437	Inhibitor 8504	0.27 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Unknown 2596

PubMed

Title	Date	PubMed
The effect of pharmacological PI3Kγ inhibitor on eotaxin-induced human eosinophil functions.	2014-04	24333185
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.	2013-04-15	23398362
Selective PI3Kδ inhibitors, a review of the patent literature.	2011-11	22017414
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.	2011-10-30	22037377
Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.	2005-09	16127437

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

The effect of AS605240, synthetic phosphoinositide 3-kinase gamma inhibitor on eotaxin-induced adhesion, chemotaxis, and degranulation was studied on human peripheral blood eosinophils. Although AS605240 did not affect the eosinophil spontaneous apoptosis, eotaxin-induced chemotaxis, adhesion to intracellular adhesion molecule-1 coated plate, and eosinophil-derived neurotoxin release were inhibited by AS605240. AS605240 also inhibited the eotaxin-induced extracellular signal-regulated kinase 1/2 phosphorylation without down-regulation of surface C-C motif chemokine receptor 3 expression.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:30:40 GMT 2025` Edited by `admin` on `Mon Mar 31 21:30:40 GMT 2025`
Record UNII	8GRW063UT7
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AS-605240

Common Name

English

AS 605240

Preferred Name

English

5-(QUINOXALIN-6-YLMETHYLENE)THIAZOLIDINE-2,4-DIONE

Systematic Name

English

PI 3-KG INHIBITOR

Common Name

English

(E)-5-(QUINOXALIN-6-YLMETHYLENE)THIAZOLIDINE-2,4-DIONE

Systematic Name

English

2,4-THIAZOLIDINEDIONE, 5-(6-QUINOXALINYLMETHYLENE)-

Systematic Name

English

AS605240

Common Name

English

Code System Code Type Description

CHEBI

45302