TASP0415914

Modify Date: 2025-08-31 12:03:45

TASP0415914 Structure
TASP0415914 structure
Common Name TASP0415914
CAS Number 1292300-75-4 Molecular Weight 323.37100
Density N/A Boiling Point N/A
Molecular Formula C13H17N5O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of TASP0415914


TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research[1].

 Names

Name N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide

 TASP0415914 Biological Activity

Description TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research[1].
Related Catalog
Target

PI3Kγ:29 nM (IC50)

Akt:294 nM (IC50)

In Vitro TASP0415914 (compound 8j) shows high metabolic stability in rat/human liver microsomes. TASP0415914 has no CYP inhibition up to 10 μM for CYP1A2, 2C9, 2C19, 2D6 and 3A4[1].
In Vivo TASP0415914 (compound 8j; 10-100 mg/kg; orally administration; twice daily; for 14 days) treatment suppressed the progression of the disease in a dose-dependent manner in a mouse collagen-induced arthritis (CIA) model[1]. Animal Model: Collagen-primed DBA/1 mice[1] Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg Administration: Orally administration; twice daily; for 14 days Result: Suppressed the progression of the disease in a dose-dependent manner.
References

[1]. Yusuke Oka, et al. Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases. Bioorg Med Chem. 2013 Dec 15;21(24):7578-83.

 Chemical & Physical Properties

Molecular Formula C13H17N5O3S
Molecular Weight 323.37100
Exact Mass 323.10500
PSA 132.62000
LogP 1.55900
InChIKey WFQFHKQIDOCQTL-UHFFFAOYSA-N
SMILES CC(=O)Nc1nc(C)c(-c2nc(N3CCCC(O)C3)no2)s1

 Safety Information

Hazard Codes Xi

 TASP0415914Bioassay

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Name: Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM af...
Source: ChEMBL
Target: Liver microsome
External Id: CHEMBL3097329
Name: Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM ...
Source: ChEMBL
Target: Liver microsome
External Id: CHEMBL3097330
Name: Mutagenicity in Escherichia coli WP2uvrA up to 5000 ug/ml by Ames test in absence of ...
Source: ChEMBL
Target: Escherichia coli
External Id: CHEMBL3097332
Name: Mutagenicity in Escherichia coli WP2uvrA up to 5000 ug/ml by Ames test in presence of...
Source: ChEMBL
Target: Escherichia coli
External Id: CHEMBL3097333
Name: Mutagenicity in Salmonella typhimurium TA100 up to 5000 ug/ml by Ames test in absence...
Source: ChEMBL
Target: Salmonella enterica subsp. enterica serovar Typhimurium
External Id: CHEMBL3097334
Name: Mutagenicity in Salmonella typhimurium TA98 up to 5000 ug/ml by Ames test in absence ...
Source: ChEMBL
Target: Salmonella enterica subsp. enterica serovar Typhimurium
External Id: CHEMBL3097336
Name: Mutagenicity in Salmonella typhimurium TA98 up to 5000 ug/ml by Ames test in presence...
Source: ChEMBL
Target: Salmonella enterica subsp. enterica serovar Typhimurium
External Id: CHEMBL3097337
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