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1292300-75-4

1292300-75-4 structure
1292300-75-4 structure
  • Name: TASP0415914
  • Chemical Name: N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide
  • CAS Number: 1292300-75-4
  • Molecular Formula: C13H17N5O3S
  • Molecular Weight: 323.37100
  • Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
  • Create Date: 2018-02-02 10:50:07
  • Modify Date: 2024-01-30 21:26:31
  • 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].

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

Molecular Formula C13H17N5O3S
Molecular Weight 323.37100
Exact Mass 323.10500
PSA 132.62000
LogP 1.55900
Hazard Codes Xi