TSAP0415914|cas 1292300-75-4|DC Chemicals

Cas No.:	1292300-75-4
Synonyms:	TASP-0415914
SMILES:	C1C(O)CN(C2N=C(C3SC(NC(C)=O)=NC=3C)ON=2)CC1
Formula:	C₁₃H₁₇N₅O₃S
M.Wt:	323.4
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
Target:	PI3Kγ:29 nM (IC50) Akt:294 nM (IC50)
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.
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].
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.

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TASP0415914