955977-50-1

955977-50-1 structure

Name: PI 3065
Chemical Name: Thieno[3,2-d]pyrimidine, 6-[[4-(cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)
CAS Number: 955977-50-1
Molecular Formula: C₂₇H₃₁FN₆OS
Molecular Weight: 506.638
Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) PI3K inhibitor
Create Date: 2016-05-22 06:54:22
Modify Date: 2024-01-02 16:33:31
PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.

Name	Thieno[3,2-d]pyrimidine, 6-[[4-(cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)
Synonyms	pi 3065 Thieno[3,2-d]pyrimidine, 6-[[4-(cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)- 6-{[4-(Cyclopropylmethyl)-1-piperazinyl]methyl}-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidine PI-3065

Description	PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
Related Catalog	Research Areas >> Inflammation/Immunology
Target	p110δ:5 nM (IC50) p110β:600 nM (IC50) p110α:910 nM (IC50)
In Vitro	PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110δ[1].
In Vivo	PI-3065 (75 mg/kg, p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice without obvious body weight loss[1].
Animal Admin	Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1×105 4T1 cells. Drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) is administered by oral gavage from day -1 (administered 12 h prior to tumour cell inoculation). Tumour growth is monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imaging platform. On day 35, mice are euthanized, tumours and peripheral organs extracted for in vitro luminescence measurement, followed by fixation in 4% PFA and H&E staining. KPC mice are allowed to develop advanced lesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI-3065 for a total of 14 days.
References	[1]. Ali K, et al. Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;509(7505):407-11.