PI-3065

Cas No.:	955977-50-1
Chemical Name:	4-[6-[[4-(Cyclopropylmethyl)piperazin-1-yl]methyl]-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl]morpholine
Synonyms:	PI-3065;4-(6-((4-(Cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl)morpholine;PI3065;PI 3065;6-[[4-(Cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine;4-[6-[[4-(cyclopropylmethyl)piperazin-1-yl]methyl]-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl]morpholine;GTPL8242;AOB87791;BCP12801;s7623;PI30
SMILES:	S1C2C(=NC(C3=C(C([H])=C([H])C4=C3C([H])=C([H])N4[H])F)=NC=2C([H])=C1C([H])([H])N1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C1([H])C([H])([H])C1([H])[H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H]
Formula:	C27H31FN6Os
M.Wt:	506.6380
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR. IC50 value: 15 nM Target: p110δFor the detailed information of PI-3065, the solubility of PI-3065 in water, the solubility of PI-3065 in DMSO, the solubility of PI-3065 in PBS buffer, the animal experiment (test) of PI-3065, the cell expriment (test) of PI-3065, the in vivo, in vitro and clinical trial test of PI-3065, the EC50, IC50,and Affinity of PI-3065, Please contact DC Chemicals.
Target:	p110δ:5 nM (IC50) p110β:600 nM (IC50) p110α:910 nM (IC50)
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].
In Vitro:	PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110δ[1].
Animal Administration:	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.