PI-3065 955977-50-1

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Molecular Weight: 506.64 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.

PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ.

In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor
growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, PI-3065 prolongs
survival and reduces the incidence of macroscopic metastases and Other
disease-associated pathologies.

Cell lines	4T1 cells
Concentrations	~10 μM
Incubation Time	48 hours
Method	Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ Inhibitors, then washing and MTS staining are carried out after 48 h culture.

Animal Study: [1]

Animal Models	Female WT BALB/c mice bearing 4T1 tumors
Formulation	0.5% methylcellulose with 0.2% Tween 80
Dosages	75 mg/kg, once daily
Administration	p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	506.64
Formula	C27H31FN6OS
CAS No.	955977-50-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Chemical Name	6-((4-(cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)-4-morpholinothieno[3,2-d]pyrimidine

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Product Categories : PI3K/Akt/mTOR > PI3K Inhibitor