PI-103 371935-74-9

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Molecular Weight: 348.36 PI-103 is a multi-targeted PI3K Inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.


PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and
rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. In blast cells, PI-103 inhibits leukemic proliferation, the
clonogenicity of leukemic progenitors and induces mitochondrial
Apoptosis, especially in the compartment containing leukemic stem cells.
PI-103 inhibits p110α >200-fold more potently than p110β.


PI-103
also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and
PIP3 in myotubes. PI-103 inhibits phosphorylation of Akt
with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103
completely protects animals from insulin-stimulated decline in blood
glucose. PI-103 has additive proapoptotic effects with etoposide in
blast cells and in immature leukemic cells.





When tumors reach 50-100 mm3, animals are randomized and
treated with vehicle or PI-103. PI-103 exhibits significant activity,
decreasing average tumor size by 4-fold after 18 days. Mice treated with PI-103 have no obvious signs of toxicity premorbidly
(based on body weight, food and water intake, activity, and general
exam) or at necropsy. Treated tumors display decreased levels of
phosphorylated Akt and S6, consistent with blockade of p110α and mTOR.
PI-103 treatment is cytostatic to glioma xenografts.

Enzyme Assays

Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.

Cell lines	U87MG cells
Concentrations	0.5 μM
Incubation Time	24 hours
Method	U87MG cells are treated with PI-103 for 24 hours. Cell death is quantified by colorimetric determination of LDH activity using a cytotoxicity detection kit. Percentage of cell death (mean of three 12-well plates per experimental point) is calculated [(experimental value- low control)/(high control -low control) × 100], where the low-control cells are DMSO treated and high-control cells are Triton treated (1% Triton X-100, 30 min, 37 °

Animal Study: [2]

Animal Models	6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
Formulation	50% DMSO
Dosages	5 mg/kg
Administration	Administered via i.p.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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)	348.36
Formula	C19H16N4O3
CAS No.	371935-74-9

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

Solubility (25°C) *	In vitro	DMSO	24 mg/mL (68.89 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	Phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-

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Product Categories : PI3K/Akt/mTOR > PI3K Inhibitor