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PI103

(CAS No:371935-74-9)
PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
CAS No:371935-74-9
Molecular Weight(MW):348.36
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 371935-74-9
Molecular formula(MF) C19H16N4O3
Molecular Weight(MW): 348.36
Alias 3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol hydrochloride
Solubility
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
Biological Activity
Description PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
Features The first potent, synthetic mTOR inhibitor.
Targets
p110α [3]
(Cell-free assay)		 p110β [3]
(Cell-free assay)		 p110δ [3]
(Cell-free assay)		 p110γ [3]
(Cell-free assay)		 DNA-PK [3]
(Cell-free assay)
2 nM 3 nM 3 nM 15 nM 23 nM
In vitro

PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. [1] PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. [2] 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. [2] 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. [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-BE Growth Inhibition Assay 0-8 μM 24/48/72 h induces time- and concentration-dependent inhibition on NB cell growth 26224681
SH-SY5Y Growth Inhibition Assay 0-8 μM 24/48/72 h induces time- and concentration-dependent inhibition on NB cell growth 26224681
SH-SY5Y  Apoptosis Assay 1 μM 0.5-24 h sensitizes neuroblastoma cells to doxorubicin-induced apoptosis 26224681
G 35 SC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 38 SC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 40 SC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 35 DC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 38 DC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
G 40 DC Growth Inhibition Assay 0.05-20 μM 24/72 h DMSO inhibits cell viability dose and time dependently 26121251
RD Apoptosis Assay 1/1.5/2 μM 72 h induces apoptosis combined with GANT61 25749378
TE381.T Apoptosis Assay 1/1.5/2 μM 72 h induces apoptosis combined with GANT61 25749378
RMS13 Apoptosis Assay 1/1.5/2 μM 72 h induces apoptosis combined with GANT61 25749378
RH30  Apoptosis Assay 1/1.5/2 μM 72 h induces apoptosis combined with GANT61 25749378
VJ Apoptosis Assay 1/1.5/2 μM 72 h induces apoptosis combined with GANT61 25749378
HS578T Cell Viability Assay 0-3 μM 72 h inhibits cell viability dose dependently 25721419
BT549 Cell Viability Assay 0-3 μM 72 h inhibits cell viability dose dependently 25721419
MDA-MB-231 Cell Viability Assay 0-3 μM 72 h inhibits cell viability dose dependently 25721419
MDA-MB-468 Cell Viability Assay 0-3 μM 72 h inhibits cell viability dose dependently 25721419
MDA-MB-436 Cell Viability Assay 0-3 μM 72 h inhibits cell viability dose dependently 25721419
SUM149PT Cell Viability Assay 0-3 μM 72 h inhibits cell viability dose dependently 25721419
MDA-MB-468 Function Assay 0.01-10 μM 24 h downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins  25721419
MDA-MB-231 Function Assay 0.01-10 μM 24 h downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins  25721419
HS578T Function Assay 0.01-10 μM 24 h downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins  25721419
SW872 Function Assay 0.01-0.5 μM 24 h reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner  24695632
SW982 Function Assay 0.01-0.5 μM 24 h reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner  24695632
SW872 Apoptosis Assay 0.01-0.5 μM 48 h induces apoptosis dose dependently 24695632
SW982 Apoptosis Assay 0.01-0.5 μM 48 h induces apoptosis dose dependently 24695632
AGS HG Growth Inhibition Assay IC50=0.68 ± 0.031 μM 24597478
AGS LG Growth Inhibition Assay IC50=0.05 ± 0.001 μM 24597478
HGC27 HG Growth Inhibition Assay IC50=0.38 ± 0.022 μM 24597478
HGC27 LG Growth Inhibition Assay IC50=0.02 ± 0.004 μM 24597478
MKN45 HG Growth Inhibition Assay IC50=1.01 ± 0.051 μM 24597478
MKN45 LG Growth Inhibition Assay IC50=0.87 ± 0.030 μM 24597478
NUGC4 HG Growth Inhibition Assay IC50=14.0 ± 3.913 μM 24597478
NUGC4 LG Growth Inhibition Assay IC50=14.0 ± 5.321 μM 24597478
A549 Function Assay 0.25/0.5/1 μM 24 h inhibits Akt phosphorylation slightly 24351425
H460 Function Assay 0.25/0.5/1 μM 24 h inhibits Akt phosphorylation slightly 24351425
H661 Function Assay 0.25/0.5/1 μM 24 h inhibits Akt phosphorylation significantly 24351425
SAS Function Assay 0.25/0.5/1 μM 24 h inhibits Akt phosphorylation significantly 24351425
UT5 Function Assay 0.25/0.5/1 μM 24 h inhibits Akt phosphorylation significantly 24351425
FaDu Function Assay 0.25/0.5/1 μM 24 h inhibits Akt phosphorylation significantly 24351425
RD Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
TE671 Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
RH30  Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
RMS13 Apoptosis Assay 1/1.5/2 μM 72 h DMSO induces caspase-dependent apoptosis combined with UO126 23684925
SUM149PT Cell Viability Assay 0.3 μM 72 h enhances cytotoxic effects of PI3K/AKT pathway inhibitors 23601074
MDA-MB-468 Cell Viability Assay 0.3 μM 72 h enhances cytotoxic effects of PI3K/AKT pathway inhibitors 23601074
MDA-MB-231 Cell Viability Assay 0.3 μM 72 h enhances cytotoxic effects of PI3K/AKT pathway inhibitors 23601074
SY5Y Function Assay 1.5/2.5/5 μM 24 h induces G1 cell-cycle arrest and apoptosis 23378341
SKNBE(2c) Function Assay 1.5/2.5/5 μM 24 h induces G1 cell-cycle arrest and apoptosis 23378341
RD Apoptosis Assay 3 µM 12 h DMSO sensitizes RD cells to DOX-induced apoptosis 23300809
TP5014 Apoptosis Assay 3 µM 12 h DMSO sensitizes RD cells to DOX-induced apoptosis 23300809
HT1080 Apoptosis Assay 3 µM 12 h DMSO sensitizes RD cells to DOX-induced apoptosis 23300809
A549 Function Assay 0-3.3 μM 72 h induces complete downregulation of pAKT 23259591
HCC827 Function Assay 0-3.3 μM 72 h induces complete downregulation of pAKT 23259591
H3122 Function Assay 0-3.3 μM 72 h induces complete downregulation of pAKT 23259591
TALL-1 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
HPB-ALL Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
DND41 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
SUP-T1 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
PEER Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
ALL-SIL Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
KE37 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
Karpas-45 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
RPMI-8402 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
Jurkat Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
MOLT-4 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
PF-382 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
CCRF-CEM Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
LOUCY Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
MOLT-16 Growth Inhibition Assay 1 μM 7 d decreases the cell number significantly 23038273
MM1S Growth Inhibition Assay 0-2 μM 24 h IC50=0.5 μM 22829234
NCI-H929 Growth Inhibition Assay 0-2 μM 24 h IC50=0.25 μM 22829234
KMS12-BM  Growth Inhibition Assay 0-2 μM 24 h IC50＞2 μM 22829234
MDA-MB-436 Function Assay 1 μM 24 h reduces the phosphorylation of AKT 22488590
SUM149PT Function Assay 1 μM 24 h reduces the phosphorylation of AKT 22488590
SUM1315MO2 Function Assay 1 μM 24 h reduces the phosphorylation of AKT 22488590
HCC1937 Function Assay 1 μM 24 h reduces the phosphorylation of AKT 22488590
HCC827 Growth Inhibition Assay 0-3 μM 72 h IC50=0.3 μM 21220474
PC-9  Growth Inhibition Assay 0-3 μM 72 h IC50=0.8 μM 21220474
LN229 Function Assay 1 μM 48 h induces autophagosome formation 21062993
U87 Function Assay 1 μM 48 h induces autophagosome formation 21062993
U373 Function Assay 1 μM 48 h induces autophagosome formation 21062993
SF767 Function Assay 1 μM 48 h induces autophagosome formation 21062993
Mel-Juso Cell Viability Assay 0.01–10 μM 72 h inhibits cell viability dose dependently 21048785
518A2  Cell Viability Assay 0.01–10 μM 72 h inhibits cell viability dose dependently 21048785
Mel-Juso  Function Assay 0.001–1 μM 24 h suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets 21048785
518A2 Function Assay 0.001–1 μM 24 h suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets 21048785
PC3  Growth Inhibition Assay 24h GI50 = 100 nM 20551061
U87MG Function Assay 0.1-1 μM 24 h  DMSO inhibits PI3K-mediated signaling 19633683
U138MG Function Assay 0.1-1 μM 24 h  DMSO inhibits PI3K-mediated signaling 19633683
U118MG Function Assay 0.1-1 μM 24 h  DMSO inhibits PI3K-mediated signaling 19633683
U87MG Growth Inhibition Assay IC50=0.14 μM 19584227
IGROV-1 Growth Inhibition Assay IC50=0.06 μM 19584227
DETROIT562 Growth Inhibition Assay IC50=0.13 μM 19584227
PC3  Growth Inhibition Assay IC50=0.10 μM 19584227
SKOV-3 Growth Inhibition Assay IC50=0.12 μM 19584227
HUVEC Growth Inhibition Assay IC50=0.08 μM 19584227
UCH-1  Function Assay 0-5 μM inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner 19528441
UCH-1  Growth Inhibition Assay 0.01-10 μM 6 d inhibits proliferation dose dependently 19528441
UCH-1  Apoptosis Assay 0.1-10 μM 24 h DMSO induces apoptosis 19528441

... Click to View More Cell Line Experimental Data
In vivo 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. [2] 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. [2]
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