Cat. No.: HY-10115

PI-103

33 Cited Publications

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Based on 33 publication(s) in Google Scholar

PI-103 is a potent PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.

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Pureté: 99.82%
CAS No.: 371935-74-9
Formule: C₁₉H₁₆N₄O₃
Masse moléculaire:348.36

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

PI-103 Chemical Structure

CAS No.: 371935-74-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (33)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Activité biologique

Description

IC₅₀ & Target^[1]^[4]

p110α

8 nM (IC₅₀)

p110β

88 nM (IC₅₀)

p110δ

48 nM (IC₅₀)

p110γ

150 nM (IC₅₀)

PI3KC2β

26 nM (IC₅₀)

PI3KC2α

1 μM (IC₅₀)

hsVPS34

2.3 μM (IC₅₀)

mTORC1

20 nM (IC₅₀)

mTORC2

83 nM (IC₅₀)

DNA-PK

2 nM (IC₅₀)

ATR

850 nM (IC₅₀)

ATM

920 nM (IC₅₀)

PI4KIIIβ

50 μM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	0.5 μM Compound: Chemical probe : PI103	Antiproliferative activity against human A2780 cells harboring PI3KCA/PTEN mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human A2780 cells harboring PI3KCA/PTEN mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
A549	GI₅₀	0.21 μM Compound: Chemical probe : PI103	Antiproliferative activity against human A549 cells harboring AKT assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human A549 cells harboring AKT assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
A549	IC₅₀	0.18 μM Compound: 7; PI-103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
A549	IC₅₀	4 μM Compound: PI-103	Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
Caco-2	IC₅₀	0.8 μM Compound: Pi103	Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
Caco-2	IC₅₀	0.9 μM Compound: PI-103	Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
Caco-2	IC₅₀	2 μM Compound: PI-103	Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
CHO	IC₅₀	11 nM Compound: Chemical probe : PI103	Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged AKT3 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged AKT3 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay	[PMID: 17575152]
CHO	IC₅₀	13 nM Compound: Chemical probe : PI103	Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged AKT2 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged AKT2 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay	[PMID: 17575152]
CHO	IC₅₀	17 nM Compound: Chemical probe : PI103	Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged AKT1 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged AKT1 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay	[PMID: 17575152]
CHO	IC₅₀	66 nM Compound: Chemical probe : PI103	Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged PDK1 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay Inhibition of recombinant human PI3K in cricetulus griseus CHO cells expressing GFP-tagged PDK1 assessed as translocation to the plasma membrane following IGF-1 stimulation by fluorescence assay	[PMID: 17575152]
CWR22R	IC₅₀	0.1 μM Compound: 7; PI-103	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
Detroit 562	GI₅₀	0.36 μM Compound: Chemical probe : PI103	Antiproliferative activity against human Detroit 562 cells harboring PI3KCA mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human Detroit 562 cells harboring PI3KCA mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
ECV-304	IC₅₀	6.3 μM Compound: PI-103	Antiproliferative activity against human ECV304 cells Antiproliferative activity against human ECV304 cells	[PMID: 22130133]
EOL1	IC₅₀	1.6 μM Compound: PI-103	Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth	[PMID: 36706844]
Fibroblast	IC₅₀	>20 μM Compound: PI-103	Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Fibroblast	IC₅₀	>25 μM Compound: Pi103	Antiproliferative activity against human fibroblast cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human fibroblast cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HaCaT	IC₅₀	2 μM Compound: Pi103	Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HaCaT	IC₅₀	3.5 μM Compound: PI-103	Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HCT-116	GI₅₀	0.93 μM Compound: Chemical probe : PI103	Antiproliferative activity against human HCT-116 cells harboring PI3KCA mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human HCT-116 cells harboring PI3KCA mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
HCT-116	IC₅₀	1 μM Compound: PI-103	Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
HCT-116	IC₅₀	3 μM Compound: Pi103	Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HCT-116	IC₅₀	3.9 μM Compound: PI-103	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HCT-15	IC₅₀	1.76 μM Compound: PI-103	Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HeLa	IC₅₀	0.16 μM Compound: 7; PI-103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
HeLa	IC₅₀	0.23 μM Compound: PI-103	Antiproliferative activity against human HeLa cells Antiproliferative activity against human HeLa cells	[PMID: 34284105]
HeLa	IC₅₀	3.72 μM Compound: PI-103	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HepG2	IC₅₀	8 μM Compound: PI-103	Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
HL-60	IC₅₀	0.0656 μM Compound: PI-103	Antiproliferative activity against human HL-60 cells Antiproliferative activity against human HL-60 cells	[PMID: 34284105]
HL-60	IC₅₀	0.089 μM Compound: PI-103	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth	[PMID: 36706844]
HT-29	IC₅₀	>50 μM Compound: PI-103	Antiproliferative activity against human HT-29 cells Antiproliferative activity against human HT-29 cells	[PMID: 22130133]
HT-29	IC₅₀	1.31 μM Compound: PI-103	Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
Huh-7	IC₅₀	>20 μM Compound: PI-103	Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Huh-7	IC₅₀	1.5 μM Compound: PI-103	Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
Huh-7	IC₅₀	6 μM Compound: Pi103	Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HUVEC	IC₅₀	0.6 nM Compound: PI-103	Antiangiogenic activity against HUVEC after 24 hrs by calcein AM staining-based fluorescent microscopy Antiangiogenic activity against HUVEC after 24 hrs by calcein AM staining-based fluorescent microscopy	[PMID: 18849971]
IGROV-1	GI₅₀	0.06 μM Compound: Chemical probe : PI103	Antiproliferative activity against human IGROV-1 cells harboring PI3KCA/PTEN mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human IGROV-1 cells harboring PI3KCA/PTEN mutant assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
KG-1	IC₅₀	0.088 μM Compound: PI-103	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth	[PMID: 36706844]
Lung cancer cell line	IC₅₀	20 nM Compound: 29; PI-103	Anticancer activity against Lung cancer cell line (unknown origin) assessed as cell growth inhibition Anticancer activity against Lung cancer cell line (unknown origin) assessed as cell growth inhibition	[PMID: 37725577]
MCF7	IC₅₀	13.3 μM Compound: PI-103	Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MCF7	IC₅₀	22.4 μM Compound: PI-103	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 22130133]
MCF7	IC₅₀	3 μM Compound: PI-103	Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
MDA-MB-231	IC₅₀	>20 μM Compound: PI-103	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MDA-MB-231	IC₅₀	0.14 μM Compound: 7; PI-103	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
MDA-MB-231	IC₅₀	15 μM Compound: PI-103	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
MDA-MB-231	IC₅₀	8 μM Compound: Pi103	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
MDA-MB-435	GI₅₀	0.13 μM Compound: Chemical probe : PI103	Antiproliferative activity against human MDA-MB-435 cells harboring AKT assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human MDA-MB-435 cells harboring AKT assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
MDA-MB-468	GI₅₀	0.69 μM Compound: Chemical probe : PI103	Antiproliferative activity against human MDA-MB-468 cells harboring PTEN deletion assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human MDA-MB-468 cells harboring PTEN deletion assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
Melanoma tumor cell line	IC₅₀	20 nM Compound: 29; PI-103	Anticancer activity against Melanoma tumor cell line (unknown origin) assessed as cell growth inhibition Anticancer activity against Melanoma tumor cell line (unknown origin) assessed as cell growth inhibition	[PMID: 37725577]
MIA PaCa-2	IC₅₀	6 μM Compound: PI-103	Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
MOLM-16	IC₅₀	0.058 μM Compound: PI-103	Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth	[PMID: 36706844]
MV4-11	IC₅₀	0.054 μM Compound: PI-103	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth	[PMID: 36706844]
NCI-H3122	IC₅₀	2.51 μM Compound: PI-103	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H446	IC₅₀	2.16 μM Compound: PI-103	Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H727	IC₅₀	>20 μM Compound: PI-103	Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
NCI-H727	IC₅₀	>25 μM Compound: Pi103	Antiproliferative activity against human NCI-H727 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human NCI-H727 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
NCI-H727	IC₅₀	3 μM Compound: PI-103	Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
PC-3	GI₅₀	0.1 μM Compound: Chemical probe : PI103	Antiproliferative activity against human PC-3 cells harboring PTEN deletion assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human PC-3 cells harboring PTEN deletion assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]
PC-3	IC₅₀	0.17 μM Compound: 7; PI-103	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
PC-3	IC₅₀	1.2 μM Compound: Pi103	Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
PC-3	IC₅₀	1.5 μM Compound: PI-103	Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
PC-3	IC₅₀	7.6 μM Compound: PI-103	Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
RL	IC₅₀	2.9 μM Compound: PI-103	Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Sf9	IC₅₀	1034.4 nM Compound: PI103	Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
Sf9	IC₅₀	17.9 nM Compound: PI103	Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
Sf9	IC₅₀	74 nM Compound: PI103	Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
Sf9	IC₅₀	796.3 nM Compound: PI103	Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
SK-OV-3	IC₅₀	0.11 μM Compound: 7; PI-103	Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
SW-620	IC₅₀	1.07 μM Compound: PI-103	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
TT	IC₅₀	2.2 nM Compound: PI-103	Antiproliferative activity against human TT cells after 13 days by fluorescence assay Antiproliferative activity against human TT cells after 13 days by fluorescence assay	[PMID: 18849971]
U-87MG ATCC	GI₅₀	0.18 μM Compound: Chemical probe : PI103	Antiproliferative activity against human U-87MG cells harboring PTEN deletion assessed as cell growth inhibition incubated for 96 hrs by SRB assay Antiproliferative activity against human U-87MG cells harboring PTEN deletion assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 17575152]

In Vitro

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines^[1]. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. 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 ^[2]. PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC₅₀=20 nM) and rapamycin-insensitive (mTORC2, IC₅₀=83 nM) complexes of the protein kinase mTOR^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects^[1]. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 371935-74-9
Appearance Solid
Masse moléculaire 348.36
Formule C₁₉H₁₆N₄O₃
Color Off-white to light green
SMILES

OC1=CC(C2=NC3=C(C(N4CCOCC4)=N2)OC5=C3C=CC=N5)=CC=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (33)

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Journal Impact Factor

Adv Funct Mater

2021 May 24.
Mol Cell

PI3Kβ functions as a protein kinase to promote cellular protein O-GlcNAcylation and acetyl-CoA production for tumor growth. [Abstract]

2025 Mar 19:S1097-2765(25)00186-8. PMID: 40132583
Nat Commun

TIGIT deficiency promotes autoreactive CD4+ T-cell responses through a metabolic‒epigenetic mechanism in autoimmune myositis. [Abstract]

2025 May 15;16(1):4502. PMID: 40374622
Nat Commun

Domain-specific p53 mutants activate EGFR by distinct mechanisms exposing tissue-independent therapeutic vulnerabilities. [Abstract]

2023 Mar 28;14(1):1726. PMID: 36977662
Adv Sci (Weinh)

EGR Proteins Mediate Interferon-Independent Anti-HSV-1 Responses Through Viral and Host Targets. [Abstract]

2026 Mar;13(13):e15546. PMID: 41486724
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Clin Cancer Res

Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. [Abstract]

2014 Nov 1;20(21):5483-95. PMID: 25186968
Cancer Lett

LncRNA HITT inhibits autophagy by attenuating ATG12-ATG5-ATG16L1 complex formation. [Abstract]

2025 Apr 28:616:217532. PMID: 40021040
Adv Healthc Mater

Arming Immune Cell Therapeutics with Polymeric Prodrugs. [Abstract]

2022 May;11(9):e2101944. PMID: 34889072
Acta Biomater

A general prodrug nanohydrogel platform for reduction-triggered drug activation and treatment of taxane-resistant malignancies. [Abstract]

2021 Aug:130:409-422. PMID: 34087447
Cell Syst

Large-scale control over collective cell migration using light-activated epidermal growth factor receptors. [Abstract]

2025 Mar 19;16(3):101203. PMID: 40037348
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
J Transl Med

Delineation of colorectal cancer ligand-receptor interactions and their roles in the tumor microenvironment and prognosis. [Abstract]

2021 Dec 7;19(1):497. PMID: 34876143
Oncogenesis

STAG2 expression imparts distinct therapeutic vulnerabilities in muscle-invasive bladder cancer cells. [Abstract]

2025 Mar 1;14(1):4. PMID: 40025053
Biochem Pharmacol

Ticagrelor reverses multidrug resistance in breast cancer by inhibiting PI3K/AKT/mTOR pathway and suppressing ABCB1 expression and function. [Abstract]

2026 Mar 15:249:117903. PMID: 41846011
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
cell rep methods

A stress-reduced passaging technique improves the viability of human pluripotent cells. [Abstract]

2022 Jan 24;2(2):100155. PMID: 35474962
Antimicrob Agents Chemother

Inhibitory Effect of PIK-24 on Respiratory Syncytial Virus Entry by Blocking Phosphatidylinositol-3 Kinase Signaling. [Abstract]

2020 Sep 21;64(10):e00608-20. PMID: 32718963
J Virol

PIK-24 Inhibits RSV-Induced Syncytium Formation via Direct Interaction with the p85α Subunit of PI3K. [Abstract]

2022 Dec 14;96(23):e0145322. PMID: 36416586
Cell Signal

HK2 promotes migration and invasion of intrahepatic cholangiocarcinoma via enhancing cancer stem-like cells' resistance to anoikis. [Abstract]

2024 Jun:118:111126. PMID: 38453126
Heliyon

Novel cancer-fighting role of ticagrelor inhibits GTSE1-induced EMT by regulating PI3K/Akt/NF-κB signaling pathway in malignant glioma. [Abstract]

2024 May 7;10(9):e30833. PMID: 38774096
BMC Cancer

Artificial intelligence to guide precision anticancer therapy with multitargeted kinase inhibitors. [Abstract]

2022 Nov 24;22(1):1211. PMID: 36434556
ChemMedChem

Oxidative Cyclization-Induced Activation of a Phosphoinositide 3-Kinase Inhibitor for Enhanced Selectivity of Cancer Chemotherapeutics. [Abstract]

2019 Nov 20;14(22):1933-1939. PMID: 31696673
FEBS Lett

LncRNA YIYA drives pancreatic cancer proliferation under high-glucose conditions by reinforcing a RAS-PKM2-dependent Warburg phenotype. [Abstract]

2026 Jun 8. PMID: 42253181
Am J Cancer Res

A long-lasting PI3Kδ inhibitor zandelisib forms a water-shielded hydrogen bond with p110δ and demonstrates sustained inhibitory effects. [Abstract]

2025 May 15;15(5):2097-2110. PMID: 40520883
Expert Rev Anticancer Ther

JARID2 activation by NFYA promotes stemness of triple-negative breast cancer cells through the PI3K/AKT pathway. [Abstract]

2024 Sep 10:1-12. PMID: 39254227
Exp Eye Res

Expression and regulation of alarmin cytokine IL-1α in human retinal pigment epithelial cells. [Abstract]

2018 Jul:172:10-20. PMID: 29551335
bioRxiv

2026 May 20.
bioRxiv

2025 Oct 31.
Princeton University

2025.
bioRxiv

Large-scale control over collective cell migration using light-controlled epidermal growth factor receptors. [Abstract]

2024 May 31:2024.05.30.596676. PMID: 38853934
Research Square Preprint

2022 Jul.

Solvant et solubilité

In Vitro:

DMSO : 10 mg/mL (28.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8706 mL

14.3530 mL

28.7059 mL

5 mM

0.5741 mL

2.8706 mL

5.7412 mL

10 mM

0.2871 mL

1.4353 mL

2.8706 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.05 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 1.05 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.05 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 1.05 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[4]

IC₅₀ values are measured using either a standard thin-layer chromatography (TLC) assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl₂), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl₃:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl₃. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC₅₀ determinations are repeated two to four times, and the reported value is the average of these independent measurements^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

For proliferation assays, MOLM14, OCI-AmL3 and MV4-11 cells are cultured during 48 h at 10⁵ cells/mL, in triplicate, in 10% FCS, without or with 0.1 or 1 μM PI-103, and then pulsed 6 h with 1μCi (37 kBq) [⁴H]-thymidine. The amounts oadioactivity are determined after trichloracetic acid precipitation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
Five to six month old males of either FVB/N strain or nude BALB/c strain are injected subcutaneously with one million cells in PBS. When tumor reaches between 50 and 100 mm³, mice are treated with 10 mg/kg or 70 mg/kg of PI-103 by IP injection daily. Control mice are treated with the same volume of DMSO. Tumor size and mice weight is monitored every 2 days. When mice are sacrificed, tumors are dissected and processed^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39. [Content Brief]

[2]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47. [Content Brief]

[3]. Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706. [Content Brief]

[4]. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8706 mL	14.3530 mL	28.7059 mL	71.7648 mL
	5 mM	0.5741 mL	2.8706 mL	5.7412 mL	14.3530 mL
	10 mM	0.2871 mL	1.4353 mL	2.8706 mL	7.1765 mL
	15 mM	0.1914 mL	0.9569 mL	1.9137 mL	4.7843 mL
	20 mM	0.1435 mL	0.7176 mL	1.4353 mL	3.5882 mL
	25 mM	0.1148 mL	0.5741 mL	1.1482 mL	2.8706 mL

Keywords

PI-103

33 Cited Publications

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PI-103

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PI-103

Voir tous les produits spécifiques à Isoform PI3K

Voir tous les produits spécifiques à Isoform mTOR

Activité biologique

Chemical Information

Publications (33)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PI-103 Related Classifications

HY-10115 Related Classifications