Cat. No.: HY-50094

Pictilisib

(Synonyms: GDC-0941)

68 Cited Publications

Customer Review

Based on 68 publication(s) in Google Scholar

Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

For research use only. We do not sell to patients.

Purity: 99.77%
CAS No.: 957054-30-7
Formula: C₂₃H₂₇N₇O₃S₂
Molecular Weight:513.64

Storage:

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

Pictilisib Chemical Structure

CAS No.: 957054-30-7

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (68)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Bioz

Biological Activity

Description

Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

IC₅₀ & Target^[5]

p110α

3 nM (IC₅₀)

p110α-H1047R

3 nM (IC₅₀)

p110α-E545K

3 nM (IC₅₀)

p110δ

3 nM (IC₅₀)

p110β

33 nM (IC₅₀)

p110γ

75 nM (IC₅₀)

mTOR

0.58 μM (Ki)

DNA-PK

1.23 μM (IC₅₀)

Autophagy

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.14 μM Compound: 17, GDC-0941	Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay	[PMID: 18754654]
A549	GI₅₀	1217 nM Compound: 2	Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32184963]
A549	IC₅₀	1.03 μM Compound: GDC-0941	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
A549	IC₅₀	1.2 μM Compound: GDC-0941	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27043268]
A549	IC₅₀	2.28 μM Compound: GDC0941	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 25911625]
A549	IC₅₀	2.48 μM Compound: GDC-0941	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
A549	IC₅₀	6.9 μM Compound: 1, GDC-0941	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
A549	IC₅₀	6.99 μM Compound: GDC-0941b	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 27353887]
Calu-3	IC₅₀	2.87 μM Compound: GDC-0941	Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
CHO-K1	IC₅₀	64 μM Compound: GDC-0941	Displacement of [3H]-astemizole from human ERG expressed in CHO-K1 cells membrane Displacement of [3H]-astemizole from human ERG expressed in CHO-K1 cells membrane	[PMID: 22325943]
HCC1954	IC₅₀	1.3 μM Compound: GDC0941	Cytotoxicity against human HCC1954 cells by MTT assay Cytotoxicity against human HCC1954 cells by MTT assay	[PMID: 28006668]
HCT-116	IC₅₀	0.37 μM Compound: GDC0941	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 25911625]
HeLa	IC₅₀	2.97 μM Compound: GDC-0941	Antiproliferative activity against paclitaxel-resistant human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
HeLa	IC₅₀	3.15 μM Compound: GDC-0941	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
Hep 3B2	IC₅₀	2.03 μM Compound: Pic; GDC-0941	Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
HepG2	IC₅₀	1 μM Compound: 1, GDC-0941	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HepG2	IC₅₀	6.22 μM Compound: Pic; GDC-0941	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
HT-29	IC₅₀	0.66 μM Compound: 1, GDC-0941	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HT-29	IC₅₀	0.86 μM Compound: 1, GDC-0941	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25086238]
HT-29	IC₅₀	0.86 μM Compound: 1, GDC-0941	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
Huh-7	IC₅₀	1.72 μM Compound: Pic; GDC-0941	Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
JeKo-1	GI₅₀	5 μM Compound: GDC-0941	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
K562	IC₅₀	6.34 μM Compound: Pic; GDC-0941	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
LNCaP	IC₅₀	0.34 μM Compound: 1; GDC-0941	Antiproliferative activity against PTEN deficient human LNCAP cells after 72 hrs by CCK-8 assay Antiproliferative activity against PTEN deficient human LNCAP cells after 72 hrs by CCK-8 assay	[PMID: 28409639]
MCF7	GI₅₀	70.2 nM Compound: GDC-0941	Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay	[PMID: 23360348]
MCF7	IC₅₀	0.07 μM Compound: GDC-0941b	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 27353887]
MCF7	IC₅₀	0.22 μM Compound: Pic; GDC-0941	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
MCF7	IC₅₀	1.09 μM Compound: GDC0941	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 25911625]
MCF7	IC₅₀	1.2 μM Compound: GDC-0941	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
MCF7	IC₅₀	2 μM Compound: GDC0941	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 28006668]
MDA-MB-231	GI₅₀	12 μM Compound: GDC-0941	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	>30 μM Compound: GDC0941	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	[PMID: 28006668]
MDA-MB-231	IC₅₀	0.28 μM Compound: 1, GDC-0941	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25086238]
MDA-MB-231	IC₅₀	0.28 μM Compound: 1, GDC-0941	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
MDA-MB-231	IC₅₀	73.82 μM Compound: 1, GDC-0941	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
MDA-MB-361	IC₅₀	0.028 μM Compound: 17, GDC-0941	Inhibition of Akt Ser 473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation Inhibition of Akt Ser 473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation	[PMID: 18754654]
MDA-MB-361	IC₅₀	0.72 μM Compound: 17, GDC-0941	Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation after 96 hrs by alamar blue assay Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation after 96 hrs by alamar blue assay	[PMID: 18754654]
MIA PaCa-2	GI₅₀	12 μM Compound: GDC-0941	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MKN-45	IC₅₀	0.6 μM Compound: 1, GDC-0941	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 25086238]
MKN-45	IC₅₀	0.6 μM Compound: 1, GDC-0941	Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
MM1.S	IC₅₀	0.1 μM Compound: GDC-0941	Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay	[PMID: 30715878]
MOLM-13	GI₅₀	0.048 μM Compound: 16; GDC-0941c	Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLM-14	GI₅₀	0.21 μM Compound: 16; GDC-0941c	Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLT-4	IC₅₀	0.18 μM Compound: Pic; GDC-0941	Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
MV4-11	EC₅₀	10.7 μM Compound: Pic; GDC-0941	Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis	[PMID: 29360358]
MV4-11	EC₅₀	2.71 μM Compound: Pic; GDC-0941	Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis	[PMID: 29360358]
MV4-11	GI₅₀	0.88 μM Compound: 16; GDC-0941c	Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MV4-11	GI₅₀	3 μM Compound: GDC-0941	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MV4-11	IC₅₀	1.46 μM Compound: Pic; GDC-0941	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
NALM-6	GI₅₀	0.15 μM Compound: 16; GDC-0941c	Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
NCI-H1650	IC₅₀	4.73 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H1975	IC₅₀	0.27 μM Compound: 1, GDC-0941	Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
NCI-H1975	IC₅₀	0.703 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H1975	IC₅₀	2.42 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
NCI-H2228	IC₅₀	1.07 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
NCI-H226	IC₅₀	2.9 μM Compound: 1, GDC-0941	Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
NCI-H226	IC₅₀	5.91 μM Compound: GDC-0941	Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H23	IC₅₀	0.936 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H358	IC₅₀	1.33 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H460	IC₅₀	0.87 μM Compound: 1, GDC-0941	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
NCI-H460	IC₅₀	0.87 μM Compound: 1, GDC-0941	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25086238]
NCI-H460	IC₅₀	0.87 μM Compound: 1, GDC-0941	Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25440879]
NCI-H460	IC₅₀	1.26 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
NCI-H460	IC₅₀	2.68 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
NCI-H522	IC₅₀	2.14 μM Compound: GDC-0941	Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
PC-3	EC₅₀	0.34 μM Compound: 1, GDC-0941	Antiproliferative activity against human PC3 cells after 3 to 4 days by Cell titer Glo assay Antiproliferative activity against human PC3 cells after 3 to 4 days by Cell titer Glo assay	[PMID: 21985639]
PC-3	GI₅₀	3 μM Compound: GDC-0941	Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PC-3	IC₅₀	0.037 μM Compound: 17, GDC-0941	Inhibition of Akt Ser 473 phosphorylation in PTEN-null human PC3 cells Inhibition of Akt Ser 473 phosphorylation in PTEN-null human PC3 cells	[PMID: 18754654]
PC-3	IC₅₀	0.2 μM Compound: GDC-0941b	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27353887]
PC-3	IC₅₀	0.28 μM Compound: 17, GDC-0941	Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay	[PMID: 18754654]
PC-3	IC₅₀	0.39 μM Compound: 2, GDC-0941	Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days	[PMID: 20050669]
PC-3	IC₅₀	0.457 μM Compound: 1; GDC-0941	Antiproliferative activity against PTEN deficient human PC3 cells after 72 hrs by CCK-8 assay Antiproliferative activity against PTEN deficient human PC3 cells after 72 hrs by CCK-8 assay	[PMID: 28409639]
PC-3	IC₅₀	0.75 μM Compound: Pic; GDC-0941	Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
PC-3	IC₅₀	0.8 μM Compound: GDC-0941	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27043268]
PC-3	IC₅₀	280 nM Compound: 1, GDC-0941	Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay	[PMID: 21981714]
PF-382	GI₅₀	0.14 μM Compound: 16; GDC-0941c	Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
PLC-PRF-5	IC₅₀	3.07 μM Compound: Pic; GDC-0941	Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
Raji	IC₅₀	6.5 μM Compound: Pic; GDC-0941	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
Ramos	IC₅₀	4.86 μM Compound: Pic; GDC-0941	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
RAW	IC₅₀	298 nM Compound: 37, GDC-0941	Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA	[PMID: 22548342]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.003 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	0.033 μM Compound: 17, GDC-0941	Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay	[PMID: 18754654]
Sf9	IC₅₀	17 nM Compound: 37, GDC-0941	Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP	[PMID: 23540645]
Sf9	IC₅₀	42 nM Compound: 37, GDC-0941	Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay	[PMID: 22548342]
SGC-7901	IC₅₀	1.8 μM Compound: 1, GDC-0941	Cytotoxicity against human SGC7901 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SGC7901 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
SJRH30	IC₅₀	0.478 μM Compound: GDC-0941	Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
SJRH30	IC₅₀	0.8 μM Compound: GDC-0941	Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition by SRB assay Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition by SRB assay	[PMID: 32317209]
SK-BR-3	IC₅₀	0.9 μM Compound: GDC0941	Cytotoxicity against human SKBR3 cells by MTT assay Cytotoxicity against human SKBR3 cells by MTT assay	[PMID: 28006668]
SK-HEP1	IC₅₀	4.3 μM Compound: Pic; GDC-0941	Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
SK-MEL19	GI₅₀	6 μM Compound: GDC-0941	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	GI₅₀	147.6 nM Compound: GDC-0941	Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay	[PMID: 23360348]
SK-OV-3	IC₅₀	0.864 μM Compound: 1; GDC-0941	Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay	[PMID: 28409639]
SU-DHL-6	IC₅₀	0.03 μM Compound: Pic; GDC-0941	Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay	[PMID: 29360358]
T47D	GI₅₀	3 μM Compound: GDC-0941	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T47D	IC₅₀	1.2 μM Compound: GDC0941	Cytotoxicity against human T47D cells by MTT assay Cytotoxicity against human T47D cells by MTT assay	[PMID: 28006668]
U-87MG ATCC	GI₅₀	0.07 μM Compound: 61	Antiproliferative activity against human U87MG cells after 96 hrs Antiproliferative activity against human U87MG cells after 96 hrs	[PMID: 30583248]
U-87MG ATCC	GI₅₀	6 μM Compound: GDC-0941	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-87MG ATCC	IC₅₀	0.046 μM Compound: 17, GDC-0941	Inhibition of Akt Ser 473 phosphorylation in PTEN-null human U87MG cells Inhibition of Akt Ser 473 phosphorylation in PTEN-null human U87MG cells	[PMID: 18754654]
U-87MG ATCC	IC₅₀	0.55 μM Compound: 1; GDC-0941	Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay	[PMID: 28409639]
U-87MG ATCC	IC₅₀	0.95 μM Compound: 17, GDC-0941	Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay	[PMID: 18754654]
U-87MG ATCC	IC₅₀	1.24 μM Compound: GDC0941	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 25911625]
U-87MG ATCC	IC₅₀	3.13 μM Compound: GDC-0941	Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36599263]
U-87MG ATCC	IC₅₀	7.77 μM Compound: 1, GDC-0941	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]

In Vitro

Pictilisib (GDC-0941) and RP-56976 reduce tumor cell viability by 80% or greater in the breast cancer cell lines than single-agent treatment. GDC-0941 inhibits Akt phosphorylation and downstream targets of Akt signaling such as pPRAS40 and pS6 in Hs578T1.2 (PI3Kα wild-type), MCF7-neo/HER2 (PI3Kα-mutant), and MX-1 (PTEN-null) tumor models. Pictilisib (GDC-0941) decreases the time of RP-56976-induced mitotic arrest prior to apoptosis^[1]. Pictilisib (GDC-0941) shows a high efficacy of antitumor activity in two ZD1839-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460. Pictilisib (GDC-0941) is highly efficacious in combination with U0126 in inducing cell growth inhibition, G0-G1 arrest and cell apoptosis. H460 cells with activating mutations of PIK3CA are relatively more sensitive to Pictilisib (GDC-0941) than A549 cells with wild-type PIK3CA^[3]. Pictilisib (GDC-0941) reduces PI3K pathway activity in both cell lines, illustrated by decreased pAK. Pictilisib (GDC-0941) significantly reduces secreted VEGF detected in the medium after hypoxic/anoxic exposure in all cells^[4].

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

In Vivo

Pictilisib (GDC-0941) (150 mg/kg, p.o.) leads to tumor stasis in MCF7-neo/HER2-bearing animals model. Pictilisib (GDC-0941) and RP-56976 result in tumor regressions during the treatment period leading to enhanced antitumor responses^[1]. Tumours in the Pictilisib (GDC-0941)-treated mice show a marked non-linear shrinkage, and when the Pictilisib (GDC-0941) treatment ceased, the tumours in the test cohort mice grow again^[2]. Pictilisib (GDC-0941) (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 957054-30-7
Appearance Solid
Molecular Weight 513.64
Formula C₂₃H₂₇N₇O₃S₂
Color White to yellow
SMILES

CS(N1CCN(CC2=CC3=C(C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)S2)CC1)(=O)=O
Synonyms

GDC-0941
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (68)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. [Abstract]

2018 Aug;560(7719):499-503. PMID: 30051890
Cell

Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]

2025 May 29;188(11):3065-3080.e21. PMID: 40393457
Cell

Distinct longevity mechanisms across and within species and their association with aging. [Abstract]

2023 Jun 22;186(13):2929-2949.e20. PMID: 37269831
Cancer Discov

Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. [Abstract]

2012 May;2(5):425-33. PMID: 22588880

Pictilisib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2012 May;2(5):425-33. [Abstract]

Effects of KIN-193, GDC-0941, PIK-75 and IC87114 on AKT phosphorylation in PTEN-deficient cell lines as indicated. Representative western blots are shown. Bar graphs represent mean ± SD of western blot quantitations of AKTT308 (n=3).
Cell Metab

Fasting-mimicking diet blocks triple-negative breast cancer and cancer stem cell escape. [Abstract]

2021 Nov 2;33(11):2247-2259.e6. PMID: 34731655
Cell Metab

Pten positively regulates brown adipose function, energy expenditure, and longevity. [Abstract]

2012 Mar 7;15(3):382-94. PMID: 22405073

Pictilisib purchased from MedChemExpress. Usage Cited in: Cell Metab. 2012 Mar 7;15(3):382-94. [Abstract]

Effect of the indicated PI3K inhibitors on pre-brown adipocytes. Cultures are treated with the inhibitors at the indicated concentrations (μM) for 4 h. Protein levels (top) and mRNA levels (bottom) of the indicated proteins and genes, respectively, are analyzed. Assays are performed in triplicate cultures. Values represent mean ± sd, and statistical significance is determined by the two-tailed Student’s t-test. *p<0.05, **p<0.01.
Nat Cancer

Loss of Pip4k2c confers liver-metastatic organotropism through insulin-dependent PI3K-AKT pathway activation. [Abstract]

2024 Mar;5(3):433-447. PMID: 38286827
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Gastroenterology

Targeting Mutual Dependence of Phosphatidylinositol-3-Kinase α/δ and Small Ubiquitin-Like Modifier Signaling in Pancreatic Cancer. [Abstract]

2025 Oct 27:S0016-5085(25)05903-7. PMID: 41143762
Mol Cell

HIF-independent oxygen sensing via KDM6A regulates ferroptosis. [Abstract]

2025 Aug 7;85(15):2973-2987.e6. PMID: 40712585
Cancer Res

Oncogenic Calreticulin Induces Immune Escape by Stimulating TGF-β Expression and Regulatory T Cell Expansion in the Bone Marrow Microenvironment. [Abstract]

2024 Sep 16;84(18):2985-3003. PMID: 38885318
Cancer Res

A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. [Abstract]

2014 Jan 1;74(1):15-23. PMID: 24322983
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Stabilization of p21 by mTORC1/4E-BP1 predicts clinical outcome of head and neck cancers. [Abstract]

2016 Feb 2;7:10438. PMID: 26832959

Pictilisib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2016 Feb 2;7:10438. [Abstract]

Western blot illustrating the effect of PI3K inhibitors on p21 protein levels in MEFs. Cells are treated for 24 hours with the indicated concentrations of the different drugs.
Nat Commun

A PI3K p110β-Rac signalling loop mediates Pten-loss-induced perturbation of haematopoiesis and leukaemogenesis. [Abstract]

2015 Oct 7;6:8501. PMID: 26442967
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Sci Transl Med

mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. [Abstract]

2013 Jul 31;5(196):196ra99. PMID: 23903756

Pictilisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]

Sensitivity to GDC-0941 in parental MDA453 and T47D and BYL719-resistant MDA453R and T47DR cells. Protein lysates are isolated after 24 hours of treatment with 1 μM GDC-0941 and probed against the indicated proteins.
Adv Sci (Weinh)

IL1R2 Marks and Sorts a Spermatogonial Stem Cell Population Critical for Restoring Spermatogenesis Upon Interruption in Mammals. [Abstract]

2026 Mar;13(13):e01810. PMID: 41486830
Nat Chem Biol

A multiplex single-cell RNA-Seq pharmacotranscriptomics pipeline for drug discovery. [Abstract]

2025 Mar;21(3):432-442. PMID: 39482470
Nat Chem Biol

Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation. [Abstract]

2017 Jan;13(1):38-45. PMID: 27820799
J Clin Invest

Oncogenic KRAS signaling drives evasion of innate immune surveillance in lung adenocarcinoma by activating CD47. [Abstract]

2023 Jan 17;133(2):e153470. PMID: 36413402
MedComm (2020)

Ubiquitin-specific protease 22 controls melanoma metastasis and vulnerability to ferroptosis through targeting SIRT1/PTEN/PI3K signaling. [Abstract]

2024 Aug 12;5(8):e684. PMID: 39135915
J Pharm Anal

Screen of FDA-approved drug library identifies vitamin K as anti-ferroptotic drug for osteoarthritis therapy through Gas6. [Abstract]

2025 May;15(5):101092. PMID: 40496065
Free Radic Biol Med

7,8-Dihydroxyflavone protects acetaminophen induced liver injury through activating PI3K/Akt/NRF2/GPX4 mediated ferroptosis suppression. [Abstract]

2025 Oct 30:242:275-287. PMID: 41173313
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
Oncogene

PIK3CA(H1047R)- and Her2-initiated mammary tumors escape PI3K dependency by compensatory activation of MEK-ERK signaling. [Abstract]

2016 Jun 9;35(23):2961-70. PMID: 26640141

Pictilisib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]

Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC⁺PIK3CA^H1047R tumors treated as indicated.
Cell Death Discov

The protective up-regulation of metallothionein-2A in intervertebral disc degeneration inhibits nucleus pulposus cell ferroptosis through activation of the PI3K/AKT/mTOR pathway. [Abstract]

2026 Feb 25;12(1):111. PMID: 41741409
Cell Rep

Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]

2023 May 29;42(6):112570. PMID: 37252843
Cell Rep

Divergent Roles of PI3K Isoforms in PTEN-Deficient Glioblastomas. [Abstract]

2020 Sep 29;32(13):108196. PMID: 32997991
Br J Cancer

PI3K activation promotes resistance to eribulin in HER2-negative breast cancer. [Abstract]

2021 Apr;124(9):1581-1591. PMID: 33723394
Sci Signal

MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells. [Abstract]

2025 Sep 2;18(902):eadw3231. PMID: 40892895
Sci Signal

Suppression of caspase 8 activity by a coronin 1-PI3Kδ pathway promotes T cell survival independently of TCR and IL-7 signaling. [Abstract]

2021 Dec 21;14(714):eabj0057. PMID: 34932374
J Cell Biol

Inhibition of class I PI3K enhances chaperone-mediated autophagy. [Abstract]

2020 Dec 7;219(12):e202001031. PMID: 33048163
Cell Biosci

Anti-tumor effects of dual PI3K-HDAC inhibitor CUDC-907 on activation of ROS-IRE1α-JNK-mediated cytotoxic autophagy in esophageal cancer. [Abstract]

2022 Aug 21;12(1):135. PMID: 35989326
J Clin Endocrinol Metab

Targeting Corticotroph HDAC and PI3-Kinase in Cushing Disease. [Abstract]

2021 Jan 1;106(1):e232-e246. PMID: 33000123
Int J Oncol

Downregulation of BRD4 inhibits gallbladder cancer proliferation and metastasis and induces apoptosis via PI3K/AKT pathway. [Abstract]

2017 Sep;51(3):823-831. PMID: 28766687

Pictilisib purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Sep;51(3):823-831. [Abstract]

Protein levels of BRD4, p-AKT and AKT in GDC-0941 treated NOZ cells after 72 h.
Bioorg Chem

Eupalinolide B prevents cerebral ischemia-reperfusion injury via the PI3K/Akt/GSK3β(Ser9) signaling pathway. [Abstract]

2026 Jun 5:173:109635. PMID: 41719922
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
Molecules

Screening of PI3K-Akt-targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. [Abstract]

2019 Apr 1;24(7):1260. PMID: 30939726
Cancers

Expression of MALAT1 Promotes Trastuzumab Resistance in HER2 Overexpressing Breast Cancers. [Abstract]

2020 Jul 16;12(7):1918. PMID: 32708561
Biochem J

Up-regulation of the PI3K/AKT and RHO/RAC/PAK signalling pathways in CHK1 inhibitor resistant Eµ-Myc lymphoma cells. [Abstract]

2022 Oct 14;479(19):2131-2151. PMID: 36240067
Lipids Health Dis

MG-132 activates sodium palmitate-induced autophagy in human vascular smooth muscle cells and inhibits senescence via the PI3K/AKT/mTOR axis. [Abstract]

2024 Sep 4;23(1):282. PMID: 39232759
Transl Oncol

A novel strategy for combination of clofarabine and pictilisib is synergistic in gastric cancer. [Abstract]

2022 Jan;15(1):101260. PMID: 34735897
Oncol Rep

Aprepitant inhibits the progression of esophageal squamous cancer by blocking the truncated neurokinin‑1 receptor. [Abstract]

2023 Jul;50(1):131. PMID: 37203393
Sci Rep

The role of the PIK3CA gene in the development and aging of the brain. [Abstract]

2021 Jan 11;11(1):291. PMID: 33431926
J Virol

SFTSV utilizes AXL/GAS6 for entry via PI3K-PLC-dependent macropinocytosis activated by AXL-kinase. [Abstract]

2025 Aug 25:e0022125. PMID: 40853130
Cell Cycle

HER2-L755S mutation induces hyperactive MAPK and PI3K-mTOR signaling, leading to resistance to HER2 tyrosine kinase inhibitor treatment. [Abstract]

2019 Jul;18(13):1513-1522. PMID: 31135266
Cancer Med

Focal Adhesion Kinase Intersects With the BRD4-MYC Axis and YAP1 to Drive Tumor Cell Growth, Phenotypic Plasticity, Stemness, and Metastatic Potential in Colorectal Cancer. [Abstract]

2025 Sep;14(18):e71227. PMID: 40959971
Chem Biodivers

Shikonin Derivative Suppresses Colorectal Cancer Cells Growth via Reactive Oxygen Species-Mediated Mitochondrial Apoptosis and PI3K/AKT Pathway. [Abstract]

2025 Apr;22(4):e202403291. PMID: 40022742
Biochem Biophys Res Commun

Loss of DNA replication fork protection by TIMELESS degradation supports oncogene-induced senescence. [Abstract]

2025 Jun 12:776:152203. PMID: 40517672
Oncol Lett

AKR1B10 inhibits the proliferation and metastasis of hepatocellular carcinoma cells by regulating the PI3K/AKT pathway. [Abstract]

2023 Nov 15;27(1):18. PMID: 38034486
Bioorg Med Chem Lett

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. [Abstract]

2012 Mar 1;22(5):1874-8. PMID: 22325943
Anticancer Res

Akt Regulates Extracellular Vesicle Secretion in Hypoxia-adapted Multiple Myeloma RPMI8226 Cells. [Abstract]

2025 Apr;45(4):1355-1366. PMID: 40155008
J Surg Res

Anal Cancer Prevention Through the Topical Use of Single or Dual PI3K/mTOR Inhibitors. [Abstract]

2023 Feb:282:137-146. PMID: 36274448
Arab J Gastroenterol

NNMT suppresses H3K9me3 to facilitate malignant progression and drug resistance in gastric cancer. [Abstract]

2025 Feb;26(1):104-111. PMID: 39757078
Int J Clin Exp Pathol

2017;10(3):3033-3042.
bioRxiv

2026 Mar 25.
bioRxiv

IPF AT2 cells are stuck in transition and biophysically dysfunctional. [Abstract]

2026 Feb 17:2026.02.14.705941. PMID: 41756935
bioRxiv

Loss of the tumor suppressor PTEN activates cell-intrinsic interferon signaling to drive immune resistance. [Abstract]

2025 Sep 20:2025.09.17.676669. PMID: 41000885
bioRxiv

Endocrine therapy induces oxidative stress in ER+ breast cancer that sensitizes persister cells to ferroptosis. [Abstract]

2025 Jul 23:2025.07.18.665614. PMID: 40777469
Research Square Preprint

2024 Nov 26.
Patent

US20210236501A1.
Debreceni egyettemmolekularis orvostudomany

2024 Dec.
Patent

US20220313694A1.
Tierärztliche Hochschule Hannover

2021 Jul.
bioRxiv

2020 Mar.
Oncotarget

Simultaneous inhibition of Vps34 kinase would enhance PI3Kδ inhibitor cytotoxicity in the B-cell malignancies. [Abstract]

2016 Aug 16;7(33):53515-53525. PMID: 27447747

Pictilisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]

PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.
Oncotarget

Characterization of selective and potent PI3Kδ inhibitor (PI3KDIN- 015) for B-Cell malignances. [Abstract]

2016 May 31;7(22):32641-51. PMID: 27081697

Pictilisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]

The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC₅₀ of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (194.69 mM; ultrasonic and warming and heat to 60°C; 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

1.9469 mL

9.7344 mL

19.4689 mL

5 mM

0.3894 mL

1.9469 mL

3.8938 mL

10 mM

0.1947 mL

0.9734 mL

1.9469 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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: ≥ 2.5 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 5 mg/mL (9.73 mM); Suspened solution; Need ultrasonic

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

Protocol

Cell Assay^[1]

Cells are treated at EC₅₀ concentrations of Pictilisib (GDC-0941), RP-56976, or both for 4 or 24 hours and lysed in 1×Cell Extraction Buffer supplemented with protease inhibitors and Phosphatase Inhibitor Cocktails 1 and 2. Protein concentrations are determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal amounts of protein are separated by electrophoresis through NuPAGE Bis-Tris 10% gradient gels, transferred onto polyvinylidene difluoride membranes using the Criterion system, and probed with monospecific primary antibodies. Specific antigen-antibody interactions are detected with IRDye 680 or IRDye 800 infrared secondary antibodies using a LI-COR imaging system.

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

Animal Administration^[1]

Female nu/nu mice are inoculated subcutaneously with MCF7-neo/HER2 or MX-1 breast cancer cells. When tumors reach a mean volume of 200 to 250 mm³, animals are size-matched and distributed into groups consisting of 10 animals per group. RP-56976 formulated in 3% EtOH, 97% saline is administered intravenously once weekly. Pictilisib (GDC-0941), formulated in MCT (0.5% methylcellulose, 0.2% Tween-80) is dosed orally and daily. MAXF1162 is an HER2+/ER+/PR+ patient-derived breast cancer tumor xenograft model established by directly implanting tumors subcutaneously from patient to NMRI nu/nu mice. Tumor volume is calculated. Tumor sizes are recorded twice weekly over the course of a study.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 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)
- 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)
Handling Instructions (2659 KB)

References

[1]. Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18(14):3901-11. Epub 2012 May 14. [Content Brief]

[2]. Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.Anticancer Res. 2012 Feb;32(2):415-20. [Content Brief]

[3]. Zou ZQ, et al. The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5(2):503-8. [Content Brief]

[4]. Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct [Content Brief]

[5]. Folkes AJ, et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem. 2008 Sep 25;51(18):5522-32. [Content Brief]

[6]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [Content Brief]

[7]. Cheng H, et al. A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. Cancer Res. 2014 Jan 1;74(1):15-23. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9469 mL	9.7344 mL	19.4689 mL	48.6722 mL
	5 mM	0.3894 mL	1.9469 mL	3.8938 mL	9.7344 mL
	10 mM	0.1947 mL	0.9734 mL	1.9469 mL	4.8672 mL
	15 mM	0.1298 mL	0.6490 mL	1.2979 mL	3.2448 mL
	20 mM	0.0973 mL	0.4867 mL	0.9734 mL	2.4336 mL
	25 mM	0.0779 mL	0.3894 mL	0.7788 mL	1.9469 mL
	30 mM	0.0649 mL	0.3245 mL	0.6490 mL	1.6224 mL
	40 mM	0.0487 mL	0.2434 mL	0.4867 mL	1.2168 mL
	50 mM	0.0389 mL	0.1947 mL	0.3894 mL	0.9734 mL
	60 mM	0.0324 mL	0.1622 mL	0.3245 mL	0.8112 mL
	80 mM	0.0243 mL	0.1217 mL	0.2434 mL	0.6084 mL
	100 mM	0.0195 mL	0.0973 mL	0.1947 mL	0.4867 mL

Keywords

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Pictilisib

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Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Chemical Probe 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

Glucose Metabolism Compound 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

Membrane Protein-targeted Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive 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

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Pictilisib

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (68)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Pictilisib Related Classifications

Cat. No.: HY-50094