Pictilisib (Synonyms: GDC-0941)

Name: Pictilisib
Brand: MedChemExpress
SKU: HY-50094
Rating: 5.0 (58 reviews)

Cat. No.: HY-50094 Purity: 99.62%: FAQs
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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.

Pictilisib Chemical Structure

CAS No. : 957054-30-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
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10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 58 publication(s) in Google Scholar

Other Forms of Pictilisib:

Pictilisib dimethanesulfonate In-stock

48 Publications Citing Use of MCE Pictilisib

Proliferation Assay

: 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.

: 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.

: 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.

: 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.

: 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.

: Pictilisib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]; Ectopic expression of LKB1 renders PTEN LKB1-deficient endometrial cancer cells susceptible to PI3K inhibition. Western blot analysis of pS6RP (Ser235/236) and p4EBP1(Ser65) in ETN-1 and HEC108 cells with stable expression of vector or flag- tagged LKB1. Cell lysates were harvested 24 hours after GDC-0941 treatment.

: Pictilisib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]; Differential responses of Pten Lkb1-deficient endometrial tumors to inhibitors targeting PI3K and/or mTOR. Mice bearing transplanted Pten Lkb1-deficient endometrial tumors are treated with indicated drugs for 3 days and sacrificed three hours after their dose on day 3 of treatment; their tumors are isolated and tumor lysates are immunoblotted with the indicated antibodies.

: 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.

: 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.

: 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).

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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

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	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	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	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]
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 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]
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]
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	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]
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]
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 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	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	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	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	0.72 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 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]
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]
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	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	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]
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	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]
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 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	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	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	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	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	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]
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]
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	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]
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]
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	IC₅₀	1.2 μM Compound: GDC0941	Cytotoxicity against human T47D cells by MTT assay Cytotoxicity against human T47D cells by MTT assay	[PMID: 28006668]
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]
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	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	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	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

Molecular Weight

513.64

Formula

C₂₃H₂₇N₇O₃S₂

CAS No.

957054-30-7

Appearance

Solid

Color

White to yellow

SMILES

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (251 KB) HNMR (268 KB) LCMS (266 KB) Elemental Analysis Report (109 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]

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

Complete Stock Solution Preparation Table

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

Pictilisib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pictilisib957054-30-7GDC-0941GDC0941GDC 0941PI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Pictilisib (Synonyms: GDC-0941)

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