Referencia número: HY-10297

Omipalisib

Name: Omipalisib
Brand: MedChemExpress
SKU: HY-10297
Price: 72.00 USD
Availability: InStock
Rating: 5 (21 reviews)

(Synonyms: GSK2126458; GSK458)

21 Cited Publications

Revisión del cliente

Based on 21 publication(s) in Google Scholar

Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with K_is of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 99.94%
No. CAS: 1086062-66-9
Fòrmula: C₂₅H₁₇F₂N₅O₃S
Peso molecular:505.50

Almacenamiento:

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

Omipalisib Chemical Structure

No. CAS: 1086062-66-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (21)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

^[1]

p110α

0.019 nM (Ki)

p110α-E545K

0.008 nM (Ki)

p110α-E542K

0.008 nM (Ki)

p110α-H1047R

0.009 nM (Ki)

p110β

0.13 nM (Ki)

p110δ

0.024 nM (Ki)

p110γ

0.06 nM (Ki)

mTORC1

0.18 nM (Ki)

mTORC2

0.3 nM (Ki)

Ver todos los productos específicos de isoformas PI3K :

Ver todos los productos específicos de isoformas mTOR :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	26.6 nM Compound: GSK; GSK-2126458	Growth inhibition of human A549 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human A549 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
A549	IC₅₀	0.6 μM Compound: GSK2126458	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26819001]
A549	IC₅₀	0.86 μM Compound: Omipalisib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
A549	IC₅₀	140 nM Compound: GSK-2126458	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 27448924]
BEL-7404 tumor cell line	IC₅₀	0.01 μM Compound: GSK2126458	Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay	[PMID: 26819001]
BT-474	IC₅₀	2.4 nM Compound: 1; GSk2126458	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 24900173]
DU-145	GI₅₀	16.3 nM Compound: GSK; GSK-2126458	Growth inhibition of human DU-145 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human DU-145 cells harboring wild type p110alpha and PTEN measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
HCT-116	IC₅₀	0.01 μM Compound: GSK2126458	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26819001]
HCT-116	IC₅₀	0.14 μM Compound: Omipalisib	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
HCT-116	IC₅₀	154 nM Compound: GSK-2126458	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 27448924]
HT-29	GI₅₀	19.9 nM Compound: GSK; GSK-2126458	Growth inhibition of human HT-29 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human HT-29 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
MCF7	IC₅₀	0.03 μM Compound: Omipalisib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
MDA-MB-231	IC₅₀	0.13 μM Compound: GSK2126458	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: 26819001]
NCI-H1975	GI₅₀	14.4 nM Compound: GSK; GSK-2126458	Growth inhibition of human NCI-H1975 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human NCI-H1975 cells harboring mutated p110alpha measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
PC-3	GI₅₀	0.25 μM Compound: 3; GSK2126458	Growth inhibition of human PC3 cells after 72 hrs by sulforhodamine B assay Growth inhibition of human PC3 cells after 72 hrs by sulforhodamine B assay	[PMID: 33561608]
PC-3	GI₅₀	197 nM Compound: GSK; GSK-2126458	Growth inhibition of human PC-3 cells harboring PTEN inactivation measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay Growth inhibition of human PC-3 cells harboring PTEN inactivation measured after 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 33360802]
T47D	IC₅₀	3 nM Compound: 1; GSk2126458	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 24900173]
U-87MG ATCC	GI₅₀	0.22 μM Compound: 3; GSK2126458	Growth inhibition of human U87MG cells after 72 hrs by sulforhodamine B assay Growth inhibition of human U87MG cells after 72 hrs by sulforhodamine B assay	[PMID: 33561608]
U-87MG ATCC	IC₅₀	537 nM Compound: GSK-2126458	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 27448924]

In Vitro

Omipalisib (GSK2126458) potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with K_i of 8 pM, 8 pM and 9 pM, respectively. Omipalisib causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC₅₀ of 0.41 nM and 0.18 nM, respectively. Furthermore, Omipalisib (GSK2126458) leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC₅₀ of 3 nM and 2.4 nM, respectively^[1]. The combination of Omipalisib or GSK1120212 with Omipalisib enhances cell growth inhibition and decreases S6 ribosomal protein phosphorylation in drug-resistant clones from the A375 BRAF(V600E) and the YUSIT1 BRAF(V600K) melanoma cell lines^[2]. Omipalisib (GSK2126458) potentiates the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines^[3].

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

In Vivo

In a BT474 human tumor xenograft model, Omipalisib (GSK2126458) treatment results in a dose-dependent reduction in pAkt-S473 levels, and exhibits dose-dependent tumor growth inhibition at a low dose of 300 μg/kg. Besides, Omipalisib (GSK2126458) shows low blood clearance and good oral bioavailability in four preclinical species (mouse, rat, dog, and monkey)^[1].

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

Ensayo clínico

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

Chemical Information

No. CAS 1086062-66-9
Appearance Solid
Peso molecular 505.50
Fòrmula C₂₅H₁₇F₂N₅O₃S
Color White to yellow
SMILES

COC1=NC=C(C=C1NS(C2=CC=C(C=C2F)F)(=O)=O)C3=CC=C(C4=C3)N=CC=C4C5=CN=NC=C5
Synonyms

GSK2126458; GSK458
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (21)

All Cell Imaging/StainingBio/Physico-chemical AssayWB

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Journal Impact Factor

Mol Cancer

The phospholipid transporter PITPNC1 links KRAS to MYC to prevent autophagy in lung and pancreatic cancer. [Abstract]

2023 May 20;22(1):86. PMID: 37210549

Omipalisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 May 20;22(1):86. [Abstract]

Western blot of PITPNC1 expression in A549, H2009 and HPAFII cells treated for 24 h with pharmacologic inhibitors: Trametinib (MEKi, 0.5 μmol/L), BIX02189 (MEK5i, 10 μmol/L), SP600125 (JNKi, 10 μmol/L) or GSK2126458 (Omipalisib, PI3Ki, 0.1 μmol/L). Twenty μg of protein were loaded per sample. β-TUBULIN was used as loading marker.
J Hepatol

FOSL1 promotes cholangiocarcinoma via transcriptional effectors that could be therapeutically targeted. [Abstract]

2021 Aug;75(2):363-376. PMID: 33887357
Exp Hematol Oncol

Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]

2016 Jul 29:5:22. PMID: 27478685
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
Clin Cancer Res

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

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

Omipalisib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]

Quantification of total nuclear EdU content in gated S-phase cells (red cells, top row, panel D; SNR cells excluded). Al:alpelisib, A8:AZD8055, D:DMSO, M:MK-2206, O:Omipalisib, R:Rapamycin, T2:Torin2. P<0.001 for each drug vs DMSO (Mann-Whitney U test).

Omipalisib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]

Time-lapse imaging of asynchronous HCC1806 cells expressing H2B:mTurquoise and mVenus:hGeminin(1-110). mTurquoise was used to score cell division and death; mVenus intensity levels were used to identify cell cycle stage, as illustrated for a representative DMSO-exposed cell. Heatmaps show the progression of 340 cells through the cell cycle after exposure to DMSO or a 0.3xGR_max dose (1 μM) of Omipalisib or Torin2 for 48h. Colors denote cell cycle stages and cell fates (see legend).

Omipalisib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]

Phenotypic responses caused by drug exposure. Shown are representative traces of mVenus fluorescence intensity vs time for single cells treated with Omipalisib (blue) or Torin2 (red). The trace for a DMSO-exposed cell is shown in the background (grey) for comparison.

Omipalisib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]

Quantification of nuclear intensity values in gated S-phase cells. Boxplots show median and 25th/75th percentiles. D:DMSO, A8:AZD8055, O:Omipalisib, T2:Torin2, AZ:AZ20, R:Rabusertib.
J Invest Dermatol

Identification of Small-Molecule Inhibitors Targeting Different Signaling Pathways in Cancer-Associated Fibroblast Reprogramming Under Tumor-Stroma Interaction. [Abstract]

2025 Jan;145(1):65-76.e13. PMID: 38848988
Mol Cancer Ther

Navitoclax, a Bcl-2/xL Inhibitor, and YM155, a Survivin Inhibitor, in Combination with Carboplatin, Effectively Inhibit Ovarian Cancer Tumor Growth. [Abstract]

2025 Apr 28:OF1-OF13. PMID: 40293279
Ecotoxicol Environ Saf

The ROS/AKT/S6K axis induces corneal epithelial dysfunctions under LED blue light exposure. [Abstract]

2024 Nov 15:287:117345. PMID: 39541698
Mol Cancer Res

Multifunctional APJ Pathway Promotes Ovarian Cancer Progression and Metastasis. [Abstract]

2019 Jun;17(6):1378-1390. PMID: 30858172
Front Pharmacol

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

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

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

2020 Apr 23;25(8):1980. PMID: 32340370
Cancer Res Commun

Remodeling of Stromal Immune Microenvironment by Urolithin A Improves Survival with Immune Checkpoint Blockade in Pancreatic Cancer. [Abstract]

2023 Jul 12;3(7):1224-1236. PMID: 37448553
Anal Methods

Estimation of the metabolic stability of omipalisib in human liver microsomes employing an ultra-fast UPLC-MS/MS approach: in silico screening for structural alarms and metabolic lability. [Abstract]

2026 Feb 5;18(5):1101-1115. PMID: 41586454
PLoS One

Omipalisib reduces hyperphosphorylated tau protein by modulating mTOR-autophagy pathway. [Abstract]

2026 Jun 23;21(6):e0352120. PMID: 42335126
University of Central Florida

2026.
Blood Neoplasia

From cell lines to PDXs: in vivo confirmation of synergistic drug responses identified in leukemia cell line models. [Abstract]

2026 Apr 9;3(3):100230. PMID: 42294111
bioRxiv

A pharmacological toolkit for human microglia identifies Topoisomerase I inhibitors as immunomodulators for Alzheimer's disease. [Abstract]

2024 Feb 6:2024.02.06.579103. PMID: 38370689
Am J Dig Dis (Madison)

2015;2(2):95-99.
J Clin Toxicol

2014 October 4, 4:5.
J Clin Toxicol 2014, 4:5

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (98.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9782 mL

9.8912 mL

19.7824 mL

5 mM

0.3956 mL

1.9782 mL

3.9565 mL

10 mM

0.1978 mL

0.9891 mL

1.9782 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (4.95 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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Knight SD, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1 (1), 39-43. [Content Brief]

[2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20. [Content Brief]

[3]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. [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	1.9782 mL	9.8912 mL	19.7824 mL	49.4560 mL
	5 mM	0.3956 mL	1.9782 mL	3.9565 mL	9.8912 mL
	10 mM	0.1978 mL	0.9891 mL	1.9782 mL	4.9456 mL
	15 mM	0.1319 mL	0.6594 mL	1.3188 mL	3.2971 mL
	20 mM	0.0989 mL	0.4946 mL	0.9891 mL	2.4728 mL
	25 mM	0.0791 mL	0.3956 mL	0.7913 mL	1.9782 mL
	30 mM	0.0659 mL	0.3297 mL	0.6594 mL	1.6485 mL
	40 mM	0.0495 mL	0.2473 mL	0.4946 mL	1.2364 mL
	50 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9891 mL
	60 mM	0.0330 mL	0.1649 mL	0.3297 mL	0.8243 mL
	80 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6182 mL

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Omipalisib

21 Cited Publications

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Omipalisib

Publications Citing Use of MedChemExpress (MCE) Omipalisib

Ver todos los productos específicos de isoformas PI3K

Ver todos los productos específicos de isoformas mTOR