Omipalisib (Synonyms: GSK2126458; GSK458)

Name: Omipalisib
Brand: MedChemExpress
SKU: HY-10297
Rating: 5.0 (17 reviews)

Cat. No.: HY-10297 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Omipalisib Chemical Structure

CAS No. : 1086062-66-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 365	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

17 Publications Citing Use of MCE Omipalisib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All mTOR Isoform Specific Products:

View All Isoforms

mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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.

Clinical Trial

Molecular Weight

505.50

Formula

C₂₅H₁₇F₂N₅O₃S

CAS No.

1086062-66-9

Appearance

Solid

Color

Off-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

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 : 50 mg/mL (98.91 mM; Need ultrasonic; 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	1.9782 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

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 (4.95 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(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: 99.93%

Select Batch:

Data Sheet (285 KB) SDS (252 KB)

COA (255 KB) LCMS (97 KB) Elemental Analysis Report (114 KB)

Handling Instructions (2659 KB)

References

[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]

Cell Assay
^[1]

BT474, HCC1954 and T-47D (human breast) are cultured in RPMI-1640 containing 10% fetal bovine serum at 37°C in 5% CO₂ incubator. Cells are split into T75 flask two to three days prior to assay set up at density which yields approximately 70-80% confluence at time of harvest for assay. Cells are harvested using 0.25% trypsin-EDTA. Cell counts are performed on cell suspension using Trypan Blue exclusion staining. Cells are then plated in 384 well black flat bottom polystyrene in 48 μL of culture media per well at 1,000 cells/well. All plates are placed at 5% CO₂, 37°C overnight and Omipalisib (GSK2126458) is added the following day. One plate is treated with CellTiter-Glo for a day 0 (t=0) measurement and read as described below. Omipalisib (GSK2126458) is prepared in clear bottom polypropylene 384 well plates with consecutive two fold dilutions. 4 μL of these dilutions are added to 105 μL culture media, after mixing the solution, 2 μL of these dilutions are added into each well of the cell plates. The final concentration of DMSO in all wells is 0.15%. Cells are incubated at 37°C, 5% CO₂ for 72 hours. Following 72 hours of incubation with Omipalisib each plate is developed and read. CellTiter-Glo reagent is added to assay plates using a volume equivalent to the cell culture volume in the wells. Plates are shaken for approximately two minutes and incubated at room temperature for approximately 30 minutes and chemiluminescent signal is read on the Analyst GT reader. Results are expressed as a percent of the t=0 and plotted against the Omipalisib (GSK2126458) concentration. Cell growth inhibition is determined for Omipalisib (GSK2126458) by fitting the dose response with a 4 or 6 parameter curve fit using XLfit software and determining the concentration that inhibits 50% of the cell growth (gIC₅₀) with the Y min as the t=0 and Y max as the DMSO control. Value from wells with no cells is subtracted from all samples for background correction..

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

References

[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]

Complete Stock Solution Preparation Table

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

Omipalisib 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:

Omipalisib1086062-66-9GSK2126458 GSK458GSK 2126458GSK-2126458GSK458GSK 458GSK-458PI3KmTORAutophagyPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Omipalisib (Synonyms: GSK2126458; GSK458)

Customer Review

Omipalisib Related Antibodies

17 Publications Citing Use of MCE Omipalisib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All mTOR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Omipalisib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Omipalisib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report