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Fig. 1 · Structure
Cat. No.
A11035
CAS No.
1086062-66-9
Formula
C25H17F2N5O3S
Mol. Weight
505.5

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Omipalisib (GSK2126458)

Cat. No. A11035 CAS 1086062-66-9

mTOR/PI3K Inhibitor,

GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.

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Biological Activity

Target & Activity

Target Activity Value
p110α ki 0.019nM
p110δ ki 0.024nM
p110γ ki 0.06nM
p110β ki 0.13nM
mTORC1 ki 0.18nM
mTORC2 ki 0.3nM

6 targets · Scroll to view more

Cellular Effect

Cell Line Activity Value Description Reference
A549 IC50 0.6 μM Cytotoxicity against human A549 cells after 72 hrs by MTT assay [PMID: 26819001]
A549 IC50 0.86 μM 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 Cytotoxicity against human A549 cells after 72 hrs by MTT assay [PMID: 27448924]
A549 GI50 26.6 nM 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 Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay [PMID: 26819001]
DU-145 GI50 16.3 nM 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 Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay [PMID: 26819001]
HCT-116 IC50 0.14 μM 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 Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay [PMID: 27448924]
HT-29 GI50 19.9 nM 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 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 Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay [PMID: 26819001]
NCI-H1975 GI50 14.4 nM 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 Growth inhibition of human PC3 cells after 72 hrs by sulforhodamine B assay [PMID: 33561608]
PC-3 GI50 197 nM 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 Growth inhibition of human U87MG cells after 72 hrs by sulforhodamine B assay [PMID: 33561608]
U-87MG ATCC IC50 537 nM Cytotoxicity against human U87MG cells after 72 hrs by MTT assay [PMID: 27448924]

17 records · Scroll to view more

In Vitro Studies

IPF BALF cells were incubated with increasing concentrations of Omipalisib. Treatment produced a concentration-dependent reduction in pAkt levels, with a geometric mean IC50 of 0.58 nM. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Concentration-dependent reduction of pAkt in IPF BALF cells

Cell-based study · IPF BALF cells (n=6) [1]

IPF BALF cells were incubated with increasing concentrations of Omipalisib. Treatment produced a concentration-dependent reduction in pAkt levels, with a geometric mean IC50 of 0.58 nM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
pAktS473 signal was normalised to total Akt signalAkt phosphorylation IC50 for 30 min at 37°C: geometric mean IC50=0.58 nM[1]

Literature-Reported Treatment Conditions

Treatment concentration
increasing concentrations
Exposure duration
for 30 min at 37°C
Method
incubated
Vehicle
0.1% DMSO
Methods and source locations

Compound reported in the paper: Omipalisib; Compound label in the paper: GSK-2126458

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > GSK2126458 inhibits Akt phosphorylation in IPF BALF cells (S45); Figure 4 legend (S90, S91)

pAktS473 signal was normalised to total Akt signal: pAktS473 signal was normalised to total Akt signal; comparator: 0.1% DMSO (vehicle control) — Results > GSK2126458 inhibits Akt phosphorylation in IPF BALF cells (S45); Figure 4 legend (S90, S91)

In Vivo Studies

In mice with induced endometriosis following introduction of syngeneic menstrual endometrial tissue into the peritoneum, oral Omipalisib produced much lower peritoneal concentrations of NGF and IGF-1 compared to vehicle-treated mice. In Tsc2+/− BALB/c mice, Omipalisib administered by intraperitoneal injection reduced the median percentage of Ki67-positive tumour cells from 18.13% to 5.82%. [2,3]

Peritoneal NGF in induced endometriosis

Animal study · C57BL/6JNarl mice; induced endometriosis; n = 15 for each group [2]

Mice with induced endometriosis received oral Omipalisib after syngeneic menstrual endometrial tissue was introduced into the peritoneum. Peritoneal concentrations of NGF and IGF-1 were much lower compared to vehicle-treated mice.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
protein levels of NGF (left)Reported result GSK2126458 (75 μg in 100 μL/mouse/day), administered orally five days per week for three weeks: much lower concentrations of NGF and IGF-1 in the peritoneal cavity compared to vehicle-treated mice.[2]

Conditions shared by the study groups

Route
orally
Treatment course
five days per week for three weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Omipalisib 75 μg in 100 μL/mouse/dayvehicle-treated miceGSK2126458 (75 μg in 100 μL/mouse/day), administered orally five days per week for three weeks: much lower concentrations of NGF and IGF-1 in the peritoneal cavity compared to vehicle-treated mice.[2]
Omipalisib 75 μg in 100 μL/mouse/day
Model: C57BL/6JNarl mice; induced endometriosis; n = 15 for each group
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Omipalisib; Compound label in the paper: GSK-2126458

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

2. Materials and Methods > 2.2. Mouse Model of Induced Endometriosis (S3); 3. Results > 3.1. Blockage of Ribosome Biogenesis Led to Reduced Formation of Endometriotic Lesions (S34); 3. Results > 3.3. Anti-Ribosome Biogenesis Agents Suppressed Concentrations of Peritoneal Neurotrophic Factors and Nerve Fiber Growth in Endometriotic Lesions (S55); Figure 1 legend (S73); Figure 4 legend (S98, S99)

protein levels of NGF (left): protein levels of NGF (left); comparator: vehicle-treated mice — 3. Results > 3.1. Blockage of Ribosome Biogenesis Led to Reduced Formation of Endometriotic Lesions (S34); 3. Results > 3.3. Anti-Ribosome Biogenesis Agents Suppressed Concentrations of Peritoneal Neurotrophic Factors and Nerve Fiber Growth in Endometriotic Lesions (S55); Figure 4 legend (S98)

Omipalisib 75 μg in 100 μL/mouse/day · 3. Results > 3.1. Blockage of Ribosome Biogenesis Led to Reduced Formation of Endometriotic Lesions (S34); 3. Results > 3.3. Anti-Ribosome Biogenesis Agents Suppressed Concentrations of Peritoneal Neurotrophic Factors and Nerve Fiber Growth in Endometriotic Lesions (S55)

Tumour cell Ki67 positivity in mice

Animal study · Tsc2+/− BALB/c mice [3]

Tsc2+/− BALB/c mice received Omipalisib at 2 mg/kg by intraperitoneal injection. The median percentage of Ki67-positive tumour cells decreased from 18.13% to 5.82%.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Percentage of Ki67-positive tumour cellspercentage of Ki67-positive cells from 18.13% to 5.82%[3]

Conditions shared by the study groups

Route
intraperitoneal injection
Treatment course
for 2 months from the age of 12 months via intraperitoneal injection 5 times a week
Vehicle
2.5% PEG-400, 2.5% Tween-80 and 2.5% DMSO
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Omipalisib 2 mg/kgvehicleGSK2126458 (2 mg/kg, MTD), for 2 months from the age of 12 months via intraperitoneal injection 5 times a week: reduced the median percentage of Ki67-positive cells from 18.13% to 5.82%.[3]
Omipalisib 2 mg/kg
Model: Tsc2+/− BALB/c mice
Methods and source locations

Compound reported in the paper: Omipalisib; Compound label in the paper: GSK-2126458

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > Effect of GSK2126458 and rapamycin on proliferation and apoptosis in renal tumours of Tsc2+/- mice (S34); MATERIALS AND METHODS > Animal procedures (S45, S47, S50); MATERIALS AND METHODS > Immunohistochemistry (IHC) and Western blot (S62); Figure 6 legend (S95, S97, S99)

Percentage of Ki67-positive tumour cells: Percentage of Ki67-positive tumour cells; comparator: vehicle — RESULTS > Effect of GSK2126458 and rapamycin on proliferation and apoptosis in renal tumours of Tsc2+/- mice (S34); MATERIALS AND METHODS > Animal procedures (S47); Figure 6 legend (S99)

Omipalisib 2 mg/kg · RESULTS > Effect of GSK2126458 and rapamycin on proliferation and apoptosis in renal tumours of Tsc2+/- mice (S34); MATERIALS AND METHODS > Animal procedures (S47)

Peritoneal IGF-1 in induced endometriosis

Animal study · C57BL/6JNarl mice; induced endometriosis; n = 15 for each group [2]

Mice with induced endometriosis received oral Omipalisib after syngeneic menstrual endometrial tissue was introduced into the peritoneum. Peritoneal concentrations of NGF and IGF-1 were much lower compared to vehicle-treated mice.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
IGF-1 (right) in the peritoneal fluid were analyzed by sandwich ELISAReported result GSK2126458 (75 μg in 100 μL/mouse/day), administered orally five days per week for three weeks: much lower concentrations of NGF and IGF-1 in the peritoneal cavity compared to vehicle-treated mice.[2]

Conditions shared by the study groups

Route
orally
Treatment course
five days per week for three weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Omipalisib 75 μg in 100 μL/mouse/dayvehicle-treated miceGSK2126458 (75 μg in 100 μL/mouse/day), administered orally five days per week for three weeks: much lower concentrations of NGF and IGF-1 in the peritoneal cavity compared to vehicle-treated mice.[2]
Omipalisib 75 μg in 100 μL/mouse/day
Model: C57BL/6JNarl mice; induced endometriosis; n = 15 for each group
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Omipalisib; Compound label in the paper: GSK-2126458

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

2. Materials and Methods > 2.2. Mouse Model of Induced Endometriosis (S3); 3. Results > 3.1. Blockage of Ribosome Biogenesis Led to Reduced Formation of Endometriotic Lesions (S34); 3. Results > 3.3. Anti-Ribosome Biogenesis Agents Suppressed Concentrations of Peritoneal Neurotrophic Factors and Nerve Fiber Growth in Endometriotic Lesions (S55); Figure 1 legend (S73); Figure 4 legend (S98, S99)

IGF-1 (right) in the peritoneal fluid were analyzed by sandwich ELISA: IGF-1 (right) in the peritoneal fluid were analyzed by sandwich ELISA; comparator: vehicle-treated mice — 3. Results > 3.1. Blockage of Ribosome Biogenesis Led to Reduced Formation of Endometriotic Lesions (S34); 3. Results > 3.3. Anti-Ribosome Biogenesis Agents Suppressed Concentrations of Peritoneal Neurotrophic Factors and Nerve Fiber Growth in Endometriotic Lesions (S55); Figure 4 legend (S98)

Omipalisib 75 μg in 100 μL/mouse/day · 3. Results > 3.1. Blockage of Ribosome Biogenesis Led to Reduced Formation of Endometriotic Lesions (S34); 3. Results > 3.3. Anti-Ribosome Biogenesis Agents Suppressed Concentrations of Peritoneal Neurotrophic Factors and Nerve Fiber Growth in Endometriotic Lesions (S55)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1086062-66-9
Applications mTOR/PI3K Inhibitor,
Formula C25H17F2N5O3S
Molecular Weight 505.5
Synonyms GSK-2126458
SMILES
COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 96 mg/mL (189.91 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
3 mg/mL
Vehicle
2% DMSO+40% PEG 300+2% Tween 80+ddH2O

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Mercer PF, Woodcock HV, Eley JD, et al. Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF. Thorax (2016). PMID: 27103349 DOI: 10.1136/thoraxjnl-2015-207429 Source material
  2. [2] Chang CY, Chiang AJ, Yan MJ, et al. Ribosome Biogenesis Serves as a Therapeutic Target for Treating Endometriosis and the Associated Complications. Biomedicines (2022). PMID: 35052864 DOI: 10.3390/biomedicines10010185 Source material
  3. [3] Narov K, Yang J, Samsel P, et al. The dual PI3K/mTOR inhibitor GSK2126458 is effective for treating solid renal tumours in Tsc2+/- mice through suppression of cell proliferation and induction of apoptosis. Oncotarget (2017). PMID: 28938574 DOI: 10.18632/oncotarget.17215 Source material

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