GSK2126458
GSK2126458 (CAS 1086062-66-9) is a small molecule inhibitor targeting PI3K and mTOR, pivotal regulators in cell growth, proliferation, and tumor progression. GSK2126458 demonstrates potent inhibitory activity against PI3K (Ki = 19 pM). In colon cancer cells, combined use with DDR1-IN-1 enhances its antiproliferative effects. Additionally, the compound induces G1 phase arrest in BT474 breast cancer cells and sensitizes nasopharyngeal carcinoma (NPC) cell lines to radiation therapy. In vivo studies show that combining GSK2126458 with radiation or with MEK and BRAF inhibitors suppresses tumor growth. GSK2126458 also influences cellular autophagy pathways, highlighting its utility in oncology-focused biomedical research.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 505.5 |
| Cas No. | 1086062-66-9 |
| Formula | C25H17F2N5O3S |
| Synonyms | GSK212; GSK-2126458; GSK 2126458; GSK-212; GSK 212 |
| Solubility | ≥25.3 mg/mL in DMSO; insoluble in H2O; ≥2.29 mg/mL in EtOH |
| Chemical Name | 2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide |
| SDF | Download SDF |
| Canonical 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
NPC cell lines (CNE-2, 5-8F, and 6-10B) |
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Preparation method |
The solubility of this compound in DMSO is >25.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.003 mmol/L |
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Applications |
GSK2126458 decreased the viability of NPC cells at low nanomolar concentrations and in a concentration- and time-dependent manner. GSK2126458 inhibited migration and invasion of NPC cells. Treatment with GSK2126458 led to an increased percentage of cells in G1 phase. |
| Animal experiment [1]: | |
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Animal models |
Female BALB/c-nu/nu nude mice bearing 5-8F cells |
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Dosage form |
300 μg/kg, Intragastric administration once daily for 5 consecutive days each week. |
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Application |
The combination of IR with GSK2126458 resulted in >50% reduction in xenograft volume and tumor regrowth delay. Treatment with GSK2126458 or PKI-587 alone slightly inhibited tumor growth. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Liu T, Sun Q, Li Q, et al. Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma[J]. Molecular cancer therapeutics, 2015, 14(2): 429-439. |
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| Description | GSK2126458 is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki values of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM, respectively. | |||||
| Targets | p110α | p110δ | p110γ | p110β | mTORC1 | mTORC2 |
| IC50 | 0.019 nM(Ki) | 0.024 nM(Ki) | 0.06 nM(Ki) | 0.13 nM(Ki) | 0.18 nM(Ki) | 0.3 nM(Ki) |
Quality Control & MSDS
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Chemical structure
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