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CAS 1086062-66-9 GSK-2126458

Name:GSK-2126458 CAS:1086062-66-9 MF:C25H17F2N5O3S MW:505.5 Purity:97% Package:100g;1kg;10kg; Made in China Worldwide Delivery

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Product introduction

Introduction and application of CAS 1086062-66-9 GSK-2126458

Synonyms:

GSK2126458;

HYR-582;

GSK2126458 (HYR-582);

Omipalisib GSK2126458;

2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide;

Specification:

ITEMS	SPECIFICATION
CAS	1086062-66-9
MF	C25H17F2N5O3S
MW	505.5
Melting point	187-189℃
Boiling point	715.6±70.0 °C(Predicted)
Density	1.45
Acidity coefficient	6.23±0.40(Predicted)
Color	White to light yellow
Form	Solid
Storage condition	Refrigerator

Use:

Scientific research synthesis

GSK2126458 effectively inhibits common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer cells, with Ki of 8pM, 8pM, and 9pM respectively. GSK2126458 acts on T47D and BT474 cells and significantly reduces the levels of pAKChemicalbookT-S473, with IC50 of 0.41nM and 0.18nM respectively. Moreover, GSK2126458 acts on a variety of cell lines, including T47D and BT474 breast cancer cell lines, causing cell cycle arrest in the G1 phase and inhibiting cell proliferation, with IC50s of 3nM and 2.4nM respectively.

GSK2126458 reduces pAKT-S473 levels in the BT474 human xenograft model in a dose-dependent manner, and inhibits tumor growth at a low dose of 300 μg/kg in a dose-dependent manner. In addition, GSK2126458 has low blood clearance and good oral bioavailability in four preclinical species (mice, rats, dogs, and monkeys).

Package and transportation:Normal

Package:100g;1kg;10kg;