Omipalisib (GSK2126458) | PI3K/mTOR inhibitor | Probechem Biochemicals

Chemical Structure : Omipalisib

CAS No.: 1086062-66-9

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Omipalisib (GSK458, GSK-2126458, GSK2126458)

货号: PC-42513Not For Human Use, Lab Use Only.

Omipalisib (GSK2126458) is a highly potent dual inhibitor PI3K/mTOR inhibitor with app Ki of 19/130/24/60/180/300 nM for p110α/p110β/p110γ/p110δ/mTORC1/mTORC2 respectively.

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10 mg	￥780	In stock
25 mg	￥1280	In stock
50 mg	￥2180	In stock
100 mg	￥3580	In stock
250 mg		Get quote

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生物&药学活性

Omipalisib (GSK2126458) is a highly potent dual inhibitor PI3K/mTOR inhibitor with app Ki of 19/130/24/60/180/300 nM for p110α/p110β/p110γ/p110δ/mTORC1/mTORC2 respectively.
GSK2126458 shows equivalent activity for p110α mutants E542K/E545K/H1047R with Ki of 8/8/9 nM.
GSK2126458 inhibits pAKT-S473 in T47D cells (IC50=0.41 nM), also inhibits phosphorylation of AKTT308 and p70S6K.
GSK2126458 is active in vivo and orally bioavailable.

物理化学性质&存储条件

分子量	505.496
分子式	C25H17F2N5O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]-

参考文献

1. Knight SD, et al. ACS Med Chem Lett. 2010 Jan 19;1(1):39-43.

2. Khalili JS, et al. Clin Cancer Res. 2012 Aug 15;18(16):4345-55.

3. Munster P, et al. Clin Cancer Res. 2016 Apr 15;22(8):1932-9.

Omipalisib (GSK458, GSK-2126458, GSK2126458)

生物&药学活性

物理化学性质&存储条件

参考文献

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Omipalisib (GSK458, GSK-2126458, GSK2126458)

生物&药学活性

物理化学性质&存储条件

参考文献

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