Omipalisib

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Cat.No. 6792 - Omipalisib | C25H17F2N5O3S | CAS No. 1086062-66-9
说明: Highly potent PI 3-kinase inhibitor; also potent inhibitor of mTOR and DNA-PK
别名: GSK2126458
化学名: 2,3-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide
纯度: ≥98% (HPLC)
说明书
引用文献
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文献

生物活性

Highly potent PI 3-K inhibitor (IC50 = 0.04 nM). Also inhibits mTOR (Ki = 0.18 - 0.3 nM) and DNA-PK (IC50 = 0.28 nM). Induces G1 cell cycle arrest and inhibits proliferation of some breast cancer cells lines in vitro. Reduces pAKT-S473 levels in and inhibits growth of BT474 breast cancer xenografts in mice. Orally bioavailable.

技术数据

分子量 505.5
公式 C25H17F2N5O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1086062-66-9
PubChem ID 25167777
InChI Key CGBJSGAELGCMKE-UHFFFAOYSA-N
Smiles COC1=NC=C(C2=CC3=C(N=CC=C3C4=CN=NC=C4)C=C2)C=C1NS(=O)(C5=C(C=C(C=C5)F)F)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 10.11 20

制备储备液

以下数据基于产品分子量 505.5。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 9.89 mL 49.46 mL 98.91 mL
1 mM 1.98 mL 9.89 mL 19.78 mL
2 mM 0.99 mL 4.95 mL 9.89 mL
10 mM 0.2 mL 0.99 mL 1.98 mL

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参考文献

参考文献是支持产品生物活性的出版物。

Knight et al (2010) Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Med.Chem.Lett. 1 39 PMID: 24900173


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关键词: Omipalisib, Omipalisib supplier, PI, 3-Kinase, PI3K, mTOR, DNA-PK, highly, potent, inhibitors, inhibits, orally, bioavailable, anticancer, GSK2126458, DNA-dependent, Protein, Kinase, 6792, Tocris Bioscience

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