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Eganelisib

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Chemical Structure| 1693758-51-8 同义名 : IPI-549
CAS号 : 1693758-51-8
货号 : A175847
分子式 : C30H24N8O2
纯度 : 99%+
分子量 : 528.564
MDL号 : MFCD30533720
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(47.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:16 nM
描述 PI3Ks are divided into three classes (I, II, and III) based on substrate specificity, sequence homology, and types of regulatory subunits. Class I PI3Ks are further divided into Class IA and Class IB. Class IB of PI3Ks containing the only member, PI3Kγ, is activated primarily by G-protein coupled receptors. The PI3Kγ isoform is mainly expressed in immune cells. Preclinical studies suggest that PI3Kγ inhibition in tumor-associated myeloid cells may be effective to prevent tumor growth. IPI-549 is a potent inhibitor of PI3Kγ (IC50 = 16 nM, measured by Promega ADP-Glo Max assay kit) with >100-fold selectivity over other lipid and protein kinases. IPI-549 shows excellent PI3Kγ potency (IC50 = 1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold) measured by cellular phospho-AKT inhibition assays in SKOV-3, 786-O, RAW 264.7, and RAJI cells. Also, IPI-549 inhibited PI3Kγ-dependent BMDM migration in a dose-dependent manner in vitro. 0.1 - 3 mg/kg oral treatment of IPI-549 significantly reduced neutrophil migration in a dose-dependent manner while a significant inhibition of PI3Kγ can be observed in the mouse air pouch model. IPI-549 is currently in Phase 1 clinical evaluation of advanced solid tumors[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.46mL

1.89mL

0.95mL

18.92mL

3.78mL

1.89mL
参考文献

[1]Evans CA, Liu T, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7.

[2]Kaneda MM, Messer KS, et al. PI3Kγ is a molecular switch that controls immune suppression. Nature. 2016 Nov 17;539(7629):437-442.

[3]De Vera AA, Gupta P, et al. Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo. Cancer Lett. 2019 Feb 1;442:91-103.