TG 100713

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Chemical Structure| 925705-73-3 同义名 : -
CAS号 : 925705-73-3
货号 : A427622
分子式 : C12H10N6O
纯度 : 98%+
分子量 : 254.25
MDL号 : MFCD20926347
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(19.67 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
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:50 nM

  • p110β

    PI3Kβ, IC50:215 nM

  • p110α

    PI3Kα, IC50:165 nM

  • p110δ

    PI3Kδ, IC50:24 nM
描述 The phosphoinositide 3-kinase (PI3K) signaling pathway plays a central role in regulating cell growth, proliferation, survival, angiogenesis, metabolism, and motility[2]. The class I PI3-Ks (p110α, p110β, p110δ, and p110γ) are activated by tyrosine kinases or G protein-coupled receptors to generate PIP3, which engages downstream effectors such as the Akt/PDK1 pathway, the Tec family kinases, and the Rho family GTPases[3]. TG100713 is a pan-PI3K inhibitor with IC50s of 50 nM, 24 nM, 165 nM and 215 nM for PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ, respectively. In a vitro study, TG 100713 at 10 M strongly inhibited human umbilical vein endothelial cell proliferation[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.93mL

0.79mL

0.39mL

19.67mL

3.93mL

1.97mL

39.33mL

7.87mL

3.93mL
参考文献

[1]Doukas J, Wrasidlo W, et al. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71.

[2]Yuan J, Mehta PP, Yin MJ, Sun S, Zou A, Chen J, Rafidi K, Feng Z, Nickel J, Engebretsen J, Hallin J, Blasina A, Zhang E, Nguyen L, Sun M, Vogt PK, McHarg A, Cheng H, Christensen JG, Kan JL, Bagrodia S. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011 Nov;10(11):2189-99. doi: 10.1158/1535-7163.MCT-11-0185. Epub 2011 Jul 12. PMID: 21750219.

[3]Martin KJ, Muessel MJ, Pullar CE, Willars GB, Wardlaw AJ. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb 6;10(2):e0116250. doi: 10.1371/journal.pone.0116250. Erratum in: PLoS One. 2015;10(7):e0134924. PMID: 25659107; PMCID: PMC4320071.

[4]Doukas J, Wrasidlo W, Noronha G, Dneprovskaia E, Fine R, Weis S, Hood J, Demaria A, Soll R, Cheresh D. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71. doi: 10.1073/pnas.0606956103. Epub 2006 Dec 15. PMID: 17172449; PMCID: PMC1702529.