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3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol

3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Structure
3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol
  • CAS No.677297-51-7
  • Chemical Name:3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol
  • CBNumber:CB82484695
  • Molecular Formula:C18H14N6O2
  • Formula Weight:346.34
  • MOL File:677297-51-7.mol
3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Property
  • Boiling point 699.6±65.0 °C(Predicted)
  • Density 1.516±0.06 g/cm3(Predicted)
  • storage temp. Store at -20°C
  • solubility insoluble in H2O; insoluble in EtOH; ≥3.46 mg/mL in DMSO
  • form Yellow powder solid.
  • pka 8.54±0.10(Predicted)
  • color Light yellow to yellow
  • FDA UNII 7ACH1U1E2M
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements

3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Chemical Properties,Usage,Production

  • Uses TG100-115 is a potent and selective phosphoinositide 3-kinase gamma/delta (PI3Kγ/δ) inhibitor. It can provide potent cardioprotection, reduce infarct development, and preserve myocardial function.
  • Definition ChEBI: 3-[2,4-diamino-7-(3-hydroxyphenyl)-6-pteridinyl]phenol is a member of pteridines.
  • Biological Activity tg100-115 is an inhibitor of pi3kγ and pi3kδ with ic50 values of 83 nm and 235 nm, respectively. tg100-115 shows no obvious activity against pi3kα and pi3kβ [1].tg100-115 remarkably reduced eosinophil accumulation, balf levels of classic th2 cytokine il-13, perivascular and peribronchial leukocyte accumulations, and bronchiolar mucin accumulation in a murine model. besides, tg100-115 showed to reduce airway hyper-responsiveness (ahr) by approximately 50% in asthmatic mice. moreover, tg100-115 has been reported to reduce both smoke-and lps-induced neutrophil and lps-induced classic th1 cytokine tnfα accumulations in mice [2].
  • in vivo

    To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition[1].

  • target PI3K-γ
  • IC 50 PI3Kγ: 83 nM (IC50); PI3Kδ: 235 nM (IC50)
  • References [1] doukas j1, wrasidlo w, noronha g, dneprovskaia e, fine r, weis s, hood j, demaria a, soll r, cheresh d. hosphoinositide 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] doukas j1, eide l, stebbins k, racanelli-layton a, dellamary l, martin m, dneprovskaia e, noronha g, soll r, wrasidlo w, acevedo lm, cheresh da. aerosolized phosphoinositide 3-kinase gamma/delta inhibitor tg100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. j pharmacol exp ther. 2009 mar;328(3):758-65.
3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Preparation Products And Raw materials
Raw materials
Preparation Products
3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Suppliers
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3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Spectrum
677297-51-7, 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenolRelated Search:
  • APIs
  • PI3K
  • mTOR
  • Akt
  • Inhibitors
  • 抑制剂
  • 生物试剂
  • 药靶配体
  • 合成有机化合物配体
  • 小分子抑制剂，天然产物
  • 小分子抑制剂
  • 化合物TG100-115,10 MM DMSO 溶液
  • TG100-115,PI3KΓ/Δ抑制剂
  • 3,3'-(2,4-二氨基蝶啶-6,7-二基)二酚
  • 3,3'-(2,4-二氨基-6,7-蝶啶二基)二苯酚
  • 677297-51-7
  • TG100-115, 10 mM in DMSO
  • T 100-115
  • 3,3'-(2,4-Diaminopteridine-6,7-diyl)diphenol
  • PI3K,TG100 115,Phosphoinositide 3-kinase,inhibit,TG-100-115,TG100-115,Inhibitor,TG100115
  • 3,3'-(2,4-Diamino-6,7-pteridinediyl)bispheno
  • Phenol, 3,3'-(2,4-diamino-6,7-pteridinediyl)bis-
  • 100-115
  • CS-427
  • TG100115; TG100 115
  • TG100-115, >=98%
  • 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol TG100-115
  • 6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine
  • TG100-115;TG100115;TG100 115
  • 3,3,-(2,4-diaminopteridine-6,7-diyl)diphenol
  • 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol

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