677297-51-7

Basic information

• Product Name: 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol
• Synonyms: 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol;6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine;3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol TG100-115;TG100-115, >=98%;3,3,-(2,4-diaminopteridine-6,7-diyl)diphenol
• CAS NO: 677297-51-7
• Molecular Formula: C₁₈H₁₄N₆O₂
• Molecular Weight: 346.3
• Product Categories: Inhibitors;Akt;mTOR;PI3K
• Mol File: 677297-51-7.mol

Chemical Properties

• Boiling Point: 699.6±65.0 °C(Predicted)
• Appearance: /
• Density: 1.516±0.06 g/cm3(Predicted)
• Solubility: insoluble in H2O; insoluble in EtOH; ≥3.46 mg/mL in DMSO
• PKA: 8.54±0.10(Predicted)
• CAS DataBase Reference: 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol(CAS DataBase Reference)
• NIST Chemistry Reference: 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol(677297-51-7)
• EPA Substance Registry System: 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol(677297-51-7)

Safety Data

• Hazardous Substances Data: 677297-51-7(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol is used as an active pharmaceutical ingredient for the development of novel therapeutic agents. Its unique chemical structure allows it to interact with specific biological targets, making it a promising candidate for the treatment of various diseases.
Used in Cardiovascular Applications:
In the field of cardiology, 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol is used as a potent and selective phosphoinositide 3-kinase gamma/delta (PI3Kγ/δ) inhibitor. This application is significant because it can provide potent cardioprotection, reduce infarct development, and preserve myocardial function, which are crucial for managing and treating heart-related conditions.
Used in Drug Development:
3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol is also utilized in drug development as a key building block for the synthesis of new compounds with potential therapeutic applications. Its chemical versatility enables the creation of a wide range of derivatives that can be tailored to target specific diseases or conditions.

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].

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.

Upstream product

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Relevant articles and documents

Discovery of 3,3′-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction

In studies aimed toward identifying effective and safe inhibitors of kinase signaling cascades that underlie ischemia/reperfusion (I/R) injury, we synthesized a series of pteridines and pyridopyrazines. The design strategy was inspired by the examination

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Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases, inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.