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371935-74-9

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Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE
PI-103 (7) is a potent dual phosphatidylinositol 3-kinase (PI3K)/mTOR inhibitor, but its rapid in vivo metabolism hinders its further clinical development. To improve the bioavailability of PI-103, we designed and synthesized a PI-103 bioisostere, PI-103B
Guo, Shanchun,He, Ling,Luo, Lan,Wang, Guangdi,Zhang, Changde,Zhang, Qiang,Zheng, Shilong,Zhong, Qiu
(2020)
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Synthesis and biological evaluation of pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110α inhibitors
4-Morpholin-4-ylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine 2a was discovered in our chemical library as a novel p110α inhibitor with an IC50 of 1.4 μM. By structural modification of 2a, the 2-aryl-4-morpholinopyrido[3′,2′:4,5]furo[3,2-d]pyrimidin
Hayakawa, Masahiko,Kaizawa, Hiroyuki,Moritomo, Hiroyuki,Koizumi, Tomonobu,Ohishi, Takahide,Yamano, Mayumi,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi,Raynaud, Florence I.,Workman, Paul,Waterfield, Michael D.,Parker, Peter
p. 2438 - 2442
(2008/02/05)

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697736-71-3
C₂₃H₂₂N₄O₅

Chemical Properties

Boiling Point: 520.25 °C at 760 mmHg
Flash Point:268.438 °C
Density: 1.409 g/cm³
Solubility:Soluble in DMSO (up to 40 mg/ml)
Storage Temp.:Desiccate at +4°C
PKA: 9.06±0.10(Predicted)
PSA: 84.51000
LogP: 3.84720

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