Phosphatidylinositol 3 Kinase Inhibitor CH5132799 Cas 1007207-67-1
Phosphatidylinositol 3 Kinase Inhibitor CH5132799 Cas 1007207-67-1
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Chemical Information
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Product name:CH5132799 |
Purity:98% min |
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CAS NO:1007207-67-1 |
Solubility:DMSO: 12 mg/mL (31.79 mM) |
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Molecular Formula:C15H19N7O3S |
Package:Package according to customer requirements |
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Molecular Weight:377.421 |
Storage:Store at -20℃ |
Quality control
Remarks
CH5132799, also known as PA-799, is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3K (IC(50)=0.014 M). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice. CH5132799 selectively inhibited class I PI3Ks and PI3K mutants in in vitro kinase assays. Tumors harboring PIK3CA mutations were significantly sensitive to CH5132799 in vitro and were remarkably regressed by CH5132799 in in vivo mouse xenograft models.
Related Products:
Idelalisib; Almorexant HCL; IC-87114; Pictilisib; Pictilisib mesylate; XL147; PIK-90; Omipalisib; Buparlisib; TG100-115; A66; AS-252424; GSK2636771; 3-methyladenine; AS-604850
References
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[1].Tanaka H, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res, 2011, 17(10), 3272-3281.
[2].Ohwada J, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Leff, 2011, 21(6),
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