2242053-82-1
Chemical Structure
Izorlisib methanesulfonate
Synonym(s): CH5132799 methanesulfonate
- CAS No.: 2242053-82-1
- Formula:C16H23N7O6S2
- Molecular Weight:473.53
InChIKey: QASDCQIMDVXWHK-UHFFFAOYSA-N
SMILES: NC1=NC=C(C2=C3C(N(S(=O)(C)=O)CC3)=NC(N4CCOCC4)=N2)C=N1.CS(=O)(O)=O
Biological Activity: Izorlisib (CH5132799) methanesulfonate is an orally active, selective Class I PI3K inhibitor with an IC50 value of 14 nM against PI3Kα. Izorlisib methanesulfonate specifically inhibits Class I PI3K (particularly PI3Kα and its mutants) and blocks the PI3K/Akt/mTOR pathway; this leads to cell cycle arrest at the G1 phase and apoptosis without triggering feedback activation of Akt by competitively binding to the ATP-binding site of PI3K. Izorlisib methanesulfonate can be used in research on cancers harboring PIK3CA mutations or PTEN loss (such as breast, ovarian, prostate, and endometrial cancers)[1][2].
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Izorlisib methanesulfonate | Izorlisib (CH5132799) methanesulfonate is an orally active, selective Class I PI3K inhibitor with an IC50 value of 14 nM against PI3Kα. Izorlisib methanesulfonate specifically inhibits Class I PI3K (particularly PI3Kα and its mutants) and blocks the PI3K/Akt/mTOR pathway; this leads to cell cycle arrest at the G1 phase and apoptosis without triggering feedback activation of Akt by competitively binding to the ATP-binding site of PI3K. Izorlisib methanesulfonate can be used in research on cancers harboring PIK3CA mutations or PTEN loss (such as breast, ovarian, prostate, and endometrial cancers). | |||||||||||||||||||||
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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 May 15;17(10):3272-81. [Content Brief]
- [2]. Ohwada J, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. [Content Brief]
Keywords
