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Izorlisib

Chemical Structure : Izorlisib

CAS No.: 1007207-67-1

Izorlisib (MEN1611, CH5132799)

Catalog No.: PC-73424Not For Human Use, Lab Use Only.

Izorlisib (MEN1611, CH5132799) is a potent, selective, orally available class I PI3K inhibitor with IC50 of 14/120/400/36 nM against PI3Kα/β/δ/γ, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Izorlisib (MEN1611, CH5132799) is a potent, selective, orally available class I PI3K inhibitor with IC50 of 14/120/400/36 nM against PI3Kα/β/δ/γ, respectively.
Izorlisib (CH5132799) shows less inhibition of class II PI3Ks, class III PI3k and mTOR and also no inhibitory activity (IC50 >10 μM) against 26 protein kinases.
Izorlisib (CH5132799) exhibits more inhibitory activities against PI3Kα with oncogenic mutations E542K (IC50 = 6.7 nM), E545K (IC50 = 6.7 nM) and H1047R (IC50 = 5.6 nM) than wild-type PI3Kα.
Izorlisib (CH5132799) effectively suppresses phosphorylation of Akt PRAS40 and FoxO1/3a and phosphorylation of downstream factors, including S6K, S6 and 4E-BP1 in breast cnacer KPL-4 cells.
Izorlisib (CH5132799) shows potent in vivo antitumor activity in several different xenograft models with PIK3CA mutations.

Physicochemical Properties

M.Wt 377.423
Formula C15H19N7O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-[7-(methanesulfonyl)-2-(morpholin-4-yl)-6,7-dihydro5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amine

References

1. Ohwada J, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72.

2. Tanaka H, et al. Clin Cancer Res. 2011 May 15;17(10):3272-81.

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