For research use only. Not Intended for Therapeutic Use!
|IC50:||14/120/500/360 nM (PI3Kα/β/δ/γ)|
|We would like to match the lowest price on market if possible.|
CH5132799 selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 0.014, 0.12, 0.50, and 0.36 uM, respectively; shows less inhibition of class II PI3Ks, class III PI3ks, and mTOR.
IC50 value: 14/120/500/360 nM (PI3Kα/β/δ/γ)
Prediction of CH5132799 response on the basis of PIK3CA mutations could enable patient stratification in clinical settings. CH5132799 exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM). 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. Cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH5132799. In human tumor cell lines with PI3K pathway activation by mutation, CH5132799 shows potent antiproliferative activity [HCT116(CRC): IC50 = 0.20 lM, KPL-4(BC):13 IC50 = 0.032 lM, T-47D(BC): IC50 = 0.056 lM, SK-OV-3(Ovarian): IC50 = 0.12 lM].