CAS No. : 1007207-67-1

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000098
Molecular Formula:C₁₅H₁₉N₇O₃S
Molecular Weight:377.42
IC50:14/120/500/360 nM (PI3Kα/β/δ/γ)
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Appearance:Solid powder
Purity: > 98%
Cat No:I000098
Cas No:1007207-67-1
MDL No:MFCD22419020

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].

1:Correction: First-in-Human Study of CH5132799, an Oral Class I PI3K Inhibitor, Studying Toxicity, Pharmacokinetics, and Pharmacodynamics, in Patients with Metastatic Cancer. [No authors listed]Clin Cancer Res. 2015 Feb 1;21(3):660. doi: 10.1158/1078-0432.CCR-14-3188. No abstract available. PMID: 25646183 Free Article
2:First-in-human study of CH5132799, an oral class I PI3K inhibitor, studying toxicity, pharmacokinetics, and pharmacodynamics, in patients with metastatic cancer. Blagden S, Omlin A, Josephs D, Stavraka C, Zivi A, Pinato DJ, Anthoney A, Decordova S, Swales K, Riisnaes R, Pope L, Noguchi K, Shiokawa R, Inatani M, Prince J, Jones K, Twelves C, Spicer J, Banerji U.Clin Cancer Res. 2014 Dec 1;20(23):5908-17. doi: 10.1158/1078-0432.CCR-14-1315. Epub 2014 Sep 17. Erratum in: Clin Cancer Res. 2015 Feb 1;21(3):660. Olmin, Aurelius [corrected to Omlin, Aurelius]. PMID: 25231405 Free PMC Article
3:The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Tanaka H, Yoshida M, Tanimura H, Fujii T, Sakata K, Tachibana Y, Ohwada J, Ebiike H, Kuramoto S, Morita K, Yoshimura Y, Yamazaki T, Ishii N, Kondoh O, Aoki Y.Clin Cancer Res. 2011 May 15;17(10):3272-81. doi: 10.1158/1078-0432.CCR-10-2882. Epub 2011 May 10. PMID: 21558396 Free Article
4:Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O, Kuramoto S, Ogawa K, Aoki Y, Shimma N.Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. doi: 10.1016/j.bmcl.2011.01.065. Epub 2011 Jan 22. PMID: 21316229
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