CH5132799 - CAS 1007207-67-1
Catalog number:
1007207-67-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
PI3K
Description:
CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3K; (IC(50)=0.014 uM). 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.
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Synonyms:
CH5132799; CH-5132799; CH 5132799
MSDS:
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Current Developer:
Chugai Pharmaceutical Co., Ltd
1.Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.
Ohwada J1, 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.
Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was drastically improved by replacing phenol with aminopyrimidine moiety. CH5132799, a novel class I PI3K inhibitor, 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.
2.First-in-human study of CH5132799, an oral class I PI3K inhibitor, studying toxicity, pharmacokinetics, and pharmacodynamics, in patients with metastatic cancer.
Blagden S1, Omlin A, Josephs D3, Stavraka C1, Zivi A2, Pinato DJ1, Anthoney A4, Decordova S5, Swales K5, Riisnaes R5, Pope L5, Noguchi K6, Shiokawa R6, Inatani M6, Prince J7, Jones K7, Twelves C4, Spicer J3, Banerji U8. Clin Cancer Res. 2014 Dec 1;20(23):5908-17. doi: 10.1158/1078-0432.CCR-14-1315. Epub 2014 Sep 17.
PURPOSE: This phase I dose-escalation study investigated the maximum-tolerated dose (MTD), dose-limiting toxicities (DLT), safety, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary clinical activity of CH5132799.
3.The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations.
Tanaka H1, 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.
PURPOSE: The phosphatidylinositol 3-kinase (PI3K) pathway plays a central role in cell proliferation and survival in human cancer. PIK3CA mutations, which are found in many cancer patients, activate the PI3K pathway, resulting in cancer development and progression. We previously identified CH5132799 as a novel PI3K inhibitor. Thus, this study aimed to clarify the biochemical and antitumor activity of CH5132799 and elucidate the correlation between CH5132799 response and genetic alterations in the PI3K pathway.
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CAS 1007207-67-1 CH5132799

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