1007207-67-1 Usage
Description
CH5132799 is a selective class I phosphoinositide 3-kinase (PI3K) inhibitor, specifically designed to target human cancers with oncogenic PIK3CA mutations. It has demonstrated potent antiproliferative and antitumor activity, making it a promising compound for cancer treatment.
Uses
Used in Oncology:
CH5132799 is used as an anticancer agent for targeting human cancers with oncogenic PIK3CA mutations. Its selective inhibition of class I PI3K has shown to effectively suppress tumor growth and proliferation, making it a valuable tool in the fight against cancer.
Additionally, due to its potent antiproliferative and antitumor properties, CH5132799 may also be utilized in combination therapies with other cancer treatments to enhance their efficacy and potentially improve patient outcomes.
Biological Activity
ch5132799 is an inhibitor of class i phosphatidylinositol 3-kinase (pi3k) with ic50 value of 14nm against pi3kα [1].ch5132799 shows inhibitory effect on class i pi3k with ic50 values of 0.014μm, 0.12μm, 0.5μm and 0.036μm against pi3kα, pi3kβ, pi3kδ and pi3kγ, respectively. pi3kα is especially sensitive to ch5132799. ch5132799 is a selective inhibitor. it shows less effect on class ii pi3ks, class iii pi3k and mtor. for other 26 protein kinases, ch5132799 nearly has no inhibition with ic50 value of > 10μm. ch5132799 is found to have potent antitumor activity. it exerts ic50 values of 0.2μm, 0.032μm, 0.056μm and 0.12μm in hct116, kpl-4, t-47d and sk-ov-3 cell lines, respectively. moreover, ch5132799 is oral available in animal models. treatment of ch5132799 shows strong tumor regression at dose of 12.5 mg/kg in mice bearing human breast cancer xenografts [1].
references
[1] ohwada j, ebiike h, kawada h, et al. discovery and biological activity of a novel class i pi3k inhibitor, ch5132799. bioorganic & medicinal chemistry letters, 2011, 21(6): 1767-1772.
Check Digit Verification of cas no
The CAS Registry Mumber 1007207-67-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,7,2,0 and 7 respectively; the second part has 2 digits, 6 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1007207-67:
(9*1)+(8*0)+(7*0)+(6*7)+(5*2)+(4*0)+(3*7)+(2*6)+(1*7)=101
101 % 10 = 1
So 1007207-67-1 is a valid CAS Registry Number.
1007207-67-1Relevant articles and documents
Discovery and biological activity of a novel class i PI3K inhibitor, CH5132799
Ohwada, Jun,Ebiike, Hirosato,Kawada, Hatsuo,Tsukazaki, Masao,Nakamura, Mitsuaki,Miyazaki, Takuya,Morikami, Kenji,Yoshinari, Kiyoshi,Yoshida, Miyuki,Kondoh, Osamu,Kuramoto, Shino,Ogawa, Kotaro,Aoki, Yuko,Shimma, Nobuo
, p. 1767 - 1772 (2011/05/05)
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 (IC50 = 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.
