BEZ235, trial size  

別品名 NVP-BEZ 235;BEZ-235;BEZ 235;NVP-BEZ235
分子量 469.5365
CAS RN® 915019-65-7
構造 C30H23N5O
使用目的 BEZ235 is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50 of 4 nM/5 nM/7 nM/75 nM, and 6 nM for p110α/γ/δ/β and mTOR (p70S6K), respectively. IC50 & Target: IC50: 4 nM (p110α), 5 nM (p110γ), 7 nM (p110δ), 75 nM (p110β), 6 nM (mTOR)[1]In Vitro: BEZ235 (NVP-BEZ235) potently inhibits PI3K in an ATP Competitive Manner. NVP-BEZ235 (250 nM) significantly reduced the phosphorylation levels of the mTOR activated kinase p70S6K. NVP-BEZ235 also leads to a reduction of S235/S236P-RPS6 levels with an IC50 of 6.5 nM, suggesting that NVP-BEZ235 can directly inhibit the mTOR kinase, as the kinase domain of mTOR is highly homologous to the one of class IA PI3K. The activity of NVP-BEZ235 against mTOR is confirmed using a biochemical mTOR K-LISA assay (IC50, 20.7 nM)[1]. The IC50s of NVP-BEZ235 for HCT116, DLD-1, and SW480 cell lines are 14.3±6.4, 9.0±1.5, and 12.0±1.6 nM, respectively[2].In Vivo: BEZ235 (NVP-BEZ235) (45 mg/kg, p.o.) treatment induces colonic tumor regression in a GEM model for sporadic PIK3CA wild-type CRC[2]. NVP-BEZ235 (45 mg/kg) is administered to MENX rats (n=2 each group) by oral gavage and animals are sacrificed 1 or 6 hours after treatment. Immunostains for P-AKT and P-S6 show considerable reduction of the two proteins, and particularly of P-S6, 6 hours after administration of NVP-BEZ235 when compares with PEG-treated rats. At 6 hours after treatment, the pituitary adenomas of NVP-BEZ235-treated rats has a proteomic profile significantly different from the tumors of placebo-treated rats[3].
参考文献 Nat Commun. 2017 Jun 8;8:15617.
[注意事項] ※有償サンプルです※有償サンプルについては、1研究室あたり1年間3種各1本までです。


メーカー 品番 包装
MCH HY-50673 0.5 MG
希望販売価格 ¥5,000


当社在庫 なし
納期目安 約10日
保存温度 -20℃




メーカー名 MedChemexpress Co., limited
略号 MCH