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上海源葉生物科技有限公司
主營產品： S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶 |
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- 產品描述： Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
- 靶點： PI3Kα:14 nM (IC50);PI3Kα-H1047R:5.6 nM (IC50);PI3Kα-E545K:6.7 nM (IC50);PI3Kα-E542K:6.7 nM (IC50);PI3Kγ:36 nM (IC50);PI3Kβ:120 nM (IC50);PI3Kδ:500 nM (IC50);PI3KC2β:5.3 μM (IC50);mTOR:1.6 μM (IC50)
- 體內研究： Mice bearing BT-474 tumors (n=14) are orally administered 50 mg/kg of Everolimus on a daily basis for 31 days and then randomized. After randomization, the mice are orally administered 50 mg/kg of Everolimus (n=4) and 12.5 mg/kg (n=5), and 25 mg/kg (n=5) of Izorlisib on a daily basis for 7 days. C, the vehicle-, Everolimus, and CH5132799-treated (25 mg/kg) tumors are resected at 4 hours after terminal administration in B, lysed, and analyzed by Western blotting. Izorlisib administration leads to a remarkable regression in a dose-dependent manner of the tumors regrown after the long-term Everolimus treatment. The tumors are resected at the end of treatment and analyzed by Western blotting with respect to PI3K pathway inhibition. Izorlisib suppresses various effectors in the PI3K pathway, including Akt, FoxO1, S6K, S6, and 4E-BP1, whereas Everolimus inhibits only phosphorylation of S6K and S6, both downstream effectors of mTORC1
- 參考文獻：
1. Tanaka H, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res, 2011, 17(10), 3272-3281. 2. Ohwada J, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Leff, 2011, 21(6), 1767-1772.
- 溶解度： Soluble in DMSO
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.65 ml 13.248 ml 26.496 ml 5 mM 0.53 ml 2.65 ml 5.299 ml 10 mM 0.265 ml 1.325 ml 2.65 ml 50 mM 0.053 ml 0.265 ml 0.53 ml
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