ETP-45658

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ETP 45658 是一种 PI 3-激酶抑制剂（PI 3-Kα、PI 3-Kδ、PI 3-Kβ 和 PI 3-Kγ 的 IC50 值分别为 22、30、129 和 710 nM）。

ETP 45658 is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively).

ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells.ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC50s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively.ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells.ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC50s of 16.8 nM and 13.1 nM, respectively.ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells.ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells. Western Blot Analysis Cell Line:U2OS cells Concentration:10 μM Incubation Time:4 hours Result:Caused a 95% decrease in the phosphorylation of FOXO3a at threonine 32 and a 55% reduction on Gsk3-β at serine 9.

ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice.

ETP 45658 | ETP45658

Cell Cycle/DNA Damage

DNA-PK

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1198357-79-7

311.345

C16H17N5O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (802.98 mM)

Cn1ncc2c(nc(nc12)-c1cccc(O)c1)N1CCOCC1

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(-20℃)

With Ice Pack

≥ 2 years