1198357-79-7
1198357-79-7 structure
- Name: ETP-45658
- Chemical Name: ETP-45658
- CAS Number: 1198357-79-7
- Molecular Formula: C16H17N5O2
- Molecular Weight: 311.34
- Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA-PK
- Create Date: 2022-02-21 16:33:18
- Modify Date: 2024-01-19 22:05:48
-
ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer[1][2].
| Name | ETP-45658 |
|---|
| Description | ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer[1][2]. |
|---|---|
| Related Catalog | |
| Target |
PI3Kα:22.0 nM (IC50) PI3Kδ:39.8 nM (IC50) PI3Kβ:129.0 nM (IC50) PI3Kγ:717.3 nM (IC50) mTOR:152.0 nM (IC50) DNA-PK:70.6 nM (IC50) |
| In Vitro | ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells[1]. 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[1]. ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells[1]. ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC50s of 16.8 nM and 13.1 nM, respectively[1]. ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells[1]. ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells[1]. Western Blot Analysis[1] 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. Reduced the phosphorylation of the mTOR substrate p70 S6K. |
| In Vivo | ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice[1]. |
| References |
| Molecular Formula | C16H17N5O2 |
|---|---|
| Molecular Weight | 311.34 |