KU-0060648
Modify Date: 2024-01-14 11:41:47
KU-0060648 structure
|
Common Name | KU-0060648 | ||
|---|---|---|---|---|
| CAS Number | 881375-00-4 | Molecular Weight | 582.713 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 819.9±65.0 °C at 760 mmHg | |
| Molecular Formula | C33H34N4O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 449.7±34.3 °C | |
Use of KU-0060648KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively[1]. |
| Name | 1-Piperazineacetamide, 4-ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl] |
|---|---|
| Synonym | More Synonyms |
| Description | KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
PI3Kα:4 nM (IC50) PI3Kβ:0.5 nM (IC50) PI3Kγ:0.594 μM (IC50) PI3Kδ:0.1 nM (IC50) DNA-PK:8.6 nM (IC50) |
| In Vitro | KU-0060648 inhibits cellular DNA-PK auto-phosphorylation with IC50 values of 0.019 μM (MCF7 cells) and 0.17 μM (SW620 cells), and PI-3K-mediated AKT phosphorylation with IC50 values of 0.039 μM (MCF7 cells) and >10 μM (SW620 cells)[1]. KU-0060648 (30-500 nM; 72 hours) dose-dependently inhibits HepG2 cell proliferation, IC50=134.32nM[2]. KU-0060648 (0.1-1 μM；5 days) inhibits cell lines growth with GI50s of 0.95 μM, 0.21 μM, 0.27 μM, 0.41 μM and 1 μM in SW620, LoVo, MCF7, T47D and MDA-MB-231 cells[1]. KU-0060648 (100-300 nM;12 hours) significantly inhibits activation of PI3K (p85 phosphorylation), AKT (Ser-473 and Thr-308 phosphorylations) and mTOR (p70S6K1 Thr-389 phosphorylation) in HepG2/Huh-7 lines and primary human HCC cells[2]. Cell Proliferation Assay[1] Cell Line: Human breast (MCF7, T47D and MDA-MB-231) and colon (LoVo and SW620) cancer cells Concentration: 0.1-1 μM Incubation Time: 5 days Result: Resulted in> 50% inhibition of cell growth in all cell lines. Western Blot Analysis[2] Cell Line: HCC cells; HepG2/Huh-7 cells Concentration: 100-300 nM Incubation Time: 12 hours Result: Inhibited phosphatidylinositol 3-kinase (PI3K) and in-activates AKT-mTOR signaling. |
| In Vivo | KU-0060648 (intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days) dramatically inhibits HepG2 xenograft growth in nude mice, the tumor weights (at week 5) of KU-0060648 group mice are dramatically lighter than that of vehicle control mice and exert a dose-dependent effect in vivo[1]. Animal Model: HepG2 xenograft nude mice model[1] Dosage: 10 and 50 mg/kg Administration: Intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days Result: Suppressed HepG2 xenograft growth in nude mice. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 819.9±65.0 °C at 760 mmHg |
| Molecular Formula | C33H34N4O4S |
| Molecular Weight | 582.713 |
| Flash Point | 449.7±34.3 °C |
| Exact Mass | 582.230103 |
| PSA | 106.50000 |
| LogP | 5.56 |
| Vapour Pressure | 0.0±3.0 mmHg at 25°C |
| Index of Refraction | 1.694 |
| Storage condition | -20℃ |
| 2-(4-Ethyl-1-piperazinyl)-N-{4-[2-(4-morpholinyl)-4-oxo-4H-chromen-8-yl]dibenzo[b,d]thiophen-1-yl}acetamide |
| 1-Piperazineacetamide, 4-ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]dibenzo[b,d]thien-1-yl]- |
| KU 0060648 |