SF1126 structure
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Common Name | SF1126 | ||
|---|---|---|---|---|
| CAS Number | 936487-67-1 | Molecular Weight | 912.89600 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C41H52N8O16 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of SF1126SF1126 is a clinically relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis[1]. |
| Name | Semafore(SF1126) |
|---|
| Description | SF1126 is a clinically relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis[1]. |
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| Related Catalog | |
| Target |
PI3K/BRD4[1] |
| In Vitro | SF1126 (0-6 µM; 48 hours) inhibits Hep3B, HepG2, SK-Hep1, and Huh7 cells proliferation with IC50s of 5.05, 6.89, 3.14, and 2.14 µM, respectively[1]. SF1126 (1-10 µM; 24 hours) results in cell-cycle arrest with a proportional increase in G0-G1 and a decrease in the number of cells in the S-phase in Hep 3B, Hep G2, SK-Hep1, and Huh7 cells[1]. SF1126 (0.5-2.5 µM; pre-30 minutes) and sorafenib suggests that combined treatment of SF1126 and sorafenib blocks multiple key enzymes in PI3K/AKT/mTOR and Ras/Raf/MAPK pathway[1]. Cell Viability Assay[1] Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells Concentration: 0 µM; 1 µM; 2 µM; 3 µM; 4 µM; 5 µM; 6 µM Incubation Time: 48 hours Result: Resulted in an increased inhibition of HCC proliferation. Cell Cycle Analysis[1] Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells Concentration: 1 µM; 5 µM; 10 µM Incubation Time: 24 hours Result: Induced cell-cycle arrest. Western Blot Analysis[1] Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells Concentration: 0.5 µM and 2.5 µM Incubation Time: Pre-30 mins Result: Suppressed phosphorylation of AKT, p70S6K, 4EBP1, and ERK in all the cell lines together with sorafenib. |
| References |
| Molecular Formula | C41H52N8O16 |
|---|---|
| Molecular Weight | 912.89600 |
| Exact Mass | 912.35000 |
| PSA | 381.50000 |
| LogP | 0.07440 |
| InChIKey | SVNJBEMPMKWDCO-KCHLEUMXSA-N |
| SMILES | NC(N)=NCCCC(NC(=O)CCC(=O)OC[N+]1(c2cc(=O)c3cccc(-c4ccccc4)c3o2)CCOCC1)C(=O)NCC(=O)NC(CC(=O)[O-])C(=O)NC(CO)C(=O)O |