929016-96-6
Pracinostat (SB939)
CAS: 929016-96-6
Molecular Formula: C20H30N4O2
929016-96-6 - Names and Identifiers
929016-96-6 - Physico-chemical Properties
| Molecular Formula | C20H30N4O2 |
| Molar Mass | 358.48 |
| Density | 1.11 |
| pKa | 8.67±0.23(Predicted) |
| Storage Condition | -20℃ |
| Use | Pracinostat (SB939) is a potent pan-HDAC inhibitor with an IC50 of 40-140 nM, with the exception of HDAC6, which has no inhibitory activity against the type III isoenzyme SIRT I. |
| In vitro study | SB939 had no inhibitory effect on the type III isoenzyme SIRT I. Compared to colon and prostate cancer cell lines, SB939 was more effective on cutaneous T-cell lymphoma cells and leukemia cells with an IC50 of 50 nM (H9 cutaneous T-cell lymphoma cells). To 170 nM (HEL92.1.7 erythroleukemia cells). SB939 at a concentration of 100 μm also had no inhibitory effect on normal human skin fibroblasts. SB939 acts on HCT-116 cells, induces histone H3 acetylation, the acetylation of α-tubulin, reduces phosphorylation of retinal glioma at serine 807/811 site, and induces cell cycle arrest. SB939 had no inhibitory effect on the type III isoenzyme SIRT I. Compared to colon and prostate cancer cell lines, SB939 was more effective on cutaneous T-cell lymphoma cells and leukemia cells with an IC50 of 50 nM (H9 cutaneous T-cell lymphoma cells). To 170 nM (HEL92.1.7 erythroleukemia cells). SB939 at a concentration of 100 μm also had no inhibitory effect on normal human skin fibroblasts. SB939 acts on HCT-116 cells, induces histone H3 acetylation, the acetylation of α-tubulin, reduces phosphorylation of retinal glioma at serine 807/811 site, and induces cell cycle arrest. |
| In vivo study | SB939 has a stronger pharmacokinetic effect and oral bioavailability than SAHA in nude mice. SB939 at a dose of 50 mg/kg treatment of HCT-116 transplanted tumors, selective stimulation of tumor tissue growth. When SB939 was treated at a dose of 100 mg/kg in mice bearing tumors of HCT-116, the tumor growth inhibition rate was 94%. SB939 inhibited the formation of adenomas and increased the density of blood cells in APCmin mice, and the effect was better than that of 5-fluorouracil. SB939 acts on the tumor model (HCT-116, PC-3, A2780, MV4-11, Ramos) and has anticancer activity and high efficiency. SB939 has good absorption, distribution, metabolism, secretion and other drug properties, and is safe. SB939 has stronger pharmacokinetic effect and oral bioavailability than SAHA in nude mice. SB939 at a dose of 50 mg/kg treatment of HCT-116 transplanted tumors, selective stimulation of tumor tissue growth. When SB939 was treated at a dose of 100 mg/kg in mice bearing tumors of HCT-116, the tumor growth inhibition rate was 94%. SB939 inhibited the formation of adenomas and increased the density of blood cells in APCmin mice, and the effect was better than that of 5-fluorouracil. SB939 acts on the tumor model (HCT-116, PC-3, A2780, MV4-11, Ramos) and has anticancer activity and high efficiency. SB939 has good absorption, distribution, metabolism, secretion and other drug properties, and is safe. |
929016-96-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.79 ml | 13.948 ml | 27.896 ml |
| 5 mM | 0.558 ml | 2.79 ml | 5.579 ml |
| 10 mM | 0.279 ml | 1.395 ml | 2.79 ml |
| 5 mM | 0.056 ml | 0.279 ml | 0.558 ml |
Last Update：2024-01-02 23:10:35
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