 Chemical Structure.png)
Physicochemical Properties
| Molecular Formula | C25H35N3O6 |
| Molecular Weight | 473.56 |
| Related CAS # | Ivaltinostat;936221-33-9 |
| Appearance | Light yellow to yellow ointment |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | HDAC |
| ln Vitro | Prostate cancer cell proliferation is inhibited by ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) formic (LNCaP, DU145 and PC3 cells). Caspases-9, -3, and -8 are activated and the sub-G1 population is increased by ivaltinostat(1, 10 μM; 24, 48 hours) formic[2]. Cholangiocarcinoma cell proliferation is inhibited by ivaltinostat (0.001-100 μM; for 72 hours) (IC50s of 0.63, 0.93, and 1.80 μM for SNU-1196, SNU-1196/GR, and SNU-308 cells, respectively)[3]. The Calu6 cell growth is reduced to 40% of untreated cells when ivaltinostat (0–10 μM) is applied for 48 hours[4]. Calu6 cell fraction in G2/M phase (69%) is greatly increased by ivaltinostat (3 μM; 1-24 hours)[4]. Up to 24 hours after treatment, ivaltinostat (0–10 μM; 1–24 hours) formic therapy at low concentration dramatically enhances the acetylation of histone H3 and H4 in Calu6 cells at different locations in a time-dependent manner[4]. |
| ln Vivo | For seven days, ivaltinostat (CG-200745; po; 30 mg/kg/day) attenuates adhesion molecules, inflammatory cytokines, and oxidative stress in UUO kidneys[5]. |
| Cell Assay |
Cell Proliferation Assay[4] Cell Types: Calu6 cells Tested Concentrations: 0-10 μM Incubation Duration: 48 hrs (hours) Experimental Results: decreased the cell proliferation to 40% of untreated cells. Cell Cycle Analysis[4] Cell Types: Calu6 cells Tested Concentrations: 3 μM Incubation Duration: 1, 8, 12, 24 hrs (hours) Experimental Results: Increased Dramatically cell proportion in G2/M phase(69%). Western Blot Analysis[4] Cell Types: Calu6 cells Tested Concentrations: 3 μM Incubation Duration: 1, 4, 8, 12, 24 hrs (hours) Experimental Results: Increased the acetylation of histone H3 and H4 at various sites in a time-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Male 8weeks old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)[5] Doses: 30 mg/kg Route of Administration: PO; daily; for 7 days Experimental Results: Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys. |
| References |
[1]. Novel histone deacetylase inhibitor CG200745 induces clonogenic cell death by modulating acetylation of p53 in cancer cells. Invest New Drugs. 2012 Apr;30(2):435-42. [2]. A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL. Invest New Drugs. 2012 Aug;30(4):1434-42. [3]. CG200745, an HDAC inhibitor, induces anti-tumour effects in cholangiocarcinoma cell lines via miRNAs targeting the Hippo pathway. Sci Rep. 2017 Sep 7;7(1):10921. [4]. Epigenetic modulation with HDAC inhibitor CG200745 induces anti-proliferation in non-small cell lung cancer cells. PLoS One. 2015 Mar 17;10(3):e0119379. [5]. Histone deacetylase inhibitor, CG200745 attenuates renal fibrosis in obstructive kidney disease. Sci Rep. 2018 Aug 1;8(1):11546. |
Solubility Data
| Solubility (In Vitro) |
H2O :~50 mg/mL (~105.58 mM) DMSO :~50 mg/mL (~105.58 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 50 mg/mL (105.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1117 mL | 10.5583 mL | 21.1166 mL | |
| 5 mM | 0.4223 mL | 2.1117 mL | 4.2233 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1117 mL |