| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
HDAC
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|---|---|
| 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].
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| 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]. Oh ET, et al. 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]. Hwang JJ, et al. 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]. Dawoon E Jung, et al. 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]. Chun SM, et al. 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]. Choi HS, et al. Histone deacetylase inhibitor, CG200745 attenuates renal fibrosis in obstructive kidney disease. Sci Rep. 2018 Aug 1;8(1):11546. |
| Molecular Formula |
C25H35N3O6
|
|---|---|
| Molecular Weight |
473.56
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| Related CAS # |
Ivaltinostat;936221-33-9
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 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. View More
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. 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. |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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