Ivaltinostat formic
Based on 1 Customer Validation
Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects.
For research use only. We do not sell to patients.
- Purity: 98.04%
- CAS No.: 3078712-42-9
- Formula: C25H35N3O6
- Molecular Weight:473.56
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
HDAC |
Ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) formic inhibits growth of prostate cancer cells (LNCaP, DU145 and PC3 cells). Ivaltinostat (1, 10 μM; 24, 48 hours) formic increases sub-G1 population, and activates caspase-9, -3 and -8[2].
Ivaltinostat (0.001-100 μM; for 72 hours) inhibits proliferation of cholangiocarcinoma cells (IC50s of 0.63, 0.93, and 1.80 μM for SNU-1196, SNU-1196/GR, SNU-308 cells, respectively)[3].
Ivaltinostat (0-10 μM; 48 hours) formic reduces the Calu6 cells proliferation to 40% of untreated cells[4].
Ivaltinostat (3 μM; 1-24 hours) formic significantly increases Calu6 cells proportion in G2/M phase (69%)[4].
Ivaltinostat (0-10 μM; 1-24 hours) formic treatment with low concentration significantly increases the acetylation of histone H3 and H4 in Calu6 cells at various sites in a time-dependent manner up to 24 hours after treatment[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Calu6 cells
-
Concentration:0-10 μM
-
Incubation Time:48 hours
-
Result:Reduced the cell proliferation to 40% of untreated cells.
-
Cell Line:Calu6 cells
-
Concentration:3 μM
-
Incubation Time:1, 8, 12, 24 hours
-
Result:Increased significantly cell proportion in G2/M phase (69%).
-
Cell Line:Calu6 cells
-
Concentration:3 μM
-
Incubation Time:1, 4, 8, 12, 24 hours
-
Result:Increased the acetylation of histone H3 and H4 at various sites in a time-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male 8-week-old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)[5]
-
Dosage:30 mg/kg
-
Administration:PO; daily; for 7 days
-
Result:Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys.
Chemical Information
-
CAS No. 3078712-42-9
-
Appearance Oil
-
Molecular Weight 473.56
-
Formula C25H35N3O6
-
Color Light yellow to yellow
-
SMILES
OC=O.O=C(NCCCN(C)C)/C(COC1=C2C=CC=CC2=CC=C1)=C/CCCCC(NO)=O
-
Synonyms
CG-200745 formic
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL (105.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (105.58 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (105.58 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[5]. Choi HS, et al. Histone deacetylase inhibitor, CG200745 attenuates renal fibrosis in obstructive kidney disease. Sci Rep. 2018 Aug 1;8(1):11546. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.1117 mL | 10.5583 mL | 21.1166 mL | 52.7916 mL |
| 5 mM | 0.4223 mL | 2.1117 mL | 4.2233 mL | 10.5583 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1117 mL | 5.2792 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4078 mL | 3.5194 mL | |
| 20 mM | 0.1056 mL | 0.5279 mL | 1.0558 mL | 2.6396 mL | |
| 25 mM | 0.0845 mL | 0.4223 mL | 0.8447 mL | 2.1117 mL | |
| 30 mM | 0.0704 mL | 0.3519 mL | 0.7039 mL | 1.7597 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5279 mL | 1.3198 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4223 mL | 1.0558 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3519 mL | 0.8799 mL | |
| 80 mM | 0.0264 mL | 0.1320 mL | 0.2640 mL | 0.6599 mL | |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5279 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ivaltinostat formic Related Classifications
HY-16138A Related Classifications
Powered by Bioz