2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC MDM-2/p53 Apoptosis
  4. Ivaltinostat formic

Ivaltinostat formic  (Synonyms: CG-200745 formic)

Cat. No.: HY-16138A Purity: 98.26%
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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.

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Ivaltinostat formic Chemical Structure

Ivaltinostat formic Chemical Structure

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1 mg USD 491 In-stock
5 mg USD 1080 In-stock
10 mg USD 1750 In-stock
25 mg USD 3600 In-stock
50 mg USD 5750 In-stock
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Based on 1 publication(s) in Google Scholar

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Ivaltinostat formic Related Antibodies

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Description

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[1][2][3].

IC50 & Target[1]

HDAC

 

In Vitro

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.

Ivaltinostat formic Related Antibodies

Cell Proliferation Assay[4]

Cell Line: Calu6 cells
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Reduced the cell proliferation to 40% of untreated cells.

Cell Cycle Analysis[4]

Cell Line: Calu6 cells
Concentration: 3 μM
Incubation Time: 1, 8, 12, 24 hours
Result: Increased significantly cell proportion in G2/M phase (69%).

Western Blot Analysis[4]

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.
In Vivo

Ivaltinostat (CG-200745; p.o.; 30?mg/kg/day; for 7 days) formic attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys[5].

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.
Clinical Trial
Molecular Weight

473.56

Formula

C25H35N3O6
Appearance

Oil

Color

Light yellow to yellow

SMILES

OC=O.O=C(NCCCN(C)C)/C(COC1=C2C=CC=CC2=CC=C1)=C/CCCCC(NO)=O
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (105.58 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Ivaltinostat formic Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IvaltinostatCG-200745CG200745CG 200745HDACMDM-2/p53ApoptosisHistone deacetylaseshydroxamicacidmoietyzinccatalytichistoneH3tubulinp53MDM2p21Waf1/Cip1cholangiocarcinomaSNU-1196SNU-308prostatenon-smallcelllungInhibitorinhibitorinhibit

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