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

Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects.

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Ivaltinostat

Ivaltinostat Chemical Structure

CAS No. : 936221-33-9

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Based on 1 publication(s) in Google Scholar

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Ivaltinostat Related Antibodies

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  • Purity & Documentation

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Description

Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects[1][2][3][4].

IC50 & Target[2]

HDAC

 

In Vitro

Ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) inhibits growth of prostate cancer cells (LNCaP, DU145 and PC3 cells). Ivaltinostat (1, 10 μM; 24, 48 hours) 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) reduces the Calu6 cells proliferation to 40% of untreated cells[4].
Ivaltinostat (3 μM; 1-24 hours) significantly increases Calu6 cells proportion in G2/M phase (69%)[4].
Ivaltinostat (0-10 μM; 1-24 hours) 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 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: 0-10 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) 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

427.54

Formula

C24H33N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (233.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3390 mL 11.6948 mL 23.3896 mL
5 mM 0.4678 mL 2.3390 mL 4.6779 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.85 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

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(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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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. 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 1 mM 2.3390 mL 11.6948 mL 23.3896 mL 58.4741 mL
5 mM 0.4678 mL 2.3390 mL 4.6779 mL 11.6948 mL
10 mM 0.2339 mL 1.1695 mL 2.3390 mL 5.8474 mL
15 mM 0.1559 mL 0.7797 mL 1.5593 mL 3.8983 mL
20 mM 0.1169 mL 0.5847 mL 1.1695 mL 2.9237 mL
25 mM 0.0936 mL 0.4678 mL 0.9356 mL 2.3390 mL
30 mM 0.0780 mL 0.3898 mL 0.7797 mL 1.9491 mL
40 mM 0.0585 mL 0.2924 mL 0.5847 mL 1.4619 mL
50 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1695 mL
60 mM 0.0390 mL 0.1949 mL 0.3898 mL 0.9746 mL
80 mM 0.0292 mL 0.1462 mL 0.2924 mL 0.7309 mL
100 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL
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Ivaltinostat 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:

Ivaltinostat936221-33-9CG-200745CG200745CG 200745HDACMDM-2/p53ApoptosisHistone deacetylaseshydroxamicacidmoietyzinccatalytichistoneH3tubulinp53MDM2p21Waf1/Cip1cholangiocarcinomaSNU-1196SNU-308non-smallcelllungprostateInhibitorinhibitorinhibit

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