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

Ivaltinostat (Synonyms: CG-200745)

Cat. No.: HY-16138
Handling Instructions

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.

For research use only. We do not sell to patients.

Ivaltinostat Chemical Structure

Ivaltinostat Chemical Structure

CAS No. : 936221-33-9

Size Price Stock
5 mg USD 1080 Ask For Quote & Lead Time
10 mg USD 1750 Ask For Quote & Lead Time
25 mg USD 3600 Ask For Quote & Lead Time
50 mg USD 5750 Ask For Quote & Lead Time
100 mg USD 9200 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Other In-stock Forms of Ivaltinostat:

Other Forms of Ivaltinostat:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Ivaltinostat
Cat. No.:
HY-16138
Quantity:
MCE Japan Authorized Agent: