1. Cell Cycle/DNA Damage
    Epigenetics
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. HDAC
    Bcr-Abl
    Apoptosis
  3. Pivanex

Pivanex (Synonyms: AN-9; Pivalyloxymethyl butyrate)

Cat. No.: HY-120508
Handling Instructions

Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.

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

Pivanex Chemical Structure

Pivanex Chemical Structure

CAS No. : 122110-53-6

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Description

Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties[1].

IC50 & Target[1]

HDAC

 

Bcr-Abl

 

In Vitro

Pivanex (100-500 μM) exhibits significant anti-proliferation activity in K562 cells[1].
Pivanex (100-500 μM) also enhances apoptosis and caspase activity in K562 cells[1].
Pivanex (200 μM) induces enhancement in the G2-M phase, a moderate enhancement in the S phase and a slight reduction in G0-G1 of the cell cycle[1].
Pivanex (AN-9) has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines[2].

Cell Viability Assay[1]

Cell Line: K562 cells.
Concentration: 100-500 μM.
Incubation Time: 24 hours.
Result: Reduced the number of K562 viable cells significantly.
100 μM Pivanex with 0.125 or 0.25 μM STI571 reduced the number of viable cells synergistically.

Apoptosis Analysis[1]

Cell Line: K562 cells.
Concentration: 100-500 μM.
Incubation Time: 6-72 hours.
Result: Increased the number of K562 apoptotic cells significantly.
Increased the caspase activity in K562 cells significantly after only 4 h of incubation with 500 μM.
In Vivo

Pivanex (AN9, 200 mg/kg, b.i.d, daily) significantly improves the survival of SMN7 SMA mice. Pivanex (AN9) treatment also marked delays the end stage of disease as defined by the onset of body mass loss[3].

Animal Model: SMN7 SMA mice (SMN2+/+; SMN7+/+; mSmn−/−)[3].
Dosage: 200 mg/kg.
Administration: Oral administration, b.i.d, at 09.00 and 17.00 daily.
Result: Improved the mean lifespan of treated SMN7 SMA mice by 84.6%.
Delayed the onset of body mass loss in SMN7 SMA mice by 94.9%.
Molecular Weight

202.25

Formula

C₁₀H₁₈O₄

CAS No.

122110-53-6

SMILES

CCCC(OCOC(C(C)(C)C)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (494.44 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9444 mL 24.7219 mL 49.4438 mL
5 mM 0.9889 mL 4.9444 mL 9.8888 mL
10 mM 0.4944 mL 2.4722 mL 4.9444 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PivanexAN-9Pivalyloxymethyl butyrateAN9AN 9HDACBcr-AblApoptosisHistone deacetylasesNSCLClungcancerK562ChronicmyelogenousleukemiaCMLspinalmuscularatrophyAcutelymphoblasticALLInhibitorinhibitorinhibit

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