1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC

Quisinostat (Synonyms: JNJ-26481585)

Cat. No.: HY-15433 Purity: 98.09%
Data Sheet SDS Handling Instructions

Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with IC50 values of 0.11 nM for HDAC1.

For research use only. We do not sell to patients.
Quisinostat Chemical Structure

Quisinostat Chemical Structure

CAS No. : 875320-29-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $132 In-stock
5 mg $120 In-stock
10 mg $210 In-stock
50 mg $420 In-stock
100 mg $620 In-stock
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500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with IC50 values of 0.11 nM for HDAC1.

IC50 & Target

IC50: 0.11 nM (HDAC1), 0.33 nM (HDAC2), 0.64 nM (HDAC4), 0.46 nM (HDAC10), 0.37 nM (HDAC11)[1]

In Vitro

Quisinostat exerts broad-spectrum antiproliferative activity against a wide panel of cancer cell lines including lung, colon, breast, prostate, and ovarian cell lines at nanomolar concentrations. JNJ-26481585 shows activity toward all HDAC enzymes tested with highest potency in vitro observed toward recombinant HDAC1 (IC50, 0.11±0.03 nM), which is comparable with the potency observed toward HDAC1-immunoprecipitated complexes from tumor cells (IC50, 0.16±0.02 nM). Lowest in vitro potency is observed toward HDAC6, 7 and 9 (IC50, 32.1-119 nM) [1].

In Vivo

JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo. JNJ-26481585, a “second-generation” HDAC inhibitor with prolonged pharmacodynamic response in vivo. In agreement with the hypothesis, JNJ-26481585 showed superior efficacy compared with both standard of care agents and first-generation HDAC inhibitors in preclinical tumor models. These studies suggest that an HDAC inhibitor with continuous pharmacodynamic activity may show activity in solid tumor malignancies[1].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

JNJ-26481585 is dissolved in DMSO as 5mM stock solution and diluted with appropriate medium. Human A2780 ovarian tumor cells (107 cells/mouse) are injected s.c. into the inguinal region of male athymic nu/nu CD-1 mice. When palpable tumors are obtained, mice are treated once daily with vehicle (10% hydroxypropyl-β-cyclodextrin) or JNJ-26481585 at 10 mg/kg i.p., and tumor and plasma is harvested at day 1 and at day 7 at the indicated time points (5 mice/point). Levels of AcH3 are determined using a quantitative ELISA (300 ng tumor protein/well) and described on the basis of an indirect response pharmacodynamic model[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

394.47

Formula

C₂₁H₂₆N₆O₂

CAS No.

875320-29-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Quisinostat
Cat. No.:
HY-15433
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