Quisinostat dihydrochloride

SKU: orb1300395

Description

Quisinostat dihydrochloride is a potent and selective second-generation HDAC inhibitor, showing highest activity against HDAC1. It has been investigated in Phase 2 clinical trials for oncology research, with studies demonstrating its effects on cancer cell proliferation and apoptosis in both cellular and animal models.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 875320-31-3
• MW: 467.39
• Purity: 98.50% (May vary between batches)
• Formula: C₂₁H₂₈Cl₂N₆O₂
• SMILES: Cl.Cl.Cn1cc(CNCC2CCN(CC2)c2ncc(cn2)C(=O)NO)c2ccccc12
• Target: HDAC|||Apoptosis|||Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.28 mM);DMSO:73 mg/mL (156.19 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HDAC11:0.37 nM|HDAC10:0.46 nM|HDAC3:4.86 nM|HDAC8:4.26 nM|HDAC6:76.8 nM|HDAC5:3.69 nM|HDAC9:32.1 nM|HDAC2:0.33 nM|HDAC7:119 nM|HDAC1:0.11 nM|HDAC4:0.64 nM
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• In Vivo:
  In an HDAC1-responsive A2780 ovarian tumor screening model, Quisinostat dosing at its maximal tolerated dose (10 mg/kg i.p. and 40 mg/kg p.o.) for 3 days leads to an HDAC1-regulated fluorescence , which predicts tumor growth inhibition. Furthermore, Quisinostat also shows more potent inhibitory effects on the growth of C170HM2 colorectal liver metastases than 5-fluorouracil/Leucovorin.
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• In Vitro:
  Quisinostat exhibits broad spectrum antiproliferative activity in solid and hematologic cancer cell lines, such as all lung, breast, colon, prostate, brain, and ovarian tumor cell lines, with IC50 ranging from 3.1-246 nM, which is more potent than vorinostat, R306465, panobinostat, CRA-24781, or mocetinostat in various human cancer cell lines tested. A recent study shows that Quisinostat promotes myeloma cell death at low nanomolar concentrations by resulting in Mcl-1 depletion and Hsp72 induction.
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• Cell Research:
  All cell lines are obtained from American Type Culture Collection and cultured according to instructions. The effect of HDAC inhibitors on cell proliferation is measured using an MTT. Proliferation of non–small cell lung carcinoma (NSCLC) cell lines is assessed using an Alamar Blue–based assay. For proliferation of hematologic cell lines, cells are incubated for 72 hours and the cytotoxic activity is evaluated by MTS assay. Data are presented as mean IC50 or IC40 ± SD of at least three independent experiments.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Autophagy, deacetylase, Inhibitor, HDAC, HDAC2, HDAC10, HDAC11, HDAC1, HDAC4, hematologic, histone, Histone deacetylases, malignancies, JNJ26854165(Quisinostat), JNJ26854165(Quisinostat) 2HCl, JNJ26481585, JNJ-26481585, JNJ-26481585 2HCl, inhibit, JNJ 26481585, Quisinostat, Quisinostat (JNJ-26481585), Quisinostat (JNJ-26481585) 2HCl, Quisinostat 2HCl, Quisinostat dihydrochloride, Quisinostat Dihydrochloride

Compound Identifiers

PubChem CID

122129987