| Identification | Back Directory | [Name]
HDAC-IN-4 | [CAS]
934828-12-3 | [Synonyms]
AZD9468
HDAC-IN-4
Zabadinostat
CXD101(AZD-9468)
HDAC-IN-4 (CXD101
CXD 101;AZD9468;CXD-101;AZD 9468
CXD 101;AZD9468;CXD-101;AZD 9468;HDAC-IN-4
Benzamide, N-(2-aminophenyl)-4-[1-[(1,3-dimethyl-1H-pyrazol-4-yl)methyl]-4-piperidinyl]- | [Molecular Formula]
C24H29N5O | [MOL File]
934828-12-3.mol | [Molecular Weight]
403.52 |
| Chemical Properties | Back Directory | [Boiling point ]
531.4±50.0 °C(Predicted) | [density ]
1.23±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:31.0(Max Conc. mg/mL);76.82(Max Conc. mM) | [form ]
A crystalline solid | [pka]
13.27±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity[1][2]. | [in vivo]
Zabadinostat substantially reduces tumor size in murine xenograft lung (A549a) and colon (HT29) models at a dose of 50 mg/kg. Tumor reductions are found to be associated with increased histone acetylation and decreased HDAC enzyme activity[2].
For Zabadinostat, after oral dosing in murine and canine models, peak plasma concentrations (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-Zabadinostat at a dose of 1.6 mg/kg (4 μmol/kg), tissue radioactivity peaked 3 to 6 hours after the dose and declined slowly thereafter with Zabadinostat‐related material still present in tissue 21 days after the dose[2]. | [IC 50]
HDAC1: 63 nM (IC50); HDAC3: 550 nM (IC50); HDAC2: 570 nM (IC50) | [References]
[1] Eyre TA, et al. Predictive biomarkers for disease sensitivity in lymphoma - the holy grail for HDAC inhibitors? Oncotarget. 2018 Dec 18;9(99):37280-37281. DOI:10.18632/oncotarget.26460
[2] Eyre TA, et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer. 2019 Jan 1;125(1):99-108. DOI:10.1002/cncr.31791 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
|