An HDAC1, HDAC2, and HDAC3 inhibitor

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CXD101

Name: CXD101
Brand: -

Item No. 21159

CXD101 (AZD 9468, HDAC-IN-4, Zabadinostat, CAS Number: 934828-12-3)

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

N-(2-aminophenyl)-4-[1-[(1,3-dimethyl-1H-pyrazol-4-yl)methyl]-4-piperidinyl]-benzamide

CAS Number

934828-12-3

Synonyms

AZD 9468
HDAC-IN-4
Zabadinostat

Molecular Formula

C₂₄H₂₉N₅O

Formula Weight

403.5

Purity

≥98%

Formulation

A crystalline solid

Solubility(Learn about Variance in Solubility)

DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.16 mg/mlEthanol: 1 mg/ml

λ_max

232, 298 nm

SMILES

NC1=CC=CC=C1NC(C2=CC=C(C3CCN(CC4=CN(C)N=C4C)CC3)C=C2)=O

InChi Code

InChI=1S/C24H29N5O/c1-17-21(15-28(2)27-17)16-29-13-11-19(12-14-29)18-7-9-20(10-8-18)24(30)26-23-6-4-3-5-22(23)25/h3-10,15,19H,11-14,16,25H2,1-2H3,(H,26,30)

InChi Key

JHDZMASHNBKTPS-UHFFFAOYSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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500 µg

$72

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1 mg

$134

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5 mg

$556

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10 mg

$973

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Product Description

CXD101 is a histone deacetylase 1 (HDAC1), HDAC2, and HDAC3 inhibitor (IC₅₀s = 63, 570, and 550 nM, respectively).¹ It increases acetylation of lysine 9 on histone H3 (H3K9Ac) in Colon-26 colon cancer cells when used at a concentration of 2.7 µM.² CXD101 (50 mg/kg per day) decreases tumor volume, reduces tumor levels of macrophages, and increases tumor levels of Cd4⁺ and Cd8⁺ T cells without affecting body weight in a Colon-26 murine colon cancer model. It increases serum levels of IgG and IgM antibodies thirty days after administration in mice immunized with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike glycoprotein.³

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Eyre, T.A., Collins, G.P., Gupta, A., et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer 125(1), 99-108 (2019).

2. Blaszczak, W., Liu, G., Zhu, H., et al. Immune modulation underpins the anti-cancer activity of HDAC inhibitors. Mol. Oncol. 15(12), 3280-3298 (2021).

3. Liu, G., Barczak, W., Lee, L.N., et al. The HDAC inhibitor zabadinostat is a systemic regulator of adaptive immunity. Commun. Biol. 6(1), 102 (2023).

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