Tasquinimod

製品コードS7617 バッチS761703

印刷

化学情報

Chemical Structure Synonyms ABR-215050 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H17F3N2O4
分子量 406.36 CAS No. 254964-60-8
Solubility (25°C)* 体外 DMSO 81 mg/mL (199.33 mM)
Ethanol 36 mg/mL warmed with 50ºC water bath (88.59 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
in vitro

Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. [1]

Tasquinimod also targets infiltrating myeloid cells, and modulates local tumour immunity by blocking the interaction between S100A9 and its ligands receptor of advanced glycation end products and Toll-like receptor 4. [3]
in vivo

Tasquinimod (30 mg/kg/d p.o.) shows anti-angiogenic activity and thus causes tumor growth inhibition in mice bearing human and rodent prostate cancer models. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 LNCaP19 cells
濃度 10 μM
反応時間 72 h
実験の流れ

Cells were treated with indicated concentration of drug for 72 h.
動物実験 動物モデル Mice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts.
投薬量 ~30 mg/kg/d
投与方法 p.o.

カスタマーフィードバック

, , Oxid Med Cell Longev, 2017, doi: 10.1155/2017/7150376

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Histone deacetylase inhibitors promote breast cancer metastasis by elevating NEDD9 expression [ Signal Transduct Target Ther, 2023, 8(1):11] PubMed: 36604412
S100A9-CXCL12 activation in BRCA1-mutant breast cancer promotes an immunosuppressive microenvironment associated with resistance to immunotherapy [ Nat Commun, 2022, 13(1):1481] PubMed: 35304461
HDAC5-mediated Smad7 silencing through MEF2A is critical for fibroblast activation and hypertrophic scar formation [ Int J Biol Sci, 2022, 18(15):5724-5739] PubMed: 36263180
The p300/CBP inhibitor A485 normalizes psoriatic fibroblast gene expression in vitro and reduces psoriasis-like skin inflammation in vivo [ J Invest Dermatol, 2022, S0022-202X(22)01937-6] PubMed: 36174717
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147] PubMed: 36371227
Pharmacological and Genetic Inhibition of HDAC4 Alleviates Renal Injury and Fibrosis in Mice [ Front Pharmacol, 2022, 13:929334] PubMed: 35847036
Histone Deacetylase 4 Controls Extracellular Matrix Production in Orbital Fibroblasts from Graves' Ophthalmopathy Patients [ Thyroid, 2021, 10.1089/thy.2020.0948] PubMed: 34235979
In-Depth Immune-Oncology Studies of the Tumor Microenvironment in a Humanized Melanoma Mouse Model [ Int J Mol Sci, 2021, 22(3)E1011] PubMed: 33498319
HDAC3 inhibitor RGFP966 controls bacterial growth and modulates macrophage signaling during Mycobacterium tuberculosis infection [ Tuberculosis (Edinb), 2021, 127:102062] PubMed: 33639591
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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