Tasquinimod

製品コードS7617 バッチS761704

印刷

化学情報

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 (warmed with 50ºC water bath)

10 mg/mL (24.6 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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] This compound 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	This compound (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]

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]

This compound 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

This compound (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 this compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/23149916/
https://pubmed.ncbi.nlm.nih.gov/16955399/
https://pubmed.ncbi.nlm.nih.gov/24162378/

https://pubmed.ncbi.nlm.nih.gov/20470445/

+ 展开

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。