RO9021

製品コードS7286 バッチS728602

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₂₅N₇O

分子量

355.44

CAS No.

1446790-62-0

Solubility (25°C)*

体外

DMSO

71 mg/mL (199.75 mM)

Ethanol

18 mg/mL (50.64 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 40%PEG300 2 5%Tween80 3 50%ddH2O 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。	0.2mg/ml (0.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% 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。	0.2mg/ml (0.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 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	RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.
in vitro	RO9021 suppresses BCR signaling in human peripheral blood mononuclear cells (PBMC) and whole blood, FcγR signaling in human monocytes, and FcεR signaling in human mast cells and blocks osteoclastogenesis from mouse bone marrow macrophages in vitro. Toll-like Receptor(TLR) 9 signaling in human Bcells was inhibited by this compound, resulting in decreased levels of plasmablasts, immunoglobulin (Ig)M and IgG upon B-cell differentiation. It also potently inhibited type I interferon production by human plasmacytoid dendritic cells (pDC) upon TLR9 activation. This effect is specific to TLR9 as this chemical did not inhibit TLR4- or JAK-STAT-mediated signaling. It does not appreciably inhibit the JAK-STAT pathway^[1].
in vivo	Oral administration of RO9021 inhibits arthritis progression in the mCIA model^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human B-cell line, Ramos
	濃度	1 μM
	反応時間	5 or 15 min
	実験の流れ	The human B-cell line, Ramos, was pretreated with 1 μM RO9021 prior to anti-IgM antibody-induced cross-linking of the BCR. The activation of various BCR signaling components was assessed by western blot using phosphospecific antibodies.
動物実験	動物モデル	C57BL/6 and DBA/1J adult mice
	投薬量	5 and 45 mg/kg daily
	投与方法	oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/24286216/

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：

Spleen tyrosine kinase inhibitors disrupt human neutrophil swarming and antifungal functions [ Microbiol Spectr, 2025, 13(1):e0254921]	PubMed: 39601545
Heterogeneity of Patient-Derived Acute Myeloid Leukemia Cells Subjected to SYK In Vitro Inhibition [ Int J Mol Sci, 2022, 23(23)14706]	PubMed: 36499034

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。