MSA-2

製品コードS9681 バッチS968101

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₄H₁₄O₅S

分子量

294.32

CAS No.

129425-81-6

Solubility (25°C)*

体外

DMSO

59 mg/mL (200.46 mM)

Ethanol

5 mg/mL (16.98 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.

* <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	MSA-2は、抗腫瘍活性を有する経口利用可能な非ヌクレオチドヒトSTINGアゴニストです。
in vitro	MSA-2 in solution exists as monomers and noncovalent dimers in an equilibrium that strongly favors monomers; the monomers cannot bind STING, whereas the noncovalent dimers bind STING with nanomolar affinity. This compound exhibits substantially higher cellular potency in an acidified tumor microenvironment than normal tissue, owing to increased cellular entry and retention combined with the inherently steep concentration dependence of STING occupancy.
in vivo	MSA-2 is orally available, manifesting similar oral and subcutaneous exposure in mice. In tumor-bearing mice, this compound induced elevations of interferon-b in plasma and tumors by both routes of administration. Well-tolerated regimens of it induced tumor regressions in mice bearing MC38 syngeneic tumors. In tumor models that are moderately or poorly responsive to PD-1 blockade, combinations of this chemical and anti-PD-1 antibody are superior in inhibiting tumor growth and prolonging survival over monotherapy.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	THP-1 cells, mouse macrophages
	濃度	20 μM, 0.16 μM-100 μM
	反応時間	5 h
	実験の流れ	In the primary screen, THP-1 cells are incubated, in 1536-well plates, with test compounds (20 μM) in a RPMI1640-based assay medium in the presence of 5% carbon dioxide at 37°C for 5 hours. IFN-b levels are determined using an AlphaLISA assay and an EnVision Reader and expressed as percentages of IFN-b induced by cGAMP. STING binding activity of compounds is evaluated with a competitive radioligand binding assay using tritiated cGAMP and membrane embedded full-length recombinant human and mouse STING generated in insect cells. STING pathway activation by this compound is assessed by Western blotting, probing phosphorylation status and total protein levels of STING, TBK-1, and IRF3 by using commercially available antibodies.
動物実験	動物モデル	C57BL/6J mice, NSG mice, BALB/c mice, nude NCr mice
	投薬量	25 mg/kg, 40 mg/kg, 50 mg/kg, 60 mg/kg, 80 mg/kg, 160 mg/kg
	投与方法	intra tumor injection, SC, PO

参考

https://pubmed.ncbi.nlm.nih.gov/32820094/

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：

An albumin-prodrug injectable formulation for synergistic cancer immunotherapy [ J Colloid Interface Sci, 2025, 686:1019-1032]	PubMed: 39929010
Structural insights into a shared mechanism of human STING activation by a potent agonist and an autoimmune disease-associated mutation [ Cell Discov, 2022, 8(1):133]	PubMed: 36513640

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。