Selonsertib (GS-4997)

製品コードS8292 バッチS829204

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

C₂₄H₂₄FN₇O

分子量

445.49

CAS No.

1448428-04-3

Solubility (25°C)*

体外

DMSO

89 mg/mL (199.78 mM)

Ethanol

11 mg/mL (24.69 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。	4.450mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 89 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。	0.550mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 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	Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.
in vitro	Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor with pIC50 of 8.3.
in vivo	An orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Upon oral administration, ASK1 inhibitor GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. This prevents the phosphorylation of downstream kinases, such as c-Jun N-terminal kinases (JNKs) and p38 mitogen-activated protein kinase (p38 MAPK). By preventing the activation of ASK1-dependent signal transduction pathways, GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	8.3 (pIC50)
	反応時間
	実験の流れ
動物実験	動物モデル	C57BL/6 mice
	投薬量	15, 30, and 60 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/25531162/
https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=773700
https://pubmed.ncbi.nlm.nih.gov/28337323/

https://pubmed.ncbi.nlm.nih.gov/33413667/

+ 展开

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：

Multi-omic human pancreatic islet endoplasmic reticulum and cytokine stress response mapping provides type 2 diabetes genetic insights [ Cell Metab, 2024, 36(11):2468-2488.e7]	PubMed: 39383866
CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer [ Cell Death Dis, 2024, 15(9):662]	PubMed: 39256356
Cetylpyridinium chloride triggers paraptosis to suppress pancreatic tumor growth via the ERN1-MAP3K5-p38 pathway [ iScience, 2024, 27(8):110598]	PubMed: 39211547
ER Stress-Activated HSF1 Governs Cancer Cell Resistance to USP7 Inhibitor-Based Chemotherapy through the PERK Pathway [ Int J Mol Sci, 2024, 25(5)2768]	PubMed: 38474017
ABT‑737 increases cisplatin sensitivity through the ROS‑ASK1‑JNK MAPK signaling axis in human ovarian cancer cisplatin‑resistant A2780/DDP cells [ Oncol Rep, 2024, 52(3)122]	PubMed: 39054955
Abrogating PDK4 activates autophagy-dependent ferroptosis in breast cancer via ASK1/JNK pathway [ J Cancer Res Clin Oncol, 2024, 150(4):218]	PubMed: 38678126
Increasing expression of dual-specificity phosphatase 12 mitigates oxygen-glucose deprivation/reoxygenation-induced neuronal apoptosis and inflammation through inactivation of the ASK1-JNK/p38 MAPK pathway [ Autoimmunity, 2024, 57(1):2345919]	PubMed: 38721693
Co-targeting ASK1 and THRβ synergistically improves steatohepatitis and fibrosis in a MASH animal model [ Biochem Biophys Res Commun, 2024, 705:149739]	PubMed: 38460439
Nitric oxide-induced ribosome collision activates ribosomal surveillance mechanisms [ Cell Death Dis, 2023, 14(7):467]	PubMed: 37495584
Nitric oxide-induced ribosome collision activates ribosomal surveillance mechanisms [ Cell Death Dis, 2023, 14(7):467]	PubMed: 37495584

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。