TAS4464

製品コードS8849 バッチS884901

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₁H₂₃FN₆O₆S

分子量

506.51

CAS No.

1848959-10-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (197.42 mM)

Water

Insoluble

Ethanol

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。	5.000mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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。	0.500mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 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	TAS4464 is a highly potent and selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM.
in vitro	TAS4464 selectively inhibits NAE relative to the other E1s UAE and SAE. This compound treatment inhibits cullin neddylation and subsequently induces the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IkBa in human cancer cell lines. Cytotoxicity profiling reveals that it is highly potent with widespread antiproliferative activity not only for cancer cell lines, but also patient-derived tumor cells.^[1]
in vivo	TAS4464 shows prolonged target inhibition in human tumor xenograft mouse models; weekly or twice a week administration of this compound led to prominent antitumor activity in multiple human tumor xenograft mouse models including both hematologic and solid tumors without marked weight loss.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PBMC, AML, DLBCL, SCLC cells. Patient-derived ovary and endometrial cells. Hepatocytes.
	濃度	1 nM, 10 nM, 100 nM, 1000 nM
	反応時間	24 h, 72 h, 6 days
	実験の流れ	PBMC, AML, DLBCL, and SCLC cells are treated with TAS4464 for 72 hours, after which viability is measured. Patient-derived ovary and endometrial cells are maintained in low-attachment plates and treated with this compound or chemotherapeutic agents for 6 days. Cell viability is then measured by using the CellTiter-Glo 3D Cell Viability Assay. Hepatocytes are cultured in Cell-able plate for 10 days and then treated with this compound for 24 hours, after which viability is measured by using CellTiter-Glo 3D Cell Viability Assay.
動物実験	動物モデル	6-week-old female NOD-SCID mice
	投薬量	100 mg/kg, 75 mg/kg
	投与方法	IV

参考

https://pubmed.ncbi.nlm.nih.gov/31092565/

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：

The CUL5 E3 ligase complex negatively regulates central signaling pathways in CD8+ T cells [ Nat Commun, 2024, 15(1):603]	PubMed: 38242867
Glioblastoma vulnerability to neddylation inhibition is dependent on PTEN status, and dysregulation of the cell cycle and DNA replication [ Neurooncol Adv, 2024, 6(1):vdae104]	PubMed: 39119276

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。