TAS4464

製品コードS8849 バッチS884902

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
* <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. TAS4464 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 TAS4464 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 TAS4464 administration 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 TAS4464 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 TAS4464 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

[1] Chihoko Yoshimura, et al. Mol Cancer Ther. 2019 Jul;18(7):1205-1216.

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

The CUL5 E3 ligase complex negatively regulates central signaling pathways in CD8+ T cells [ Nat Commun, 2024, 15(1):603]

PubMed: 38242867

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。

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