Vipivotide tetraxetan (PSMA-617)

製品コードS8670 バッチS867001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₄₉H₇₁N₉O₁₆
	分子量	1042.14	CAS No.	1702967-37-0
Solubility (25°C)*	体外	Water	100 mg/mL (95.95 mM)


* <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	Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.
in vitro	PSMA-617 demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki = 2.34 ± 2.94 nM on LNCaP; Ki = 0.37 ± 0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated.^[1]
in vivo	The small-animal PET measurements show high tumor-to-background contrasts as early as 1 h after injection. In vivo distribution reveals specific uptake in LNCaP tumors and in the kidneys 1 h after injection. With regard to therapeutic use, PSMA-617 exhibits a rapid clearance from the kidneys from 113.3 ± 24.4 at 1 h to 2.13 ± 1.36 percentage injected dose per gram at 24 h. The favorable pharmacokinetics of the molecule leads to tumor-to-background ratios of 1,058 (tumor to blood) and 529 (tumor to muscle), respectively,24 h after injection.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PSMA-positive LNCaP cell line
	濃度	0–5000 nM
	反応時間	1 h
	実験の流れ	The cell-based assay is performed using 10⁵ LNCaP cells/well. The radioligand (Glu-urea-Lys-(Ahx))₂-[⁶⁸Ga]Ga(HBED-CC)(19) is added as 0.75 nM solution to 12 different concentrations of non-labeled, ^natGa- or ^natLu-labeled PSMA-617 (from 0 to 5000 nM). After 1 hour incubation at 37 ℃, the cells are washed with ice-cold PBS and the cell-bound radioactivity is measured in a gamma counter.
動物実験	動物モデル	8-wk-old BALB/c nu/nu mice which are subcutaneously inoculated into the right trunk with 5 × 10⁶ LNCaP cells in 50% Matrigel.
	投薬量	~30 MBq, 0.5 nM for small-animal PET imaging; ~1 MBq, 0.06 nM for organ distribution.
	投与方法	IV

参考

[1] Benešová M, et al.J Nucl Med. 2015 Jun;56(6):914-20.

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：

Multimodal Radiobioconjugates of Magnetic Nanoparticles Labeled with 44Sc and 47Sc for Theranostic Application [ Pharmaceutics, 2023, 15(3)850]	PubMed: 36986710
Multimodal Radiobioconjugates of Magnetic Nanoparticles Labeled with 44Sc and 47Sc for Theranostic Application [ Pharmaceutics, 2023, 15(3)850]	PubMed: 36986710

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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