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Acelarin

Name: Acelarin
Brand: TargetMol
SKU: T4060
Price: 398 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.26%

货号 T4060Cas号 840506-29-8

别名 NUC-1031, N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯

Acelarin (NUC-1031) 是核苷类似物吉西他滨的 ProTide 改造和增强产品。

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Acelarin

一键复制产品信息

很棒

纯度: 99.26%

货号 T4060 别名 NUC-1031, N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯Cas号 840506-29-8

Acelarin (NUC-1031) 是核苷类似物吉西他滨的 ProTide 改造和增强产品。

规格	价格	库存
1 mg	¥ 398	现货
2 mg	¥ 573	现货
5 mg	¥ 887	现货
10 mg	¥ 1,470	现货
25 mg	¥ 2,890	现货
50 mg	¥ 4,280	现货
100 mg	¥ 5,970	现货
1 mL x 10 mM (in DMSO)	¥ 983	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

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COA LCMS HNMR 产品操作手册

产品介绍

Acelarin AI Summary

Acelarin exhibits both cytostatic and cytotoxic activities against a broad range of cell lines, including mouse L1210, human CEM, MIAPaCa2, BxPC3, RT112, PANC1, African green monkey Vero, and human HEL cells. It shows prodrug activation in human and dog serum and maintains a metabolic stability in human liver microsomes. Notably, it has a half-life of 8.3 hours and achieves a maximum concentration of 475,000 nM in humans. The compound demonstrates toxicity levels causing various adverse effects such as anemia, fatigue, transaminitis, and thrombocytopenia in patients with solid malignancies, and body weight loss in Balb/c nude mice xenografted with human MIAPaCa2 cells. Additionally, Acelarin shows significant antiviral activity against SARS-CoV-2, Human cytomegalovirus, and Varicella zoster virus by inhibiting virus plaque formation. In terms of cytotoxic potency, it exhibits the highest activity against MIA PaCa-2 cells with an LC50 of 100.0 nM, and moderate activity against KG-1a, HT-29, and BXPC-3 cells with LC50 values of 280.0 nM, 1300.0 nM, and 2290.0 nM, respectively. It also displays good stability in cryopreserved human hepatocytes. The antiproliferative efficacy is evidenced by IC50 values ranging from 31.1 nM to 350.3 nM across different human cancer cell lines and the induction of apoptosis in BXPC-3 cells. In in vivo studies, Acelarin shows significant antitumor activity, with a tumor growth inhibition (TGI) of 55.61% and a relative increment ratio (T/C) of 51.9% in 22Rv1 cells xenografted in castrated male nude Balb/c mice when administered at 50 mg/kg biweekly for 28 days..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Acelarin (NUC-1031) (NUC-1031) is a ProTide enhancement and transformation of the nucleoside analog, gemcitabine.
靶点活性	DNA synthesis:EC50 : 0.2 nM
别名	NUC-1031, N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯

化学信息

分子量	580.47
分子式	C₂₅H₂₇F₂N₄O₈P
CAS No.	840506-29-8
Smiles	FC1(F)[C@@H](O[C@H](COP(OC2=CC=CC=C2)(N[C@H](C(OCC3=CC=CC=C3)=O)C)=O)[C@H]1O)N4C(=O)N=C(N)C=C4
密度	1.51 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 55 mg/mL (94.75 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.45 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7227 mL	8.6137 mL	17.2274 mL	86.1371 mL
5 mM	0.3445 mL	1.7227 mL	3.4455 mL	17.2274 mL
10 mM	0.1723 mL	0.8614 mL	1.7227 mL	8.6137 mL
20 mM	0.0861 mL	0.4307 mL	0.8614 mL	4.3069 mL
50 mM	0.0345 mL	0.1723 mL	0.3445 mL	1.7227 mL