Acelarin (Synonyms: NUC-1031)

目录号: HY-100885 纯度: 99.80%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Acelarin（NUC-1031）是广泛使用的核苷类似物吉西他滨的蛋白转化和增强。

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Acelarin Chemical Structure

CAS No. : 840506-29-8

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规格	价格	是否有货
1 mg	￥500	In-stock
5 mg	￥1100	In-stock
10 mg	￥1800	In-stock
25 mg	￥3500	In-stock
50 mg	￥5350	In-stock
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500 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

•Cancer Chemother Pharmacol. 2020 Jun;85(6):1063-1078. [Abstract]

Acelarin 相关产品

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

IC₅₀ & Target

EC50：0.2 nM (DNA synthesis inhibitor)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	0.15 μM Compound: 6f, NUC-1031	Cytostatic activity against human BxPC3 cells after 72 hrs by MTS assay Cytostatic activity against human BxPC3 cells after 72 hrs by MTS assay	[PMID: 24471998]
BXPC-3	IC₅₀	230.1 nM Compound: NUC-1031	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
CCRF-CEM	IC₅₀	0.1 μM Compound: 6f, NUC-1031	Cytostatic activity against human CEM cells after 72 hrs by coulter counter analysis Cytostatic activity against human CEM cells after 72 hrs by coulter counter analysis	[PMID: 24471998]
CWR22R	IC₅₀	130.1 nM Compound: NUC-1031	Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
HEL	CC₅₀	0.34 μM Compound: 2c	Cytotoxicity against human HEL cells assessed as reduce in cell growth incubated for 3 days by coulter counter analysis Cytotoxicity against human HEL cells assessed as reduce in cell growth incubated for 3 days by coulter counter analysis	[PMID: 33479570]
Huh-7	IC₅₀	350.3 nM Compound: NUC-1031	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
JeKo-1	IC₅₀	160.1 nM Compound: NUC-1031	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
L1210	IC₅₀	0.035 μM Compound: 6f, NUC-1031	Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counter analysis Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counter analysis	[PMID: 24471998]
MIA PaCa-2	IC₅₀	0.44 μM Compound: 6f, NUC-1031	Cytostatic activity against human MIAPaCa2 cells after 72 hrs by MTS assay Cytostatic activity against human MIAPaCa2 cells after 72 hrs by MTS assay	[PMID: 24471998]
MIA PaCa-2	IC₅₀	142.2 nM Compound: NUC-1031	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
MM1.S	IC₅₀	31.1 nM Compound: NUC-1031	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
MV4-11	IC₅₀	61 nM Compound: NUC-1031	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation treated for 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36867101]
PANC-1	EC₅₀	162 μM Compound: 6f, NUC-1031	Cytotoxicity against human PANC1 cells assessed as cell viability by MTT assay in presence of hENT1 inhibitor dipyridamole Cytotoxicity against human PANC1 cells assessed as cell viability by MTT assay in presence of hENT1 inhibitor dipyridamole	[PMID: 24471998]
PANC-1	EC₅₀	190 μM Compound: 6f, NUC-1031	Cytotoxicity against human PANC1 cells assessed as cell viability by MTT assay in absence of hENT1 inhibitor dipyridamole Cytotoxicity against human PANC1 cells assessed as cell viability by MTT assay in absence of hENT1 inhibitor dipyridamole	[PMID: 24471998]
RT-112	EC₅₀	0.2 nM Compound: 6f, NUC-1031	Cytotoxicity against human RT112 cells assessed as cell viability by MTT assay in absence of dCK substrate deoxycytidine Cytotoxicity against human RT112 cells assessed as cell viability by MTT assay in absence of dCK substrate deoxycytidine	[PMID: 24471998]
RT-112	EC₅₀	0.7 nM Compound: 6f, NUC-1031	Cytotoxicity against human RT112 cells assessed as cell viability by MTT assay in presence of dCK substrate deoxycytidine Cytotoxicity against human RT112 cells assessed as cell viability by MTT assay in presence of dCK substrate deoxycytidine	[PMID: 24471998]
Vero	CC₅₀	0.02 μM Compound: 2c	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by coulter counter analysis Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by coulter counter analysis	[PMID: 33479570]

体外研究
(In Vitro)

Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited efficacy due to a high susceptibility to cancer cell resistance. The addition of a phosphoramidate motif to the gemcitabine can protect it against many of the key cancer resistance mechanisms. A series of gemcitabine phosphoramidate prodrugs are synthesized and screened for cytostatic activity in a range of different tumor cell lines. Among the synthesized compounds, NUC-1031 is shown to be potent in vitro.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The ProTide demonstrates a significant reduction in tumor size against pancreatic xenograft models compared with the gemcitabine treated group, and less adverse effects on body weight, indicating a better safety profile. Data strongly suggests that the ProTides are not reliant on kinases or nucleoside transporters to exert their activity inside tumor cells and remain stable in the presence of deaminases. The ProTide NUC-1031 is currently advancing through phase I/II clinical studies and has already generated strong pharmacokinetic data that confirm significantly higher intracellular levels of gemcitabine triphosphate, together with promising early efficacy signals and a favorable safety profile. The phosphoramidate chemistry is potentially a great source of new and very effective anticancer agents, bringing a considerable array of advanced treatments specifically designed to overcome cancer resistance mechanisms that will benefit a greater proportion of patients^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

580.47

Formula

C₂₅H₂₇F₂N₄O₈P

CAS 号

840506-29-8

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 36 mg/mL (62.02 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7227 mL	8.6137 mL	17.2274 mL
5 mM	0.3445 mL	1.7227 mL	3.4455 mL
10 mM	0.1723 mL	0.8614 mL	1.7227 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.80%

选择批次：

Data Sheet (633 KB) SDS (393 KB)

COA (204 KB) LCMS (266 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Slusarczyk M, et al. Application of ProTide technology to gemcitabine: a successful approach to overcome the key cancer resistance mechanisms leads to a new agent (NUC-1031) in clinical development. J Med Chem. 2014 Feb 27;57(4):1531-42. [Content Brief]

Cell Assay ^[1]	NUC-1031(5.0 mg) is dissolved in DMSO (0.050 mL) and D₂O (0.15 mL). After recording the control ³¹P NMR at 37 °C, a previously defrosted human, rat, or dog serum (0.30 mL) is added to the sample, which is next submitted to the ³¹P NMR experiments at 37°C. The spectra are recorded every 30 min over 13 h. ³¹P NMR recorded data are processed and analyzed with the Bruker Topspin 2.1 program^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Balb/c nude mice are female, six to eight week old, with the weight of 20 ± 2 g. They are intraperitoneally given NUC-1031 (i.p 0.228 mmol/kg, 132.3 mg/kg, 2×/WK) or vehicle for 2 weeks. NUC-1031 is dissolved in 40% Captisol solution. (40% Captisol is prepared by dissolving 20mg of Captisol with pure water, and made the final volume 50 mL. The solvent is filtered with 0.22 μm filter). Mice are monitored daily for body weight change and clinical symptoms for 2 weeks^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Slusarczyk M, et al. Application of ProTide technology to gemcitabine: a successful approach to overcome the key cancer resistance mechanisms leads to a new agent (NUC-1031) in clinical development. J Med Chem. 2014 Feb 27;57(4):1531-42. [Content Brief]

Acelarin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7227 mL	8.6137 mL	17.2274 mL	43.0686 mL
	5 mM	0.3445 mL	1.7227 mL	3.4455 mL	8.6137 mL
	10 mM	0.1723 mL	0.8614 mL	1.7227 mL	4.3069 mL
	15 mM	0.1148 mL	0.5742 mL	1.1485 mL	2.8712 mL
	20 mM	0.0861 mL	0.4307 mL	0.8614 mL	2.1534 mL
	25 mM	0.0689 mL	0.3445 mL	0.6891 mL	1.7227 mL
	30 mM	0.0574 mL	0.2871 mL	0.5742 mL	1.4356 mL
	40 mM	0.0431 mL	0.2153 mL	0.4307 mL	1.0767 mL
	50 mM	0.0345 mL	0.1723 mL	0.3445 mL	0.8614 mL
	60 mM	0.0287 mL	0.1436 mL	0.2871 mL	0.7178 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Acelarin840506-29-8NUC-1031NUC1031NUC 1031DNA/RNA SynthesisInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Acelarin (Synonyms: NUC-1031)

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献