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Macropa-NH2 hydrochloride

产品编号 T11938 CAS 2443966-86-5

Macropa-NCS, conjugated to Anti-Human HER2 and the prostate-specific membrane antigen-targeting compound RPS-070, serves as a promising therapeutic radionuclide for soft-tissue metastases treatment. Its precursor, Macropa-NH2 hydrochloride, facilitates its synthesis.

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Macropa-NH2 hydrochloride Chemical Structure

Macropa-NH2 hydrochloride, CAS 2443966-86-5

规格	价格/CNY	货期
25 mg	￥ 18,200	5日内发货
50 mg	￥ 23,700	5日内发货
100 mg	￥ 37,400	5日内发货
200 mg	待询	5日内发货
500 mg	待询	5日内发货
1 mL * 10 mM (in DMSO)	￥ 7,135	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述

体外活性

A white suspension of 11?4TFA (0.1598 g, 0.16 mmol) and Na2CO3 (0.2540 g, 2.4 mmol) was heated at reflux in acetone (10 mL) for 30 min before the slow addition of CSCl2 (305 μL of CSCl2, 85%, Acros Organics).?The resulting orange suspension was heated at reflux for 3 h and then concentrated at 30 °C under reduced pressure to a pale-orange solid.?The solid was dissolved portionwise in 10% ACN/H2O containing 0.2% TFA (8 mL total), filtered, and immediately purified by preparative HPLC using Method C. Pure fractions were combined, concentrated at RT under reduced pressure to remove the organic solvent, and then lyophilized.?Fractions that were not able to be concentrated immediately were frozen at -80 °C.?Isothiocyanate 12 was obtained as a mixture of white and pale-yellow solid (0.0547 g) and was stored at –80 °C in a jar of Drierite.?A stock solution containing 4.4 mg/mL of macropa-NCS was prepared in 0.1 M pH 9.1 NaHCO3 buffer containing 0.154 M NaCl and was stored at -80 °C.?To a portion of Tmab in saline (74 μL) were added macropa-NCS (52 μL) and NaHCO3 buffer (266 μL), so that the final concentrations of Tmab and macropa-NCS were 5.1 mg/mL and 0.59 mg/mL, respectively.?Macropa-NCS was estimated to be in 16-fold molar excess to Tmab based on a molecular weight of 1045.76 g/mol for macropa-NCS (tetra-TFA salt)[1].

分子量	584.06
分子式	C26H38ClN5O8
CAS No.	2443966-86-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 83.33 mg/mL (142.67 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7122 mL	8.5608 mL	17.1215 mL	42.8038 mL
	5 mM	0.3424 mL	1.7122 mL	3.4243 mL	8.5608 mL
	10 mM	0.1712 mL	0.8561 mL	1.7122 mL	4.2804 mL
	20 mM	0.0856 mL	0.428 mL	0.8561 mL	2.1402 mL
	50 mM	0.0342 mL	0.1712 mL	0.3424 mL	0.8561 mL
	100 mM	0.0171 mL	0.0856 mL	0.1712 mL	0.428 mL

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参考文献

1. Thiele NA, et al. An Eighteen-Membered Macrocyclic Ligand for Actinium-225 Targeted Alpha Therapy. Angew Chem Int Ed Engl. 2017 Nov 13;56(46):14712-14717.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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