Macropa-NH2 TFA is the precursor of Macropa-NCS. Macropa-NCS is conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070 and is a promising therapeutic radionuclide applied in the treatment of soft-tissue metastases^[1].

A white suspension of 11o4TFA (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 ℃ 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 ℃. Isothiocyanate 12 was obtained as a mixture of white and pale-yellow solid (0.0547 g) and was stored at –80 ℃ 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 ℃. 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].

661.62

Solid

C₂₈H₃₈F₃N₅O₁₀

2705054-08-4

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

DMSO : 200 mg/mL(302.29 mM;Need ultrasonic)

H₂O : 100 mg/mL(151.14 mM;Need ultrasonic)

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℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 100 mg/mL (151.14 mM); Clear solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 5 mg/mL (7.56 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (7.56 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 5 mg/mL (7.56 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (7.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。