Macropa-NH2 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Macropa-NH2 hydrochloride 是 Macropa-NCS 的前体。Macropa-NCS 能与曲妥珠单抗 (HY-P9907) 以及前列腺特异性膜抗原靶向化合物 RPS-070 结合，可用于软组织转移瘤的研究。

Macropa-NH2 hydrochloride is the precursor of Macropa-NCS. Macropa-NCS is conjugated to Anti-Human HER2 (HY-P9907) 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.

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).

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Others

Other Targets

Others

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2443966-86-5

584.06

C26H38ClN5O8

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : ≥ 100 mg/mL (171.22 mM) DMSO 中的溶解度 : 83.33 mg/mL (142.67 mM; 超声助溶 )

Cl.Nc1cc(CN2CCOCCOCCN(Cc3cccc(n3)C(O)=O)CCOCCOCC2)nc(c1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years