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Macropa-NH2 hydrochloride

Catalog No. T11938   CAS 2443966-86-5

Macropa-NCS is conjugated to Anti-Human HER2 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. Macropa-NH2 hydrochloride is the precursor of Macropa-NCS.

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Macropa-NH2 hydrochloride Chemical Structure
Macropa-NH2 hydrochloride, CAS 2443966-86-5
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,810.00
50 mg 6-8 weeks $ 2,360.00
100 mg 6-8 weeks $ 3,730.00
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500 mg 6-8 weeks Inquiry
1 mL * 10 mM (in DMSO) 6-8 weeks $ 738.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Macropa-NCS is conjugated to Anti-Human HER2 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. Macropa-NH2 hydrochloride is the precursor of Macropa-NCS.
In vitro 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].
Molecular Weight 584.06
Formula C26H38ClN5O8
CAS No. 2443966-86-5

Storage

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

Solubility Information

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

TargetMolReferences and Literature

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.

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Keywords

Macropa-NH2 hydrochloride 2443966-86-5 Others MacropaNH2 hydrochloride Macropa-NH-2 hydrochloride Macropa NH2 hydrochloride Macropa-NH2 Hydrochloride inhibitor inhibit

 

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