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Macropa-NH2 hydrochloride 

Cat. No.: HY-111895A Purity: 98.81%
Handling Instructions

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.

For research use only. We do not sell to patients.

Macropa-NH2 hydrochloride Chemical Structure

Macropa-NH2 hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 835 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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

SMILES

O=C(O)C1=NC(CN2CCOCCOCCN(CC3=NC(C(O)=O)=CC=C3)CCOCCOCC2)=CC(N)=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (142.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7122 mL 8.5608 mL 17.1215 mL
5 mM 0.3424 mL 1.7122 mL 3.4243 mL
10 mM 0.1712 mL 0.8561 mL 1.7122 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Macropa-NH2 hydrochloride
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HY-111895A
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