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  4. Macropa-NH2 TFA

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.

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

Macropa-NH2 TFA Chemical Structure

Macropa-NH2 TFA Chemical Structure

CAS No. : 2705054-08-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 728 In-stock
Solution
10 mM * 1 mL in DMSO USD 728 In-stock
Solid
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1750 In-stock
50 mg USD 2850 In-stock
100 mg USD 4500 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Macropa-NH2 TFA:

Macropa-NH2 TFA Related Antibodies

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Description

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Macropa-NH2 TFA Related Antibodies
Molecular Weight

661.62

Formula

C28H38F3N5O10
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)C1=NC(CN2CCOCCOCCN(CC3=NC(C(O)=O)=CC=C3)CCOCCOCC2)=CC(N)=C1.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 130 mg/mL (196.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5114 mL 7.5572 mL 15.1144 mL
5 mM 0.3023 mL 1.5114 mL 3.0229 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

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

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.03%

SDS (252 KB)

COA (255 KB) HNMR (313 KB) RP-HPLC (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.5114 mL 7.5572 mL 15.1144 mL 37.7860 mL
5 mM 0.3023 mL 1.5114 mL 3.0229 mL 7.5572 mL
10 mM 0.1511 mL 0.7557 mL 1.5114 mL 3.7786 mL
15 mM 0.1008 mL 0.5038 mL 1.0076 mL 2.5191 mL
20 mM 0.0756 mL 0.3779 mL 0.7557 mL 1.8893 mL
25 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5114 mL
30 mM 0.0504 mL 0.2519 mL 0.5038 mL 1.2595 mL
40 mM 0.0378 mL 0.1889 mL 0.3779 mL 0.9447 mL
50 mM 0.0302 mL 0.1511 mL 0.3023 mL 0.7557 mL
60 mM 0.0252 mL 0.1260 mL 0.2519 mL 0.6298 mL
80 mM 0.0189 mL 0.0945 mL 0.1889 mL 0.4723 mL
100 mM 0.0151 mL 0.0756 mL 0.1511 mL 0.3779 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Macropa-NH2 TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Macropa-NH22705054-08-4OthersInhibitorinhibitorinhibit

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