Macropa-NH2 hydrochloride

Name: Macropa-NH2 hydrochloride
Brand: MedChemExpress
SKU: HY-111895A
Rating: 5.0 (3 reviews)

Cat. No.: HY-111895A Purity: 99.51%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2443966-86-5

Size	Price	Stock	Quantity
1 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1750	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 4500	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Macropa-NH2 hydrochloride:

Macropa-NCS Get quote
Macropa-NH2 diester Get quote
Macropa-NH2 Get quote
Macropa-NH2 TFA Get quote

3 Publications Citing Use of MCE Macropa-NH2 hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

Molecular Weight

584.06

Formula

C₂₆H₃₈ClN₅O₈

CAS No.

2443966-86-5

Appearance

Solid

Color

White to off-white

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : ≥ 100 mg/mL (171.22 mM)

DMSO : 83.33 mg/mL (142.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

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

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 (sealed storage, away from moisture). 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.51%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.7122 mL	8.5608 mL	17.1215 mL	42.8038 mL
	5 mM	0.3424 mL	1.7122 mL	3.4243 mL	8.5608 mL
	10 mM	0.1712 mL	0.8561 mL	1.7122 mL	4.2804 mL
	15 mM	0.1141 mL	0.5707 mL	1.1414 mL	2.8536 mL
	20 mM	0.0856 mL	0.4280 mL	0.8561 mL	2.1402 mL
	25 mM	0.0685 mL	0.3424 mL	0.6849 mL	1.7122 mL
	30 mM	0.0571 mL	0.2854 mL	0.5707 mL	1.4268 mL
	40 mM	0.0428 mL	0.2140 mL	0.4280 mL	1.0701 mL
	50 mM	0.0342 mL	0.1712 mL	0.3424 mL	0.8561 mL
	60 mM	0.0285 mL	0.1427 mL	0.2854 mL	0.7134 mL
	80 mM	0.0214 mL	0.1070 mL	0.2140 mL	0.5350 mL
	100 mM	0.0171 mL	0.0856 mL	0.1712 mL	0.4280 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.