p-SCN-Macropa
Based on 1 Customer Validation
p-SCN-Macropa is a bifunctional macrocyclic chelator featuring macrocyclic polyamine skeletons and thiocyanate (-SCN) reactive moieties. p-SCN-Macropa can conjugate with monoclonal antibodies including Nimotuzumab (HY-P9968), Rituximab (HY-P9913) and Trastuzumab (HY-P9907)-PEG6-DM1 for 225Ac radiolabeling to construct radioimmunoconjugates. p-SCN-Macropa is applicable for the research of colorectal cancer, HER2-positive breast cancer, TROP-2-positive cancers, and PSMA-positive cancers.
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- Pureté: 96.46%
- CAS No.: 2417821-30-6
- Formule: C35H43N5O9S
- Masse moléculaire:709.81
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
RDC Bifunctional Chelator |
In Vitro
p-SCN-macropa conjugates to Nimotuzumab (HY-P9968) and Rituximab (HY-P9913) with high purity, forming macropa-Nimotuzumab with an estimated 3 p-SCN-macropa molecules per antibody[1].
p-SCN-Macropa-derived[225Ac]Ac-macropa-Nimotuzumab potently inhibits viability of 2D monolayer cultures of DLD-1 (IC50 1.8 nM), SNU-C2B (IC50 3.3 nM), SW620 (IC50 4.6 nM), and HT-29 (IC50 10.1 nM) colorectal cancer cell lines[1].
p-SCN-Macropa-derived[225Ac]Ac-macropa-Nimotuzumab potently inhibits viability of 3D spheroids of DLD-1 (IC50 10.6 nM), SNU-C2B (IC50 14.7 nM), SW620 (IC50 19.5 nM), and HT-29 (IC50 41.5 nM) colorectal cancer cells[1].
p-SCN-macropa (1 MBq/300 μg; 7 days), as a bifunctional chelator in [225Ac]Ac-macropa-Trastuzumab (HY-P9907)-PEG6-DM1, supports high radiochemical purity and excellent in vitro stability in human serum and PBS[2].
p-SCN-macropa-based [225Ac]Ac-macropa-trastuzumab-PEG6-DM1 binds with high affinity to HCC1954 (KD = 36.98 nM) and JIMT-1 (KD = 20.16 nM) HER2-positive breast cancer cells, with HER2 density-dependent internalization that is significantly higher in high HER2-density HCC1954 cells[2].
p-SCN-Macropa (5-10 mg/mL; 90 min at 37°C for conjugation, 5-10 min at room temperature for radiolabeling)-conjugated rosigatamab efficiently chelates 225Ac at room temperature within 5-10 min[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
p-SCN-Macropa-based radioimmunoconjugate [225Ac]Ac-macropa-Nimotuzumab (13 kBq; i.v.) exhibits prominent long-term retention in liver and blood of healthy BALB/c mice, and displays preferential accumulation in DLD-1 colorectal tumor xenografts with a peak uptake of 32.0 % IA/g at day 5 post-administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude BALB/c mice[1]
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Dosage:13 kBq per dose; total cumulative dose 39 kBq
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Administration:i.v.; on days 0, 10, and 20
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Result:Achieved complete tumor regression in 3 of 7 mice.
Left remaining mice with tumor volumes < 100 mm3 at study end.
Extended median survival beyond 130 days, compared to 34 days for the control radioimmunoconjugate group and 27 days for the PBS group.\nAchieved complete tumor regression in 1 of 7 mice.
Led partial tumor growth reduction in 4 mice, with tumor volumes 75, 57, 200, and 550.4 mm3 on day 90.
Extended median survival beyond 90 days, compared to 16 days for the control radioimmunoconjugate group and 12.5 days for the PBS group.\nInduced partial tumor growth response in 2 of 8 mice.
Extended median survival to 41 days, compared to 16 days for the control radioimmunoconjugate group and 24.5 days for the PBS group.
Chemical Information
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CAS No. 2417821-30-6
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Appearance Solid
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Masse moléculaire 709.81
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Formule C35H43N5O9S
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Color White to off-white
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SMILES
OC(C1=NC(CN2CCOCCOCCN(CC3=NC(C(O)=O)=CC=C3)CCOCCOCC2)=CC(OCCC4=CC=C(N=C=S)C=C4)=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
H2O : 25 mg/mL (35.22 mM; Need ultrasonic)
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 and light). 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.
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 and light). 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 and light). 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 | 1 mM | 1.4088 mL | 7.0441 mL | 14.0883 mL | 35.2207 mL |
| 5 mM | 0.2818 mL | 1.4088 mL | 2.8177 mL | 7.0441 mL | |
| 10 mM | 0.1409 mL | 0.7044 mL | 1.4088 mL | 3.5221 mL | |
| 15 mM | 0.0939 mL | 0.4696 mL | 0.9392 mL | 2.3480 mL | |
| 20 mM | 0.0704 mL | 0.3522 mL | 0.7044 mL | 1.7610 mL | |
| 25 mM | 0.0564 mL | 0.2818 mL | 0.5635 mL | 1.4088 mL | |
| 30 mM | 0.0470 mL | 0.2348 mL | 0.4696 mL | 1.1740 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.
p-SCN-Macropa Related Classifications
HY-W1129940 Related Classifications
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