2. Antibody-drug Conjugate/ADC Related
  3. Radionuclide-Drug Conjugates (RDCs)
  4. p-SCN-Macropa

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.

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

p-SCN-Macropa

p-SCN-Macropa Chemical Structure

CAS No. : 2417821-30-6

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p-SCN-Macropa Related Antibodies

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Description

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[1][2][3].

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-conjugated nimotuzumab and rituximab (10 kBq/mg) can be quantitatively radiolabeled with 225Ac at high radiochemical purity and yield[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.

p-SCN-Macropa Related Antibodies
In Vivo

p-SCN-Macropa-containing radioimmunoconjugate [225Ac]Ac-macropa-nimotuzumab (13 kBq per dose; i.v.; on days 0, 10, and 20) achieved complete tumor regression in 43% of KRASG12C-mutant DLD-1 and 14% of BRAFV600E-mutant HT-29 colorectal tumor-bearing mice with median survival prolonged over 130 days and 90 days respectively, and prolonged the median survival of KRASG12C-mutant SW620 xenograft mice to 41 days[1].

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.

Animal Model: Athymic nude BALB/c mice[1]
Dosage: 13 kBq per dose; total cumulative dose 39 kBq
Administration: i.v.; on days 0, 10, and 20
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.
Molecular Weight

709.81

Formula

C35H43N5O9S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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p-SCN-Macropa Related Classifications

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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:

p-SCN-Macropa2417821-30-6Radionuclide-Drug Conjugates (RDCs)colorectal cancerHER2-positive breast cancerEGFRSNU-C2BTROP-2-positive cancersHT-29PSMA-positive cancersDLD-1SW620colorectal cancer cellsInhibitorinhibitorinhibit

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