Maleimide-DTPA
Maleimide-DTPA (MDTPA) is a maleimide-functionalized bifunctional chelator that enables site-specific conjugation via a thioether bond to single-domain antibody fragments (sdAb) containing free cysteine, and mediates 111In radiolabeling. DTPA-2Rs15d-HLC, formed by the conjugation of Maleimide-DTPA with anti-HER2 sdAb 2Rs15d-HLC, retains high affinity for HER2 with a Kd of 5.9 nM, and maintains targeting ability to HER2-positive cells and tumors after 111In labeling. Maleimide-DTPA can be used for radiotracer construction, SPECT molecular imaging, and HER2-positive tumor research.
For research use only. We do not sell to patients.
- CAS No.: 180152-82-3
- Formula: C20H29N5O11
- Molecular Weight:515.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
Maleimide-DTPA (MDTPA) (10-fold molar excess; 37 °C; 2 h) conjugates site-specifically with reduced cysteine-tagged 2Rs15d-HLC to form a homogeneous 1:1 DTPA-sdAb conjugate[1].
Maleimide-DTPA-conjugated 2Rs15d-HLC (10-5 M; 3 h, 90 min, 24 h) maintains high radiochemical stability in both PBS and human plasma at 37 °C after radiolabeling with indium-111[1].
DTPA-2Rs15d-HLC formed by Maleimide-DTPA retains binding affinity for recombinant HER2, with a Kd of 5.9 nM, and the Kd of In-labeled In-DTPA-2Rs15d-HLC is 6.2 nM[1].
Maleimide-DTPA-conjugated, radiolabeled 2Rs15d-HLC (10 nM; 1 h) binds specifically to HER2-positive SKOV3 cells, indicating that its targeting function is retained[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 180152-82-3
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Molecular Weight 515.47
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Formula C20H29N5O11
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SMILES
O=C(NCCN1C(C=CC1=O)=O)CN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC(O)=O
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Synonyms
MDTPA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : ≥ 103 mg/mL (199.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9400 mL | 9.6999 mL | 19.3998 mL | 48.4994 mL |
| 5 mM | 0.3880 mL | 1.9400 mL | 3.8800 mL | 9.6999 mL | |
| 10 mM | 0.1940 mL | 0.9700 mL | 1.9400 mL | 4.8499 mL | |
| 15 mM | 0.1293 mL | 0.6467 mL | 1.2933 mL | 3.2333 mL | |
| 20 mM | 0.0970 mL | 0.4850 mL | 0.9700 mL | 2.4250 mL | |
| 25 mM | 0.0776 mL | 0.3880 mL | 0.7760 mL | 1.9400 mL | |
| 30 mM | 0.0647 mL | 0.3233 mL | 0.6467 mL | 1.6166 mL | |
| 40 mM | 0.0485 mL | 0.2425 mL | 0.4850 mL | 1.2125 mL | |
| 50 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9700 mL | |
| 60 mM | 0.0323 mL | 0.1617 mL | 0.3233 mL | 0.8083 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2425 mL | 0.6062 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1940 mL | 0.4850 mL |
- Maleimide-DTPA
- 180152-82-3
- MDTPA
- Radionuclide-Drug Conjugates (RDCs)
- recombinant HER2 protein
- cysteine
- single-photon emission computed tomography
- 2Rs15d-HLC
- camelid single-domain antibody-fragments
- indium-111
- HER2-positive cancer
- HER2-positive SKOV3 cells
- HER2-positive tumors
- mouse xenograft model
- Inhibitor
- inhibitor
- inhibit