DPI-4452
Based on 1 Customer Validation
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models. DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- Pureza: 99.30%
- No. CAS: 2941391-49-5
- Fòrmula: C92H132N22O29S3
- Peso molecular:2106.36
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Almacenamiento:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas Radionuclide-Drug Conjugates (RDCs)
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Actividad biológica
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hCA IX 0.25 nM (Kd) |
DPI-4452 (with or without chelating lutetium or gallium ions) binds potently and specifically to CAIX with minimal internalization without interaction with an in vitro off-target receptor panel of 55 targets[1].
DPI-4452 (111In-labeled, 8 h) has a similar affinity for Chinese hamster ovary cells expressing hCAIX and cCAIX, markedly higher than that of Chinese hamster ovary cells expressing mCAIX (KD: 0.3 and 63 nM, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DPI-4452 ([177Lu]Lu-labeled, single doses of 100 MBq or 3 once-weekly 33 MBq doses, i.v.) reduces tumor burden in HT-29 and SK-RC-52 human xenograft mouse models[1].
DPI-4452 ([111In]In-labeled, 30 MBq, i.v.) exhibits high tumor uptake in the HT-29 CRC and SK-RC-52 ccRCC xenograft tumor mouse models[1].
DPI-4452 mass dose (2.5-22.5 μg/kg) does not affect uptake in healthy tissues in the tested dose range in Beagle dogs[1].
Mean Plasma Pharmacokinetics of DPI-4452 After Single Injection of DPI-4452 in Beagle Dogs
| Administration | Dose (mg/kg) | Sex | C5 min (ng/mL) | tlast (h) | AUCinf (h × ng/mL) | ||||||||||||||||||||||||||||||||||||||
| i.v. | 0.016 | Female | 37.7 (6.83) | 1 (1-1) | 12.4 (2.13) | ||||||||||||||||||||||||||||||||||||||
| i.v. | 0.016 | Male | 43.5 (2.75) | 1 (1-1) | 14 (1.29) | ||||||||||||||||||||||||||||||||||||||
| i.v. | 0.08 | Female | 346 (34.8) | 3 (2-3) | 144 (15.3) | ||||||||||||||||||||||||||||||||||||||
| i.v. | 0.08 | Male | 332 (14.7) | 2 (2-3) | 132 (5.49) | ||||||||||||||||||||||||||||||||||||||
| i.v. | 0.4 | Female | 1760 (180) | 3 (3-3) | 771 (40.6) | ||||||||||||||||||||||||||||||||||||||
| i.v. | 0.4 | Male | 1840 (257) | 3 (3-3) | 854 (120) |
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 50 mg/mL (23.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (289 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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Instrucciones de manejo (2659 KB)
Referencias
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.4748 mL | 2.3738 mL | 4.7475 mL | 11.8688 mL |
| 5 mM | 0.0950 mL | 0.4748 mL | 0.9495 mL | 2.3738 mL | |
| 10 mM | 0.0475 mL | 0.2374 mL | 0.4748 mL | 1.1869 mL | |
| 15 mM | 0.0317 mL | 0.1583 mL | 0.3165 mL | 0.7913 mL | |
| 20 mM | 0.0237 mL | 0.1187 mL | 0.2374 mL | 0.5934 mL |
DPI-4452 Related Classifications
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