2. Antibody-drug Conjugate/ADC Related Metabolic Enzyme/Protease
  3. Radionuclide-Drug Conjugates (RDCs) Carbonic Anhydrase
  4. DPI-4452

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).

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

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DPI-4452 Chemical Structure

DPI-4452 Chemical Structure

CAS No. : 2941391-49-5

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Based on 1 publication(s) in Google Scholar

DPI-4452 Related Antibodies

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Description

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[1]. DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

IC50 & Target[1]

hCA IX

0.25 nM (Kd)

In Vitro

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 Related Antibodies
In Vivo

DPI-4452 is rapidly eliminated in mice (0.7-5.5 mg/kg, i.v., single) and dogs (0.1 mg/kg, i.v., single)[1].
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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)
Animal Model: HT-29 and SK-RC-52 human xenograft mouse models (2-5 × 106)[1]
Dosage: [177Lu]Lu-labeled DPI-4452, 100 MBq, single doses; 3 once-weekly 33 MBq doses
Administration: Intravenous injection (i.v.)
Result: Both 100-MBq and three weekly doses of 33-MBq produced maximum tumor growth inhibition in HT-29 xenografts and SK-RC-52 xenografts on days 23 and 36, respectively.
Showed no significant difference in tumor size in SK-RC-52 xenografts at day 36 after treatment with a single 100-MBq or 33-MBq doses.
Molecular Weight

2106.36

Formula

C92H132N22O29S3
CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.4748 mL 2.3738 mL 4.7475 mL
5 mM 0.0950 mL 0.4748 mL 0.9495 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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DPI-4452 Related Classifications

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:

DPI-44522941391-49-5DPI4452DPI 4452Radionuclide-Drug Conjugates (RDCs)Carbonic AnhydraseCarbonate dehydrataseHT-29SK-RC-52xenograftsRadioactivityBurdenAntitumorInhibitorinhibitorinhibit

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