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 therapy. 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.

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DPI-4452 Chemical Structure

DPI-4452 Chemical Structure

CAS No. : 2941391-49-5

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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 therapy. 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].

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.
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Storage

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References
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DPI-4452 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:

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

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