| Bioactivity | 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]. |
| Invitro | DPI-4452 (螯合或不螯合镥离子或镓离子) 与 CAIX 强效且特异性结合，内化程度极低，不会与体外 55 个靶标的脱靶受体发生相互作用[1]。DPI-4452 (111In 标记，8 h) 对表达 hCAIX 和 cCAIX 的中国仓鼠卵巢细胞具有相似的亲和力，明显高于表达 mCAIX 的中国仓鼠卵巢细胞 (KD 分别为 0.3 和 63 nM) [1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> DPI-4452 相关抗体: |
| In Vivo | DPI-4452 在小鼠 (0.7-5.5 mg/kg，静脉注射，单次) 和狗 (0.1 mg/kg，静脉注射，单次) 体内会被迅速消除[1]。DPI-4452 ([177Lu]Lu 标记的，单次剂量100 MBq或每周一次，3次 33 MBq，静脉注射) 可减少HT-29和SK-RC-52人异种移植小鼠模型中的肿瘤负荷[1]。DPI-4452 ([111In]In 标记的，30 MBq, 静脉注射) 在HT-29 CRC 和 SK-RC-52 ccRCC 异种移植瘤小鼠模型中表现出高肿瘤摄取率[1]。在测试剂量范围内，DPI-4452 的质量剂量 (2.5-22.5 μg/kg) 不影响比格犬健康组织的吸收[1]。Mean Plasma Pharmacokinetics of DPI-4452 After Single Injection of DPI-4452 in Beagle DogsAdministration |
| CAS | 2941391-49-5 |
| Formula | C92H132N22O29S3 |
| Molar Mass | 2106.36 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. 1.Massière, et al. Preclinical Characterization of DPI-4452: A68Ga/177Lu Theranostic Ligand for Carbonic Anhydrase IX. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2024, 65(5), 761–767. |
DPI-4452
CAS: 2941391-49-5 F: C92H132N22O29S3 W: 2106.36
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing
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