MIP-1095
MIP-1095 (RPS-001) is a PSMA inhibitor with a Ki value of 0.24 nM. MIP-1095 binds to PSMA with high affinity and can be internalized into PSMA-expressing cancer cells. When radiolabeled with 123I, 124I or 131I, MIP-1095 enables SPECT/CT imaging, PET/CT imaging or targeted radiation delivery, respectively. 131I-MIP-1095 can alter serum PSA levels and relieve bone pain. MIP-1095 can be used in research related to metastatic castration-resistant prostate cancer.
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- CAS. Nr.: 949575-22-8
- Formel: C19H25IN4O8
- Molecular Weight:564.33
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| LNCaP | IC50 |
10 nM
Compound: 20
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Inhibition of [131I]DCIT from PSMA in human LNCAP cells
Inhibition of [131I]DCIT from PSMA in human LNCAP cells
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[PMID: 19111054] |
MIP-1095 (1-10000 nM; 30 minutes) potently inhibits the NAALADase activity of PSMA in human prostate cancer LNCaP cell lysates with a Ki of 0.24 nM[1].
[123I]MIP-1095 (3 nM; 1 hour) binds specifically to PSMA-positive human prostate cancer LNCaP cells but not to PSMA-negative human prostate cancer PC3 cells, with binding blocked by non-radiolabeled MIP-1095 or PMPA[1].
[123I]MIP-1095 (100 nM; 0-2 hour) undergoes time- and temperature-dependent internalization into human prostate cancer LNCaP cells via endocytosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fox Chase SCID (male)[1]
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Dosage:1 mCi/mouse
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Administration:i.v. tail vein
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Result:Showed high, selective uptake in PSMA-expressing tissues: LNCaP tumors and kidneys at 4 hours post-injection.
Detected PC3 PIP (PSMA+) tumors but not PC3 flu (PSMA-) tumors at 2 hours post-injection.
Chemical Information
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CAS. Nr. 949575-22-8
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Molecular Weight 564.33
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Formel C19H25IN4O8
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCCCNC(NC1=CC=C(I)C=C1)=O)=O
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Synonyms
RPS-001
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Hillier SM, et al. Preclinical evaluation of novel glutamate-urea-lysine analogues that target prostate-specific membrane antigen as molecular imaging pharmaceuticals for prostate cancer. Cancer research. 2009 Sep 01;69(17):6932-40. [Content Brief]
[2]. Zechmann CM, et al. Radiation dosimetry and first therapy results with a (124)I/ (131)I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy. European journal of nuclear medicine and molecular imaging. 2014 Jul;41(7):1280-92. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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