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.
For research use only. We do not sell to patients.
- CAS No.: 949575-22-8
- Formula: C19H25IN4O8
- Molecular Weight:564.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
In Vitro
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. .
In Vivo
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 No. 949575-22-8
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Molecular Weight 564.33
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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