MIP-1072
MIP-1072 is a competitive prostate-specific membrane antigen (PSMA) inhibitor with a Ki value of 4.6 nM. MIP-1072 specifically binds to PSMA and is internalized into PSMA-expressing prostate cancer cells. MIP-1072 accumulates in PSMA-expressing prostate cancer xenografts. MIP-1072 specifically blocks the uptake of 68Ga-NOTA-GUL by PSMA-positive prostate cancer xenografts. When radiolabeled with 123I, MIP-1072 functions as a SPECT/CT molecular imaging agent. MIP-1072 can be used in prostate cancer-related research.
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- No. CAS: 949575-20-6
- Fòrmula: C19H26IN3O7
- Peso molecular:535.33
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Almacenamiento:
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Actividad biológica
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Chemical Information
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- Referencias
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
22 nM
Compound: 11
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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-1072 (1-10000 nM; 30 min) potently inhibits the NAALAD enzymatic activity of PSMA in prostate cancer LNCaP cell lysates, with a Ki value of 4.6 nM[1].
[123I]MIP-1072 (3 nM; 1 h) binds specifically to PSMA-positive prostate cancer LNCaP cells, but does not bind to PSMA-negative prostate cancer PC3 cells; this binding is inhibited by non-radioactively labeled MIP-1072 (10 µM; 1 h)[1].
[123I]MIP-1072 (100 nM; 0-2 h) undergoes internalization into prostate cancer LNCaP cells in a temperature- and time-dependent manner at 37 °C[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
123I-MIP-1072 (74 kBq/mouse; i.v.; single bolus injection) tumor uptake is directly proportional to tumor mass (overall R2 = 0.7605; combined treatment groups R2 = 0.7066), enabling tracking of changes in tumor size in response to paclitaxel therapy in LNCaP xenograft-bearing mice[2].
MIP-1072 (50 mg/kg; single co-injection with 68Ga-NOTA-GUL) specifically blocks 68Ga-NOTA-GUL uptake in PSMA-positive prostate cancer xenografts in BALB/c nude mice, reducing tumor SUVmean to 0.098[3].
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, xenograft model via implantation of LNCaP, PC-3 PIP, or PC-3 flu cells, used when tumors reached 5-7 mm in diameter)[1]
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Dosage:1 mCi/mouse
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Administration:i.v.; single dose
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Result:Showed high, selective uptake in PSMA-expressing LNCaP tumors and kidneys at 4 hours post-injection via SPECT/CT imaging.
Detected PSMA-positive PC-3 PIP tumors but showed no uptake in PSMA-negative PC-3 flu tumors at 2 hours post-injection via SPECT/CT imaging.
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Animal Model:NCr-nu/nu (male, athymic, LNCaP human prostate cancer xenograft)[2]
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Dosage:~74 kBq/mouse
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Administration:i.v.; single bolus injection
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Result:Showed an overall linear correlation with tumor mass (R2 = 0.7605).
Increased from 2.17 %ID on day 2 to 3.93 %ID on day 23 in vehicle-treated mice, corresponding to increased tumor growth (mean tumor mass increased from 222 mg to 415 mg).
Reached 2.34 %ID on day 23 in paclitaxel-treated mice, not significantly different from day 2 vehicle-treated mice, consistent with inhibited tumor growth (mean tumor mass 161 mg).
Reached 10.0 %ID/g (day 2 vehicle), 9.8 %ID/g (day 23 vehicle), and 13.3 %ID/g (day 23 paclitaxel).
Showed a linear correlation with tumor mass in combined treatment groups (R2 = 0.7066).
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Animal Model:BALB/c nude (male, 4 weeks old, specific pathogen-free)[3]
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Dosage:50 mg/kg
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Administration:single co-injection with 68Ga-NOTA-GUL
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Result:Reduced tumor SUVmean from 1.056 to 0.098.
Partially blocked kidney uptake of 68Ga-NOTA-GUL.
Chemical Information
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No. CAS 949575-20-6
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Peso molecular 535.33
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Fòrmula C19H26IN3O7
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SMILES
OC(CC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCCCNCC1=CC=C(C=C1)I)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]. Hillier SM, et al. 123I-MIP-1072, a small-molecule inhibitor of prostate-specific membrane antigen, is effective at monitoring tumor response to taxane therapy. J Nucl Med. 2011 Jul;52(7):1087-93. [Content Brief]
[3]. Moon SH, et al. Development of a Ga-68 labeled PET tracer with short linker for prostate-specific membrane antigen (PSMA) targeting. Bioorganic & medicinal chemistry. 2018 May 15;26(9):2501-2507. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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