MIP-1095 TFA
Based on 1 Customer Validation
MIP-1095 TFA (RPS-001 TFA) is a PSMA inhibitor with a Ki value of 0.24 nM. MIP-1095 TFA binds to PSMA with high affinity and can be internalized into PSMA-expressing cancer cells. When radiolabeled with 123I, 124I or 131I, MIP-1095 TFA enables SPECT/CT imaging, PET/CT imaging or targeted radiation delivery, respectively. 131I-MIP-1095 TFA can alter serum PSA levels and relieve bone pain. MIP-1095 TFA can be used in research related to metastatic castration-resistant prostate cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.76%
- Fòrmula: C21H26F3IN4O10
- Peso molecular:678.35
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Almacenamiento:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
MIP-1095 (1-10000 nM; 30 minutes) TFA 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) TFA 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 TFA or PMPA[1].
[123I]MIP-1095 (100 nM; 0-2 hour) TFA 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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Appearance Solid
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Peso molecular 678.35
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Fòrmula C21H26F3IN4O10
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Color White to off-white
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SMILES
O=C([C@H](CCC(O)=O)NC(N[C@@H](CCCCNC(NC1=CC=C(C=C1)I)=O)C(O)=O)=O)O.OC(C(F)(F)F)=O
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Synonyms
RPS-001 TFA
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (184.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
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]. 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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4742 mL | 7.3708 mL | 14.7417 mL | 36.8541 mL |
| 5 mM | 0.2948 mL | 1.4742 mL | 2.9483 mL | 7.3708 mL | |
| 10 mM | 0.1474 mL | 0.7371 mL | 1.4742 mL | 3.6854 mL | |
| 15 mM | 0.0983 mL | 0.4914 mL | 0.9828 mL | 2.4569 mL | |
| 20 mM | 0.0737 mL | 0.3685 mL | 0.7371 mL | 1.8427 mL | |
| 25 mM | 0.0590 mL | 0.2948 mL | 0.5897 mL | 1.4742 mL | |
| 30 mM | 0.0491 mL | 0.2457 mL | 0.4914 mL | 1.2285 mL | |
| 40 mM | 0.0369 mL | 0.1843 mL | 0.3685 mL | 0.9214 mL | |
| 50 mM | 0.0295 mL | 0.1474 mL | 0.2948 mL | 0.7371 mL | |
| 60 mM | 0.0246 mL | 0.1228 mL | 0.2457 mL | 0.6142 mL | |
| 80 mM | 0.0184 mL | 0.0921 mL | 0.1843 mL | 0.4607 mL | |
| 100 mM | 0.0147 mL | 0.0737 mL | 0.1474 mL | 0.3685 mL |
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