UAMC-1110
Based on 2 publication(s) in Google Scholar
UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM.
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- Pureza: 99.51%
- No. CAS: 1448440-52-5
- Fòrmula: C17H14F2N4O2
- Peso molecular:344.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) UAMC-1110
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IF
Actividad biológica
IC50: 3.2 nM (FAP), 1.8 μM (PREP)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.0032 μM
Compound: 60
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Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
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[PMID: 24617858] |
| U-87MG ATCC | IC50 |
0.055 μM
Compound: UAMC-1110
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Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
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[PMID: 32527554] |
| U-87MG ATCC | IC50 |
41.62 nM
Compound: UAMC-1110
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Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate measured upto 60 mins by fluorescence based assay
Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate measured upto 60 mins by fluorescence based assay
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[PMID: 32527554] |
UAMC-1110 is also found to have better FAP/PREP selectivity and a very proficient ligand efficiency of 0.34[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.
Chemical Information
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No. CAS 1448440-52-5
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Appearance Solid
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Peso molecular 344.32
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Fòrmula C17H14F2N4O2
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Color White to off-white
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SMILES
O=C(C1=CC=NC2=CC=CC=C12)NCC(N3[C@H](C#N)CC(F)(F)C3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Anal Chem
2019 Dec 3;91(23):14873-14878. PMID: 31670506
UAMC-1110 purchased from MedChemExpress. Usage Cited in: Anal Chem. 2019 Dec 3;91(23):14873-14878. [Abstract]
Bioluminescence image of 50 ng/mL FAP incubated with different concentrations of SP-13786 for 60 min, then probe 1 (20 μM) is added to the mixture.
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Mol Cancer Ther
PhAc-ALGP-Dox, a Novel Anticancer Prodrug with Targeted Activation and Improved Therapeutic Index. [Abstract]2022 Apr 1;21(4):568-581. PMID: 35149549
Solvente y solubilidad
DMSO : 100 mg/mL (290.43 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. 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. 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Rats: The PK parameters are determined for inhibitors 4, 5, 60 (SP-13786), and 61 in rats. Six male rats are treated for each inhibitor tested, three of which received the compound via a single intravenous (iv) administration at 5 mg/kg. The other three animals are dosed per os (po) at 20 mg/kg. Blood samples are collected at 0.083, 0.25, 0.5, 1, 2, 4, 6, and 24 h after administration. Inhibitor concentrations are determined using UPLC−MS/MS, and pharmacokinetic parameters are calculated using standard algorithms[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 2.9043 mL | 14.5214 mL | 29.0428 mL | 72.6069 mL |
| 5 mM | 0.5809 mL | 2.9043 mL | 5.8086 mL | 14.5214 mL | |
| 10 mM | 0.2904 mL | 1.4521 mL | 2.9043 mL | 7.2607 mL | |
| 15 mM | 0.1936 mL | 0.9681 mL | 1.9362 mL | 4.8405 mL | |
| 20 mM | 0.1452 mL | 0.7261 mL | 1.4521 mL | 3.6303 mL | |
| 25 mM | 0.1162 mL | 0.5809 mL | 1.1617 mL | 2.9043 mL | |
| 30 mM | 0.0968 mL | 0.4840 mL | 0.9681 mL | 2.4202 mL | |
| 40 mM | 0.0726 mL | 0.3630 mL | 0.7261 mL | 1.8152 mL | |
| 50 mM | 0.0581 mL | 0.2904 mL | 0.5809 mL | 1.4521 mL | |
| 60 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2101 mL | |
| 80 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9076 mL | |
| 100 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7261 mL |
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