1. Immunology/Inflammation
  2. FAP
  3. NH2-UAMC1110 TFA

NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis.

For research use only. We do not sell to patients.

NH2-UAMC1110 TFA

NH2-UAMC1110 TFA Chemical Structure

CAS No. : 2990021-73-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
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Based on 1 publication(s) in Google Scholar

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Description

NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis[1][2].

In Vitro

NH2-UAMC1110 TFA was coupled with DOTA.SA in phosphate buffer at pH 9 to successfully synthesize the FAP-targeting probe DOTA.SA.FAPi. The product was purified by HPLC to achieve the required purity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

545.46

Formula

C23H24F5N5O5

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(N1[C@@H](CC(F)(C1)F)C#N)CNC(C2=CC=NC3=C2C=C(OCCCCN)C=C3)=O.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (183.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8333 mL 9.1666 mL 18.3331 mL
5 mM 0.3667 mL 1.8333 mL 3.6666 mL
View the 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.98%

References

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). 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
H2O 1 mM 1.8333 mL 9.1666 mL 18.3331 mL 45.8329 mL
5 mM 0.3667 mL 1.8333 mL 3.6666 mL 9.1666 mL
10 mM 0.1833 mL 0.9167 mL 1.8333 mL 4.5833 mL
15 mM 0.1222 mL 0.6111 mL 1.2222 mL 3.0555 mL
20 mM 0.0917 mL 0.4583 mL 0.9167 mL 2.2916 mL
25 mM 0.0733 mL 0.3667 mL 0.7333 mL 1.8333 mL
30 mM 0.0611 mL 0.3056 mL 0.6111 mL 1.5278 mL
40 mM 0.0458 mL 0.2292 mL 0.4583 mL 1.1458 mL
50 mM 0.0367 mL 0.1833 mL 0.3667 mL 0.9167 mL
60 mM 0.0306 mL 0.1528 mL 0.3056 mL 0.7639 mL
80 mM 0.0229 mL 0.1146 mL 0.2292 mL 0.5729 mL
100 mM 0.0183 mL 0.0917 mL 0.1833 mL 0.4583 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Product Name:
NH2-UAMC1110 TFA
Cat. No.:
HY-153552A
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