2. Immunology/Inflammation
  3. FAP
  4. FAPI-X5

FAPI-X5 is a fibroblast activation protein (FAP) inhibitor. FAPI-X5 binds to the FAP catalytic domain, forming hydrogen bonds with key active residues and engaging in π-π stacking to drive functional inhibition. FAPI-X5 exhibits albumin binding activity to prolong systemic circulation half-life. FAPI-X5 induces cytostatic effects on glioblastoma tumors, slowing tumor growth without regression. FAPI-X5, when labeled with 68Ga, acts as a PET tracer with rapid tumor uptake and high-contrast imaging in glioblastoma tumor-bearing mice. FAPI-X5, when labeled with 177Lu or 47Sc, functions as a targeted radionuclide agent with prolonged tumor retention. FAPI-X5 can be used for the research of glioblastoma.

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

FAPI-X5

FAPI-X5 Chemical Structure

CAS No. : 3056070-96-0

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

FAPI-X5 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

FAPI-X5 is a fibroblast activation protein (FAP) inhibitor. FAPI-X5 binds to the FAP catalytic domain, forming hydrogen bonds with key active residues and engaging in π-π stacking to drive functional inhibition. FAPI-X5 exhibits albumin binding activity to prolong systemic circulation half-life. FAPI-X5 induces cytostatic effects on glioblastoma tumors, slowing tumor growth without regression. FAPI-X5, when labeled with 68Ga, acts as a PET tracer with rapid tumor uptake and high-contrast imaging in glioblastoma tumor-bearing mice. FAPI-X5, when labeled with 177Lu or 47Sc, functions as a targeted radionuclide agent with prolonged tumor retention. FAPI-X5 can be used for the research of glioblastoma[1].

In Vitro

FAPI-X5 (10 μg) when radiolabeled with 68Ga, 177Lu, or 47Sc exhibits >95% radiochemical purity, >40% albumin binding, and high in vitro stability, with 68Ga-FAPI-X5 showing the highest hydrophilicity and 177Lu- and 47Sc-FAPI-X5 showing slightly higher albumin binding[1].
FAPI-X5 (30-240 min) when radiolabeled with 68Ga, 177Lu, or 47Sc exhibits time-dependent cellular uptake in FAP-expressing U87MG cells, with 68Ga-FAPI-X5 showing the highest uptake at 2 h, and all variants reaching peak uptake by 4 h[1].

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

FAPI-X5 Related Antibodies
In Vivo

FAPI-X5 (177Lu-FAPI-X5 and 47Sc-FAPI-X5) (18.5-55.5 MBq; i.v.; single dose) produce cytostatic effects (T/C values 35.49%-57.2%) in U87MG glioblastoma-bearing mice, but are associated with dose-dependent hepatogastrointestinal toxicity[1].

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

Animal Model: U87MG tumor-bearing mice[1]
Dosage: 18.5 MBq, 37 MBq, 55.5 MBq
Administration: I.v.; single dose
Result: Produced cytostatic effects with T/C values of 35.49% ± 3.8% at 18.5 MBq, 46.1% ± 4.7% at 37 MBq, and 57.2% ± 5.3% for 177Lu-FAPI-X5.
Produced cytostatic effects with T/C values of 37.50% ± 2.7% at 18.5 MBq, 36.8% ± 3.2% at 37 MBq, and 42.8% ± 3.6% for 47Sc-FAPI-X5.
Caused dose-dependent body weight loss, with a maximum loss of 11% at the 55.5 MBq 47Sc-FAPI-X5 dose, plateauing by day 10.
Resulted in one death in the 37 MBq 47Sc-FAPI-X5 group and one in the 55.5 MBq 177Lu-FAPI-X5 group.
Induced centrilobular coagulative necrosis of hepatocytes, ulcerative necrosis of intestinal mucosa, and mild inflammatory cell infiltration in cardiac and renal tissues.
Molecular Weight

1428.37

Formula

C63H88F2IN15O13
CAS No.
SMILES

OC(CN1CCN(CC(O)=O)CCN(CC(NCCCC[C@H](NC(CCCC2=CC=C(I)C=C2)=O)C(N[C@@H](CCCNC(N)=N)C(N3CCC(CCCOC4=CC=C(N=CC=C5C(NCC(N6CC(F)(F)C[C@H]6C#N)=O)=O)C5=C4)CC3)=O)=O)=O)CCN(CC(O)=O)CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

FAPI-X5 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FAPI-X53056070-96-0FAPFibroblast activation proteinhuman FAP protein 1Z68FAP catalytic domainhepatocyte necrosisPET tracertargeted radionuclide agentfibroblast activation protein (FAP)miceU87MG cellsglioblastoma tumorsintestinal mucosal ulcerationInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
FAPI-X5
Cat. No.:
HY-181494
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.