WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408013
Description: FAPI-4 is a Quinoline-Based Theranostic Ligands for the Targeting of Fibroblast Activation Protein. FAPI-4 was identified as the most promising tracer for clinical application. Compared with the previously published ligand, FAPI-4 showed excellent stability in human serum, higher affinity for FAP as opposed to CD26, and slower excretion in vitro. FAPI-4 represents a promising tracer for both diagnostic imaging and, possibly, targeted therapy of malignant tumors with a high content of activated fibroblasts, such as breast cancer.
MedKoo Cat#: 408013
Chemical Formula: C40H54F2N10O10
Exact Mass: 872.3992
Molecular Weight: 872.9288
Elemental Analysis: C, 55.04; H, 6.24; F, 4.35; N, 16.05; O, 18.33
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Synonym: FAPI-04; FAPI 04; FAPI04; FAPI-4; FAPI 4; FAPI4;
IUPAC/Chemical Name: (S)-2,2',2''-(10-(2-(4-(3-((4-((2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)carbamoyl)quinolin-6-yl)oxy)propyl)piperazin-1-yl)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
InChi Key: ICWDAESAANBIGG-LJAQVGFWSA-N
InChi Code: InChI=1S/C40H54F2N10O10/c41-40(42)21-29(22-43)52(28-40)34(53)23-45-39(61)31-4-5-44-33-3-2-30(20-32(31)33)62-19-1-6-46-15-17-51(18-16-46)35(54)24-47-7-9-48(25-36(55)56)11-13-50(27-38(59)60)14-12-49(10-8-47)26-37(57)58/h2-5,20,29H,1,6-19,21,23-28H2,(H,45,61)(H,55,56)(H,57,58)(H,59,60)/t29-/m0/s1
SMILES Code: O=C(C1=CC=NC2=CC=C(OCCCN3CCN(C(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)C=C12)NCC(N5[C@H](C#N)CC(F)(F)C5)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 872.9288 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Kratochwil C, Flechsig P, Lindner T, Abderrahim L, Altmann A, Mier W, Adeberg
S, Rathke H, Röhrich M, Winter H, Plinkert PK, Marme F, Lang M, Kauczor HU, Jäger
D, Debus J, Haberkorn U, Giesel FL. (68)Ga-FAPI PET/CT: Tracer Uptake in 28
Different Kinds of Cancer. J Nucl Med. 2019 Jun;60(6):801-805. doi:
10.2967/jnumed.119.227967. Epub 2019 Apr 6. PubMed PMID: 30954939.
2: Loktev A, Lindner T, Burger EM, Altmann A, Giesel F, Kratochwil C, Debus J,
Marme F, Jaeger D, Mier W, Haberkorn U. Development of novel FAP-targeted
radiotracers with improved tumor retention. J Nucl Med. 2019 Mar 8. pii:
jnumed.118.224469. doi: 10.2967/jnumed.118.224469. [Epub ahead of print] PubMed
3: Lindner T, Loktev A, Altmann A, Giesel F, Kratochwil C, Debus J, Jäger D, Mier
W, Haberkorn U. Development of Quinoline-Based Theranostic Ligands for the
Targeting of Fibroblast Activation Protein. J Nucl Med. 2018 Sep;59(9):1415-1422.
doi: 10.2967/jnumed.118.210443. Epub 2018 Apr 6. PubMed PMID: 29626119.
Fibroblast activation protein (FAP) is overexpressed in cancer-associated fibroblasts and is involved in a variety of tumor-promoting activities such as matrix remodeling, angiogenesis, chemotherapy resistance, and immunosuppression. Because FAP shows low expression in most normal organs, it presents an interesting target for imaging and endoradiotherapy.