WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H207189
CAS#: 2374782-04-2
Description: FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FABI-46 can form complex with 90Y, 177Lu and 68Ga metal ions, which can be used as PET/CT imaging agent. [68Ga]Ga-FAPI-46 is a novel positron emission tomography (PET) ligand that targets fibroblast activation protein (FAP) expression as FAP inhibitor (FAPI) and could already show promising results in several tumor entities. It could be demonstrated that an increased FAP expression correlates with tumor aggressivity in urothelial carcinoma (UC).
Hodoodo Cat#: H207189
Name: FAPI-46
CAS#: 2374782-04-2
Chemical Formula: C41H57F2N11O9
Exact Mass: 885.43
Molecular Weight: 885.972
Elemental Analysis: C, 55.58; H, 6.49; F, 4.29; N, 17.39; O, 16.25
Synonym: FAPI-46; FAPI 46; FAPI46;
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)(methyl)amino)propyl)piperazin-1-yl)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
InChi Key: SDBGUEFOSXNKBX-HKBQPEDESA-N
InChi Code: InChI=1S/C41H57F2N11O9/c1-47(30-3-4-34-33(21-30)32(5-6-45-34)40(63)46-24-35(55)54-29-41(42,43)22-31(54)23-44)7-2-8-48-17-19-53(20-18-48)36(56)25-49-9-11-50(26-37(57)58)13-15-52(28-39(61)62)16-14-51(12-10-49)27-38(59)60/h3-6,21,31H,2,7-20,22,24-29H2,1H3,(H,46,63)(H,57,58)(H,59,60)(H,61,62)/t31-/m0/s1
SMILES Code: O=C(C1=CC=NC(C=C2)=C1C=C2N(C)CCCN(CC3)CCN3C(CN(CCN(CC4)CC(O)=O)CCN(CCN4CC(O)=O)CC(O)=O)=O)NCC(N(CC5(F)F)[C@@H](C5)C#N)=O
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 885.97 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Glatting FM, Hoppner J, Kauczor HU, Huber PE, Kratochwil C, Giesel FL, Haberkorn U, Röhrich M. Subclass Analysis of Malignant, Inflammatory and Degenerative Pathologies Based on Multiple Timepoint FAPI-PET Acquisitions Using FAPI-02, FAPI-46 and FAPI-74. Cancers (Basel). 2022 Oct 28;14(21):5301. doi: 10.3390/cancers14215301. PMID: 36358720; PMCID: PMC9656977.
2: Naeimi M, Choyke PL, Dendl K, Mori Y, Staudinger F, Watabe T, Koerber SA, Röhrich M, Debus J, Kratochwil C, Haberkorn UA, Giesel FL. 3-time-point PET- analysis of FAPI-46 in a variety of cancers. J Nucl Med. 2022 Nov 10:jnumed.122.264941. doi: 10.2967/jnumed.122.264941. Epub ahead of print. PMID: 36357183.
3: Pang Y, Zhao L, Meng T, Xu W, Lin Q, Wu H, Zhang J, Chen X, Sun L, Chen H. PET imaging of fibroblast activation protein in various types of cancers by using 68Ga-FAP-2286: Comparison with 18F-FDG and 68Ga-FAPI-46 in a single-center, prospective study. J Nucl Med. 2022 Sep 2:jnumed.122.264544. doi: 10.2967/jnumed.122.264544. Epub ahead of print. PMID: 36215571.
4: Alfteimi A, Lützen U, Helm A, Jüptner M, Marx M, Zhao Y, Zuhayra M. Automated synthesis of [68Ga]Ga-FAPI-46 without pre-purification of the generator eluate on three common synthesis modules and two generator types. EJNMMI Radiopharm Chem. 2022 Jul 29;7(1):20. doi: 10.1186/s41181-022-00172-1. PMID: 35904684; PMCID: PMC9338183.
5: Fendler WP, Pabst KM, Kessler L, Fragoso Costa P, Ferdinandus J, Weber M, Lippert M, Lueckerath K, Umutlu L, Kostbade K, Mavroeidi IA, Schuler M, Ahrens M, Rischpler C, Bauer S, Herrmann K, Siveke JT, Hamacher R. Safety and Efficacy of 90Y-FAPI-46 Radioligand Therapy in Patients with Advanced Sarcoma and Other Cancer Entities. Clin Cancer Res. 2022 Oct 3;28(19):4346-4353. doi: 10.1158/1078-0432.CCR-22-1432. PMID: 35833949.
6: Aryana K, Manafi-Farid R, Amini H, Divband G, Moghadam SZ. 68 Ga-FAPI-46 PET/CT in a Metastatic Castration-Resistant Prostate Cancer Patient With Low PSMA Expression. Clin Nucl Med. 2022 Nov 1;47(11):972-973. doi: 10.1097/RLU.0000000000004315. Epub 2022 Jul 6. PMID: 35777753.
7: Wegen S, van Heek L, Linde P, Claus K, Akuamoa-Boateng D, Baues C, Sharma SJ, Schomäcker K, Fischer T, Roth KS, Klußmann JP, Marnitz S, Drzezga A, Kobe C. Head-to-Head Comparison of [68 Ga]Ga-FAPI-46-PET/CT and [18F]F-FDG-PET/CT for Radiotherapy Planning in Head and Neck Cancer. Mol Imaging Biol. 2022 Dec;24(6):986-994. doi: 10.1007/s11307-022-01749-7. Epub 2022 Jun 30. PMID: 35771317; PMCID: PMC9681697.
8: Kaghazchi F, Divband G, Amini H, Adinehpour Z, Akbarian Aghdam R. 68 Ga- FAPI-46 and 18 F-FDG in Advanced Metastatic Pancreatic Cancer. Clin Nucl Med. 2022 Oct 1;47(10):e666-e669. doi: 10.1097/RLU.0000000000004316. Epub 2022 Jun 18. PMID: 35714370.
9: Glatting FM, Hoppner J, Liew DP, van Genabith A, Spektor AM, Steinbach L, Hubert A, Kratochwil C, Giesel FL, Dendl K, Rathke H, Kauczor HU, Huber PE, Haberkorn U, Röhrich M. Repetitive Early 68Ga-FAPI PET Acquisition Comparing 68Ga-FAPI-02, 68Ga-FAPI-46, and 68Ga- FAPI-74: Methodologic and Diagnostic Implications for Malignant, Inflammatory/Reactive, and Degenerative Lesions. J Nucl Med. 2022 Dec;63(12):1844-1851. doi: 10.2967/jnumed.122.264069. Epub 2022 May 26. PMID: 35618480.
10: Rosenkrans ZT, Massey CF, Bernau K, Ferreira CA, Jeffery JJ, Schulte JJ, Moore M, Valla F, Batterton JM, Drake CR, McMillan AB, Sandbo N, Pirasteh A, Hernandez R. [68 Ga]Ga-FAPI-46 PET for non-invasive detection of pulmonary fibrosis disease activity. Eur J Nucl Med Mol Imaging. 2022 Sep;49(11):3705-3716. doi: 10.1007/s00259-022-05814-9. Epub 2022 May 12. PMID: 35556159; PMCID: PMC9553066.
11: Nader M, Valla DF, Vriamont C, Masset J, Pacelli A, Herrmann K, Zarrad F. [68Ga]/[90Y]FAPI-46: Automated production and analytical validation of a theranostic pair. Nucl Med Biol. 2022 Jul-Aug;110-111:37-44. doi: 10.1016/j.nucmedbio.2022.04.010. Epub 2022 Apr 30. PMID: 35533534.
12: Fu H, Huang J, Sun L, Wu H, Chen H. FAP-Targeted Radionuclide Therapy of Advanced Radioiodine-Refractory Differentiated Thyroid Cancer With Multiple Cycles of 177 Lu-FAPI-46. Clin Nucl Med. 2022 Oct 1;47(10):906-907. doi: 10.1097/RLU.0000000000004260. Epub 2022 Apr 29. PMID: 35485857.
13: Roth KS, Voltin CA, van Heek L, Wegen S, Schomäcker K, Fischer T, Marnitz S, Drzezga A, Kobe C. Dual-Tracer PET/CT Protocol with [18F]-FDG and [68Ga]Ga-FAPI-46 for Cancer Imaging: A Proof of Concept. J Nucl Med. 2022 Nov;63(11):1683-1686. doi: 10.2967/jnumed.122.263835. Epub 2022 Apr 14. PMID: 35422446.
14: Af Burén S, Tran TA, Klevebro F, Holstensson M, Axelsson R. A 68Ga-FAPI-46 PET/CT Imaging Pitfall in Assessing Residual Gastric Cancer Early After Chemotherapy. Clin Nucl Med. 2022 Jul 1;47(7):644-645. doi: 10.1097/RLU.0000000000004143. Epub 2022 Mar 31. PMID: 35353747.
15: Unterrainer LM, Lindner S, Eismann L, Casuscelli J, Gildehaus FJ, Bui VN, Albert NL, Holzgreve A, Beyer L, Todica A, Brendel M, Cyran CC, Karl A, Stief CG, Ledderose ST, Unterrainer M, Bartenstein P, Wenter V, Kretschmer A. Feasibility of [68Ga]Ga-FAPI-46 PET/CT for detection of nodal and hematogenous spread in high-grade urothelial carcinoma. Eur J Nucl Med Mol Imaging. 2022 Aug;49(10):3571-3580. doi: 10.1007/s00259-022-05761-5. Epub 2022 Mar 24. PMID: 35325283; PMCID: PMC9308618.
16: Telo S, Farolfi A, Castellucci P, Antonacci F, Solli P, Mosconi C, Fanti S, Agosti R, Morigi JJ, Nanni C. A case of [68Ga]Ga-FAPI-46-avid and [18F]F-FDG-negative COVID-19 pneumonia sequelae. Eur J Nucl Med Mol Imaging. 2022 Jun;49(7):2452-2453. doi: 10.1007/s00259-022-05720-0. Epub 2022 Feb 18. PMID: 35179626; PMCID: PMC8854481.
17: Da Pieve C, Costa Braga M, Turton DR, Valla FA, Cakmak P, Plate KH, Kramer- Marek G. New Fully Automated Preparation of High Apparent Molar Activity 68Ga-FAPI-46 on a Trasis AiO Platform. Molecules. 2022 Jan 20;27(3):675. doi: 10.3390/molecules27030675. PMID: 35163938; PMCID: PMC8840169.
18: Siebermair J, Kessler L, Kupusovic J, Rassaf T, Rischpler C. Cardiac fibroblast activation detected by 68Gallium-FAPI-46 positron emission tomography-magnetic resonance imaging as a sign of chronic activity in cardiac sarcoidosis. Eur Heart J Case Rep. 2022 Jan 9;6(1):ytac005. doi: 10.1093/ehjcr/ytac005. PMID: 35079689; PMCID: PMC8783545.
19: Siripongsatian D, Promteangtrong C, Kunawudhi A, Kiatkittikul P, Chotipanich C. Intense 68Ga-FAPI-46 Activity in Lesions of Recurrent Ovarian Clear Cell Carcinoma That Were Negative on FDG PET/CT Study. Clin Nucl Med. 2022 Feb 1;47(2):e210-e212. doi: 10.1097/RLU.0000000000003975. PMID: 35006122.
20: Fu K, Pang Y, Zhao L, Lin L, Wu H, Sun L, Lin Q, Chen H. FAP-targeted radionuclide therapy with [177Lu]Lu-FAPI-46 in metastatic nasopharyngeal carcinoma. Eur J Nucl Med Mol Imaging. 2022 Apr;49(5):1767-1769. doi: 10.1007/s00259-021-05634-3. Epub 2021 Dec 8. PMID: 34877610.
21: Promteangtrong C, Siripongsatian D, Jantarato A, Kunawudhi A, Kiatkittikul P, Yaset S, Boonkawin N, Chotipanich C. Head-to-Head Comparison of 68Ga-FAPI-46 and 18F-FDG PET/CT for Evaluation of Head and Neck Squamous Cell Carcinoma: A Single-Center Exploratory Study. J Nucl Med. 2022 Aug;63(8):1155-1161. doi: 10.2967/jnumed.121.262831. Epub 2021 Dec 2. PMID: 34857655.
22: Mona CE, Benz MR, Hikmat F, Grogan TR, Lueckerath K, Razmaria A, Riahi R, Slavik R, Girgis MD, Carlucci G, Kelly KA, French SW, Czernin J, Dawson DW, Calais J. Correlation of 68Ga-FAPi-46 PET Biodistribution with FAP Expression by Immunohistochemistry in Patients with Solid Cancers: Interim Analysis of a Prospective Translational Exploratory Study. J Nucl Med. 2022 Jul;63(7):1021-1026. doi: 10.2967/jnumed.121.262426. Epub 2021 Nov 5. PMID: 34740953; PMCID: PMC9258565.
23: Siripongsatian D, Promteangtrong C, Kunawudhi A, Kiatkittikul P, Chotipanich C. 68Ga-FAPI-46 PET/MR Detects Recurrent Cholangiocarcinoma and Intraductal Papillary Mucinous Neoplasm in a Patient Showing Increasing CEA with Negative 18F-FDG PET/CT and Conventional CT. Nucl Med Mol Imaging. 2021 Oct;55(5):257-260. doi: 10.1007/s13139-021-00712-8. Epub 2021 Aug 23. PMID: 34721719; PMCID: PMC8517048.
24: Hotta M, Benz MR, Allen-Auerbach MS, Crompton JG, Roth MD, Eilber FC, Calais J. High 68 Ga-FAPI-46 uptake in a pulmonary necrotizing granuloma in a patient with subcutaneous lipoma. Eur J Nucl Med Mol Imaging. 2022 Feb;49(3):1088-1089. doi: 10.1007/s00259-021-05510-0. Epub 2021 Sep 21. PMID: 34546387.
25: Liu Y, Watabe T, Kaneda-Nakashima K, Shirakami Y, Naka S, Ooe K, Toyoshima A, Nagata K, Haberkorn U, Kratochwil C, Shinohara A, Hatazawa J, Giesel F. Fibroblast activation protein targeted therapy using [177Lu]FAPI-46 compared with [225Ac]FAPI-46 in a pancreatic cancer model. Eur J Nucl Med Mol Imaging. 2022 Feb;49(3):871-880. doi: 10.1007/s00259-021-05554-2. Epub 2021 Sep 18. PMID: 34537893; PMCID: PMC8803706.
26: Ferdinandus J, Costa PF, Kessler L, Weber M, Hirmas N, Kostbade K, Bauer S, Schuler M, Ahrens M, Schildhaus HU, Rischpler C, Grafe H, Siveke JT, Herrmann K, Fendler WP, Hamacher R. Initial Clinical Experience with 90Y-FAPI-46 Radioligand Therapy for Advanced-Stage Solid Tumors: A Case Series of 9 Patients. J Nucl Med. 2022 May;63(5):727-734. doi: 10.2967/jnumed.121.262468. Epub 2021 Aug 12. PMID: 34385340; PMCID: PMC9051597.
27: Hotta M, Sonni I, Benz MR, Gafita A, Bahri S, Shuch BM, Yu R, Liu ST, Czernin J, Calais J. 68Ga-FAPI-46 and 18F-FDG PET/CT in a patient with immune-related thyroiditis induced by immune checkpoint inhibitors. Eur J Nucl Med Mol Imaging. 2021 Oct;48(11):3736-3737. doi: 10.1007/s00259-021-05373-5. Epub 2021 Apr 29. PMID: 33914106.
28: Kratochwil C, Giesel FL, Rathke H, Fink R, Dendl K, Debus J, Mier W, Jäger D, Lindner T, Haberkorn U. [153Sm]Samarium-labeled FAPI-46 radioligand therapy in a patient with lung metastases of a sarcoma. Eur J Nucl Med Mol Imaging. 2021 Aug;48(9):3011-3013. doi: 10.1007/s00259-021-05273-8. Epub 2021 Mar 17. PMID: 33728499; PMCID: PMC8263436.
29: Ferdinandus J, Kessler L, Hirmas N, Trajkovic-Arsic M, Hamacher R, Umutlu L, Nader M, Zarrad F, Weber M, Fendler WP. Equivalent tumor detection for early and late FAPI-46 PET acquisition. Eur J Nucl Med Mol Imaging. 2021 Sep;48(10):3221-3227. doi: 10.1007/s00259-021-05266-7. Epub 2021 Feb 23. PMID: 33620560; PMCID: PMC8426301.
30: Spreckelmeyer S, Balzer M, Poetzsch S, Brenner W. Fully-automated production of [68Ga]Ga-FAPI-46 for clinical application. EJNMMI Radiopharm Chem. 2020 Dec 17;5(1):31. doi: 10.1186/s41181-020-00112-x. PMID: 33331982; PMCID: PMC7746794.
31: Hayrapetian A, Girgis MD, Yanagawa J, French SW, Schelbert HR, Auerbach MS, Czernin J, Calais J. Incidental Detection of Elastofibroma Dorsi With 68Ga- FAPI-46 and 18F-FDG PET/CT in a Patient With Esophageal Cancer. Clin Nucl Med. 2021 Feb 1;46(2):e86-e87. doi: 10.1097/RLU.0000000000003218. PMID: 32701818.
32: Sonni I, Lee-Felker S, Memarzadeh S, Quinn MM, Mona CE, Lückerath K, Czernin J, Calais J. 68Ga-FAPi-46 diffuse bilateral breast uptake in a patient with cervical cancer after hormonal stimulation. Eur J Nucl Med Mol Imaging. 2021 Mar;48(3):924-926. doi: 10.1007/s00259-020-04947-z. Epub 2020 Jul 10. PMID: 32651662.
33: Meyer C, Dahlbom M, Lindner T, Vauclin S, Mona C, Slavik R, Czernin J, Haberkorn U, Calais J. Radiation Dosimetry and Biodistribution of 68Ga-FAPI-46 PET Imaging in Cancer Patients. J Nucl Med. 2020 Aug;61(8):1171-1177. doi: 10.2967/jnumed.119.236786. Epub 2019 Dec 13. PMID: 31836685; PMCID: PMC7413240.
