FAPI-4 | CAS#2374782-02-0 | FAB inhibitor

MedKoo Cat#: 408013 | Name: FAPI-04

Description:

WARNING: This product is for research use only, not for human or veterinary use.

FAPI-04, also known as FAPi-4, is a quinoline-based theranostic ligand 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.

Chemical Structure

FAPI-04

CAS#2374782-02-0

Theoretical Analysis

MedKoo Cat#: 408013

Name: FAPI-04

CAS#: 2374782-02-0

Chemical Formula: C40H54F2N10O10

Exact Mass: 872.3992

Molecular Weight: 872.93

Elemental Analysis: C, 55.04; H, 6.24; F, 4.35; N, 16.05; O, 18.33

Price and Availability

Size	Price	Availability
1mg	USD 125.00	Ready to ship
5mg	USD 250.00	Ready to ship
10mg	USD 450.00	Ready to ship
25mg	USD 950.00	Ready to ship
50mg	USD 1,650.00	Ready to ship
100mg	USD 2,650.00	Ready to ship

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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

97 % (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

More Info

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.

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot# Y23X11M01

QC Data

View QC data: current batch, Lot#Y23X11M01

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

seMpai is an AkaLumine analog, acting as an NIR emission luciferin.

In vitro activity:

To be determined

In vivo activity:

This study demonstrated the ability of FAPI-04 to detect primary and metastatic renal cell carcinoma (RCC) lesions in patients, presenting higher median values of SUVmax and tumor-to-background ratio compared to the standard FDG-PET/CT. FAPI-04 PET/CT displayed higher SUVmax values in the lungs and revealed potential staging insights for primary lesions based on TNM stages. FAPI-04 PET/CT has potential as a complementary imaging modality. Reference: Eur J Nucl Med Mol Imaging. 2023 Oct 7. https://pubmed.ncbi.nlm.nih.gov/37803246/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	114.56

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 872.93 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:

1. Civan C, Kuyumcu S, Has Simsek D, Sanli O, Isik EG, Ozkan ZG, Hurdogan O, Sanli Y. The role of [68 Ga]Ga-FAPI-04 PET/CT in renal cell carcinoma: a preliminary study. Eur J Nucl Med Mol Imaging. 2023 Oct 7. doi: 10.1007/s00259-023-06461-4. Epub ahead of print. PMID: 37803246. 2. Qiao K, Qin X, Fu S, Ren J, Jia J, Hu X, Tao Y, Yuan S, Wei Y. Value of [18F]AlF-NOTA-FAPI-04 PET/CT for differential diagnosis of malignant and various inflammatory lung lesions: comparison with [18F]FDG PET/CT. Eur Radiol. 2023 Sep 5. doi: 10.1007/s00330-023-10208-y. Epub ahead of print. PMID: 37670186.

In vitro protocol:

To be determined

In vivo protocol:

1: Jiang M, Zhang G, Li L, He Y, Li G, Yu J, Feng J, Liu X. Case Report: A case report of myocardial fibrosis activation assessment after unstable angina using 68Ga-FAPI-04 PET/CT. Front Cardiovasc Med. 2024 Jan 23;11:1332307. doi: 10.3389/fcvm.2024.1332307. PMID: 38322772; PMCID: PMC10844421. 2: Rao W, Fang XH, Zhao Y, Wang Y, Zhang B, Wei Z, Kong X, Cai JZ, Yang G, Xie M. Clinical value of [18F]AlF-NOTA-FAPI-04 PET/CT for assessing early-stage liver fibrosis in adult liver transplantation recipients compared with chronic HBV patients. Jpn J Radiol. 2024 Feb 6. doi: 10.1007/s11604-024-01528-0. Epub ahead of print. PMID: 38316724. 3: Guo C, Liu Y, Yang H, Xia Y, Li X, Chen L, Feng Y, Zhang Y, Chen Y, Huang Z. A pilot study of [68Ga]Ga-FAPI-04 PET/CT in renal cell carcinoma. Br J Radiol. 2024 Jan 30:tqae025. doi: 10.1093/bjr/tqae025. Epub ahead of print. PMID: 38290775. 4: Ergül N, Çermik TF, Alçın G, Arslan E, Erol Fenercioğlu Ö, Beyhan E, Şahin R, Baloğlu MC, Baykal Koca S, Türkay R, Yücetaş U. Contribution of 68 Ga-DOTA- FAPI-04 PET/CT to Prostate Cancer Imaging : Complementary Role in PSMA-Negative Cases. Clin Nucl Med. 2024 Mar 1;49(3):e105-e110. doi: 10.1097/RLU.0000000000005064. Epub 2024 Jan 25. PMID: 38271254. 5: Dong Y, Zhao T, Ma L, Dong A, Zhao Q. 18 F-FAPI-04 PET/CT in a Case of Primary Gastric Plasmacytoma. Clin Nucl Med. 2024 Jan 25. doi: 10.1097/RLU.0000000000005065. Epub ahead of print. PMID: 38271238. 6: Li X, Lv X, Quan Z, Han T, Tang Y, Liu Y, Wang M, Li G, Ye J, Wang J, Lan X, Zhang X, Li M, Liu S, Kang F, Wang J. Surgical evidence-based comparison of [68Ga]Ga-FAPI-04 PET and MRI-DWI for assisting debulking surgery in ovarian cancer patients. Eur J Nucl Med Mol Imaging. 2024 Jan 10. doi: 10.1007/s00259-023-06582-w. Epub ahead of print. PMID: 38197954. 7: Li X, Lu N, Lin L, Chen Y, Yang S, Wang H, Liu X, Wu C, Xue X, Su X, Bai X, Liang T. 18F-FAPI-04 Outperforms 18F-FDG PET/CT in Clinical Assessments of Patients with Pancreatic Adenocarcinoma. J Nucl Med. 2024 Feb 1;65(2):206-212. doi: 10.2967/jnumed.123.266283. PMID: 38176719; PMCID: PMC10858376. 8: Pan Q, Yang H, Zhou Z, Li M, Jiang X, Li F, Luo Y, Li M. [68 Ga]Ga-FAPI-04 PET/CT may be a predictor for early treatment response in rheumatoid arthritis. EJNMMI Res. 2024 Jan 4;14(1):2. doi: 10.1186/s13550-023-01064-4. PMID: 38175339; PMCID: PMC10766931. 9: Miao Y, Feng R, Yu T, Guo R, Zhang M, Wang Y, Hai W, Shangguan C, Zhu Z, Li B. Value of 68Ga-FAPI-04 and 18F-FDG PET/CT in Early Prediction of Pathologic Response to Neoadjuvant Chemotherapy in Locally Advanced Gastric Cancer. J Nucl Med. 2024 Feb 1;65(2):213-220. doi: 10.2967/jnumed.123.266403. PMID: 38164574. 10: Ye Z, Yao Y, Yin J, Kou Y, Zhao M, Cheng Z. Detection of occult neoplasia in a patient with dermatomyositis using [18F]AlF-NOTA-FAPI-04 and 18F-FDG PET/CT imaging. Rev Esp Med Nucl Imagen Mol (Engl Ed). 2023 Dec 28:S2253-8089(23)00099-X. doi: 10.1016/j.remnie.2023.12.004. Epub ahead of print. PMID: 38159845. 11: Khodeir M, Poerio A, Colina M. 68Ga-FAPI-04 PET/CT in Synovitis, Acne, Pustulosis, Hyperostosis, and Osteitis Syndrome. Clin Nucl Med. 2023 Dec 5. doi: 10.1097/RLU.0000000000005005. Epub ahead of print. PMID: 38049977. 12: Prashanth KA, Jain D, Manikandan R, Kalyan S, Velayutham V, Surendran R. Signet cell rectal carcinoma with prostatic involvement detected by FAPI-04 PET- MRI fusion. Eur J Hybrid Imaging. 2023 Dec 1;7(1):26. doi: 10.1186/s41824-023-00183-4. PMID: 38036687; PMCID: PMC10689635. 13: Zhao Y, Ren J. 18F-FAPI-04 PET/CT parameters predict PD-L1 expression in esophageal squamous cell carcinoma. Front Immunol. 2023 Nov 15;14:1266843. doi: 10.3389/fimmu.2023.1266843. PMID: 38035081; PMCID: PMC10684668. 14: Lyu Y, Chen X, Liu H, Xi Y, Feng W, Li B. Comparison of the diagnostic value of [68 Ga]Ga-FAPI-04 PET/MR and [18F]FDG PET/CT in patients with T stage ≤ 2a2 uterine cervical cancer: a prospective study. Eur J Nucl Med Mol Imaging. 2023 Nov 30. doi: 10.1007/s00259-023-06539-z. Epub ahead of print. PMID: 38032383. 15: Sun Y, Cai X, Wang Z, Sun Y, Cheng J. Elevated 18 F-AIF-FAPI-04 Uptake in Hepatic Hemangioma. Clin Nucl Med. 2024 Jan 1;49(1):e25-e27. doi: 10.1097/RLU.0000000000004965. Epub 2023 Nov 24. PMID: 38015630. 16: Wang J, Yu N, Wang G, Wang R, Li L, Jiang Y, Sui H, Sun Y, Li Z, Long X, Zhu Z. 68 Ga-FAPI-04 PET/CT in Assessment of Fibroblast Activation in Keloids : A Prospective Pilot Study. Clin Nucl Med. 2024 Jan 1;49(1):16-22. doi: 10.1097/RLU.0000000000004913. Epub 2023 Nov 24. PMID: 38015039. 17: Zhang Z, Hou W, Pan G, Zuo C, Cheng C. Elevated 68 Ga-FAPI-04 Activity Due to Staphylococcus aureus Intracranial Infection. Clin Nucl Med. 2024 Jan 1;49(1):e6-e7. doi: 10.1097/RLU.0000000000004958. Epub 2023 Nov 16. PMID: 37976533. 18: Liu Z, Zhou H, Li P, Wang Z, Tu T, Ezzi SHA, Kota VG, Hasan Abdulla MHA, Alhaskawi A, Dong Y, Huang Y, Dong M, Su X, Lu H. Fibroblast Activation Protein- Targeted PET/CT With Al18F-NODA-FAPI-04 for In Vivo Imaging of Tendon Healing in Rat Achilles Tendon Injury Models. Am J Sports Med. 2023 Dec;51(14):3790-3801. doi: 10.1177/03635465231208843. Epub 2023 Nov 17. PMID: 37975494. 19: Has Simsek D, Guzel Y, Denizmen D, Sanli Y, Buyukkaya F, Kovan B, Komek H, Isik EG, Ozkan ZG, Kuyumcu S. The inferior performance of [68Ga]Ga- FAPI-04 PET/CT as a diagnostic and theranostic biomarker in [177Lu]Lu-DOTATATE refractory well-differentiated neuroendocrine tumors. Eur J Nucl Med Mol Imaging. 2024 Feb;51(3):828-840. doi: 10.1007/s00259-023-06497-6. Epub 2023 Nov 10. PMID: 37947850. 20: Zhang Y, Zhou Y, Tian R, Su M. Physiological Uptake Characteristics of Breast on 68Ga-FAPI-04 PET/CT. Mol Imaging Biol. 2023 Dec;25(6):1045-1053. doi: 10.1007/s11307-023-01872-z. Epub 2023 Nov 9. PMID: 37945972.