FAP-2286
目录号 : GC65537
FAP-2286是一种强效且选择性的FAP结合肽，与放射性核素螯合剂相连，抑制人FAP蛋白酶活性的平均IC50值为2.7 ± 0.9nM。
Cas No.:2581741-18-4
Sample solution is provided at 25 µL, 10mM.
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FAP-2286 is a potent and selective FAP-binding peptide conjugated to a radionuclide chelator with a mean IC50 value of 2.7 ± 0.9nM for inhibiting human FAP protease activity. Fibroblast activation protein (FAP) is a membrane-bound protease highly expressed on cancer-associated fibroblasts (CAFs) and some tumor cells, with limited expression in normal adult tissues. The high binding affinity FAP-2286 enables the attachment of radionuclides for imaging and therapeutic use in oncology[1][2].
In vitro, [13xLa]La-FAP-2286 (1-100nM) incubated HEK-FAP+ and CHO FAP- cells confirming the strong affinity of the radiolabeled complex to the FAPI-expressing human cell line[3].
In vivo, 177Lu-FAP-2286 (30 or 60MBq/nmol) was administrated into HEK-FAP xenograft mouse model via Intravenous injection. Signifcant antitumor activity was observed with tumor growth inhibition (TGI) of 111% and 113% respectively on day 14[1]. [13xLa]La-FAP-2286 (200µL, 7.4MBq) were intravenously (i.v.) injected into both normal and HEK FAP+ tumor-bearing mice through their tail vein. The biodistribution of [13xLa]La-FAP-2286 in tumor-bearing mice showed the significant accumulation of the radiolabeled compound in tumors and kidney[3]. FAP-2286-modified LNP-based nano vector (20mg/kg) was administered via intravenous injection in subcutaneous RM-1 tumor model. Tumor accumulation was significantly increased at each time point (3, 6, 9, 12, and 24 hours after injection), with 2.1-fold, 3.2-fold, 9.2-fold, and 10.5-fold increases, respectively camparing to unmodified LNP[4].
References:
[1] Zboralski D, Hoehne A, Bredenbeck A, et al. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022 Sep;49(11):3651-3667.
[2] Pang Y C, Zhao L, Meng T H, et al. PET Imaging of Fibroblast Activation Protein in Various Types of Cancer Using 68Ga-FAP-2286: Comparison with 18F-FDG and 68Ga-FAPI-46 in a Single-Center, Prospective Study. J Nucl Med. 2023 Mar;64(3):386-394.
[3] Shirpour A, Hadadi A, Zolghadri S,et al. Preclinical evaluation of [13xLa]La-FAP-2286 as a novel theranostic agent for tumors expressing fibroblast activation protein. Sci Rep. 2025 Mar 3;15(1):7475.
[4] Qi F, Fu D, Cai H Z, et al. Metabolic Reprogramming of Cancer-Associated Fibroblasts: Transforming Tumor Accomplices into Immunotherapeutic Allies. Adv. Funct. Mater. 2024, 2418240
FAP-2286是一种强效且选择性的FAP结合肽，与放射性核素螯合剂相连，抑制人FAP蛋白酶活性的平均IC50值为2.7 ± 0.9nM。成纤维细胞激活蛋白（FAP）是一种膜结合蛋白酶，在癌症相关成纤维细胞（CAFs）和某些肿瘤细胞上高表达，而在正常成人组织中表达有限。FAP-2286的高结合亲和力使其能够连接放射性核素，用于肿瘤学中的成像和治疗应用[1][2]。
在体外实验中，[13xLa]La-FAP-2286（1-100nM）与HEK-FAP+和CHO FAP-细胞孵育，证实了放射性标记复合物对表达FAP的细胞系具有强大的亲和力[3]。
在体内实验中，将177Lu-FAP-2286（30或60MBq/nmol）腹腔注射到HEK-FAP异种移植小鼠模型中。抗肿瘤活性显著，第14天肿瘤生长抑制（TGI）分别为111%和113%[1]。[13xLa]La-FAP-2286（200µL，7.4MBq）通过尾静脉静脉注射进入正常小鼠和HEK FAP+肿瘤荷载小鼠体内。在荷瘤小鼠中，FAP-2286的生物分布显示出放射性标记化合物在肿瘤和肾脏中的显著积累[3]。FAP-2286修饰的基于LNP的纳米载体（20mg/kg）通过静脉注射给药至皮下RM-1肿瘤模型。在注射后3、6、9、12和24h的每个时间点，肿瘤积累显著增加，分别比未修饰的LNP增加了2.1倍、3.2倍、9.2倍和10.5倍[4].
| Cell experiment [1]: | |
Cell lines | HEK FAP+ cells |
Preparation Method | Approximately one million HEK FAP+ cells were seeded into the wells of a 6-well plate along containing a complete culture medium and incubated for 24h. Then, the culture medium was removed, the cells were washed, and incubated with fresh culture medium for 1h at 37°C. The plates were then placed on ice for 30min, and different concentrations of FAP-2286 (1-100nM) were added. For internalization studies, the radiolabeled compound was incubated with cells for 30, 60, 120, 240, and 360min at 37˚C. |
Reaction Conditions | 1-100nM; 30, 60, 120, 240, and 360min |
Applications | The binding of [13xLa]La-FAP-2286 on HEK FAP + cell line was evaluated, demonstrating a dissociation constant (KD) value of 0.51 ± 0.12nM, confirming the strong affinity of the radiolabeled complex to the FAP-expressing human cell line. |
| Animal experiment [1]: | |
Animal models | NOD/SCID mice |
Preparation Method | [13xLa]La-FAP-2286 (200µL, 7.4MBq) were intravenously (i.v.) injected into both normal and tumor-bearing mice through their tail vein. 8–10-week-old NOD/SCID tumor-bearing mice with an average weight of 21.4±1.7 gr were used for biodistribution studies. Tumor induction was achieved by injecting approximately 1 million HEK FAP+cells subcutaneously into the mice’s flanks. |
Dosage form | 200µL, 7.4MBq; i.v.; one dose |
Applications | The biodistribution of FAP-2286 in tumor-bearing mice showed the significant accumulation of the radiolabeled compound in tumors at different time intervals. Also, a significant accumulation of activity was observed in the kidney after injection of the radiolabeled compound, which is related to the high hydrophilicity of the compound and its excretion via the urinary tract. |
References: | |
| Cas No. | 2581741-18-4 | SDF | Download SDF |
| 分子式 | C67H99N13O18S3 | 分子量 | 1470.77 |
| 溶解度 | Water : ≥ 100 mg/mL (67.99 mM) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.6799 mL | 3.3996 mL | 6.7992 mL |
| 5 mM | 0.136 mL | 0.6799 mL | 1.3598 mL |
| 10 mM | 0.068 mL | 0.34 mL | 0.6799 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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