PD-166866
目录号 : GC19279
PD-166866是一种选择性且具有口服活性的FGFR1（成纤维细胞生长因子受体1）酪氨酸激酶抑制剂，IC50为52.4nM。
Cas No.:192705-79-6
Sample solution is provided at 25 µL, 10mM.
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PD-166866 is a selective and orally active FGFR1 (fibroblast growth factor receptor 1) tyrosine kinase inhibitor, with an IC₅₀ of 52.4nM[1]. FGFR1 is a transmembrane receptor tyrosine kinase that, upon ligand binding, activates downstream signaling cascades regulating cell proliferation, differentiation, and survival[2]. PD-166866 inhibits FGFR1 tyrosine kinase activity through an ATP-competitive mechanism and is widely used to study FGFR-driven signaling in tumor growth, angiogenesis, and related pathophysiological processes[3].
In vitro, treatment of lymphatic endothelial cells with 1μM PD-166866 for 48h significantly inhibited the proliferation, migration, invasion, and tube formation, reduced the phosphorylation levels of FGFR1, PTEN, and AKT, and decreased CXCL9 secretion[4]. PD-166866 (0.1-50μM; 24h) reduced cell viability, increased membrane damage, induced DNA fragmentation, and accumulated PARP in HeLa cells[5].
In vivo, PD-166866 (0.1 or 0.5mg/day; i.p.; 2 weeks) significantly reduced tumor volume and decreased the number of proliferating cell nuclear antigen (PCNA)-positive cells in SYO-1 xenograft tumors in BALB/c nu/nu mice[6]. Combination of PD-166866 (30mg/kg; every 2 days for 14 days; i.p.) and rapamycin significantly inhibited the growth and progression of T-ALL cells and prolonged the survival time of the Jurkat cell-derived xenograft NCG mice[7].
References:
[1] Panek RL, Lu GH, Dahring TK, et al. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J Pharmacol Exp Ther. 1998;286(1):569-577.
[2] Kaur N, Gare SR, Shen J, Raja R, Fonseka O, Liu W. Multi-organ FGF21-FGFR1 signaling in metabolic health and disease. Front Cardiovasc Med. 2022;9:962561.
[3] Calandrella N, Risuleo G, Scarsella G, et al. Reduction of cell proliferation induced by PD166866: an inhibitor of the basic fibroblast growth factor. J Exp Clin Cancer Res. 2007;26(3):405-409.
[4] Kang J, Cheng A, Chen G, Zhu L, Han Z, Xu Q. Tumor Cells-Derived FGF-2 Promotes Lymphangiogenesis as a Prognostic Marker in OSCC. J Oral Pathol Med. 2025;54(8):694-705.
[5] Risuleo G, Ciacciarelli M, Castelli M, Galati G. The synthetic inhibitor of fibroblast growth factor receptor PD166866 controls negatively the growth of tumor cells in culture. J Exp Clin Cancer Res. 2009;28(1):151.
[6] Ishibe T, Nakayama T, Okamoto T, et al. Disruption of fibroblast growth factor signal pathway inhibits the growth of synovial sarcomas: potential application of signal inhibitors to molecular target therapy. Clin Cancer Res. 2005;11(7):2702-2712.
[7] Zhang ZJ, Wu QF, Ren AQ, et al. ATF4 renders human T-cell acute lymphoblastic leukemia cell resistance to FGFR1 inhibitors through amino acid metabolic reprogramming. Acta Pharmacol Sin. 2023;44(11):2282-2295.
PD-166866是一种选择性且具有口服活性的FGFR1（成纤维细胞生长因子受体1）酪氨酸激酶抑制剂，IC50为52.4nM[1]。FGFR1是一种跨膜受体酪氨酸激酶，配体结合后可激活下游信号级联反应，调节细胞增殖、分化和存活[2]。PD-166866通过ATP竞争机制抑制FGFR1酪氨酸激酶活性，广泛用于研究FGFR驱动的肿瘤生长、血管生成及相关病理生理过程中的信号传导[3]。
在体外实验中，用1μM PD-166866处理淋巴管内皮细胞48小时显著抑制了细胞的增殖、迁移、侵袭和管状形成能力，降低了FGFR1、PTEN和AKT的磷酸化水平，并减少了CXCL9的分泌[4]。在HeLa细胞中，PD-166866（0.1-50μM；处理24小时）降低了细胞活性，增加了膜损伤，诱导了DNA片段化，并使PARP蛋白积累[5]。
在体内实验中，PD-166866（0.1或0.5mg/天；腹腔注射；2周）显著减少了SYO-1异种移植瘤在BALB/c nu/nu小鼠中的肿瘤体积，降低了增殖细胞核抗原（PCNA）阳性细胞的数量[6]。PD-166866（30mg/kg；每2天一次；共14天；腹腔注射）与雷帕霉素联合使用，显著抑制了T-ALL细胞的生长和进展，并延长了Jurkat细胞衍生异种移植NCG小鼠的存活时间[7]。
| Cell experiment [1]: | |
Cell lines | HeLa cells |
Preparation Method | HeLa cells were maintained in DMEM (Dulbecco's Modified Eagle's Medium - high glucose), supplemented with newborn bovine serum [final concentration (f.c.) 10%], penicillin-streptomycin (10000U/ml) and glutamine (2mM); the pH of the medium was 7.2 and incubation was at 37°C in a 5% CO2 atmosphere. Cells were routinely passaged when confluent. Cells were exposed to a relatively broad range of PD-166866 concentrations (0.1-50μM) for 24 hours. Then cell vitality was assessed by the MTT assay. Oxidative stress at membrane level was assessed by commercial kit. DNA damage was assessed by in situ fluorescent staining with Terminal Deoxynucleotidyl Transferase dUTP nick end labeling (TUNEL assay). The expression of PARP, consequent to DNA fragmentation, was evidenced by immunohistochemistry. |
Reaction Conditions | 0.1-50μM; 24h |
Applications | PD-166866 (0.1-50μM; 24h) reduced cell viability, increased membrane damage, induced DNA fragmentation, and accumulated PARP in HeLa cells. |
| Animal experiment [2]: | |
Animal models | male BALB/c nu/nu athymic mice |
Preparation Method | SYO-1 (5×106) cells suspended in 100μl of PBS were s.c. injected into the hind flank region of male BALB/c nu/nu athymic mice at 5 weeks of age. When the tumor volume reached about 50mm3 (usually 11-12 days after inoculation), PD-166866 (0.1 or 0.5mg) suspended in 50μl of DMSO was given i.p. , a treatment which was repeated thereafter once a day, 6 days a week, for 2 weeks. Tumor size was measured with vernier calipers, and the volume was calculated as π/6×length×width×height. |
Dosage form | 0.1 and 0.5mg/day; i.p.; 2 weeks |
Applications | PD-166866 significantly reduced tumor volume in SYO-1 xenograft tumors in BALB/c nu/nu mice. |
References: | |
| Cas No. | 192705-79-6 | SDF | |
| Canonical SMILES | O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3 | ||
| 分子式 | C20H24N6O3 | 分子量 | 396.44 |
| 溶解度 | DMSO : 10.33 mg/mL (26.06 mM) | 储存条件 | Store at -20°C |
| 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 | 2.5224 mL | 12.6122 mL | 25.2245 mL |
| 5 mM | 504.5 μL | 2.5224 mL | 5.0449 mL |
| 10 mM | 252.2 μL | 1.2612 mL | 2.5224 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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2.
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