fibroblast growth factor 2

Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K，是抗寄生虫，抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂，也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。

SM27 是一种成纤维细胞生长因子 2（FGF2） 抑制剂，具有抗血管生成活性，可用于研究肿瘤。

FIIN2 是一种 FGFR 的不可逆抑制剂，能够抑制 FGFR1 (IC50:3.1 nM)，FGFR2 (IC50:4.3 nM)，FGFR3 (IC50:27 nM) 和 FGFR4 (IC50:45 nM)。

FGFR-IN-13（compound III-30）通过调节FGFR1（IC50=0.20 ± 0.02 nM）和FGFR4（IC50=0.40 ± 0.03 nM）来抑制关键蛋白的表达，进而影响内源性信号通路。此外，FGFR-IN-13 能够下降total-PARP和Bcl-2蛋白水平，同时提升Cleaved-PARP和Bax蛋白的表达，并呈现出剂量依赖性效果。该化合物展现出显著的抗肿瘤活性和口服活性。

Vosoritide (BMN 111) 为改良重组CNP (C型钠尿肽) 类似物，作用于NPR-B (B型钠尿肽受体)，能有效降低FGFR3 (成纤维细胞生长因子受体 3) 活性，主要应用于软骨症和侏儒症研究领域。

EOC317 (ACTB-1003) 是一种口服可用的激酶抑制剂，能够抑制 FGFR1 (IC50:6 nM)，VEGFR2 (IC50:2 nM) 和 Tie-2 (IC50:4 nM)。

Tinengotinib(替恩戈替尼)是一种多激酶抑制剂，靶向一系列参与癌细胞增殖，血管生成和免疫反应调节的激酶，包括Aurora激酶A B、Janus激酶（JAK1 2）、成纤维细胞生长因子受体（FGFR1 2 3）、血管内皮生长因子受体（VEGFRs）等多种激酶，在多种晚期实体瘤的临床试验中显示出良好的耐受性和初步疗效。

Pegozafermin是一种成纤维细胞生长因子FGF21类似物，是一种内源性代谢激素，调节能量消耗和糖脂代谢。Pegozafermin降低甘油三酯水平，可用于非酒精性脂肪性肝炎 (NASH) 和严重高甘油三酯血症 (SHTG)。

E-7090 is a fibroblast growth factor receptor inhibitor. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3.

BMS-645737 is an inhibitor of vascular endothelial growth factor (VEGF) receptor-2 and fibroblast growth factor (FGF) receptor-1. BMS-646737 has anti-angiogenic activity and was evaluated in nonclinical studies as a treatment for cancer.

Masitinib (AB1010) 是生物口服可利用的选择性 c-Kit 抑制剂 (对于人重组c-Kit，IC50=200 nM)，它还抑制PDGFRα β(IC50s=540 800 nM)，Lyn(对 LynB 的IC50=510 nM)，Lck，较小程度上抑制FGFR3和FAK。它有抗增殖，促凋亡活性，且毒性低。

Dovitinib lactate (TKI-258 lactate) 是一种多靶点的酪氨酸激酶抑制剂，抑制FLT3，c-Kit，FGFR1 3，VEGFR1 2 3和PDGFRα β的IC50值分别为 1，2，8 9，10 13 8，27 210 nM。

Tec-IN-6 is an inhibitor of Tec kinase, it also blocks unconventional secretion of fibroblast growth factor 2 (FGF2).

Sucrose octasulfate (SOS), a component of the gastrointestinal protectant sucralfate, is an alkaline aluminum-sucrose complex that inhibits peptic hydrolysis and raises gastric pH, protecting esophageal epithelium against acid injury. It can bind to exosite II of thrombin (KD = ~1.4 μM) and inhibit its catalytic activity (IC50 = 4.5 μM) and, as such, has been used as a surrogate for heparin. Furthermore, SOS has been shown to inhibit tumor growth in mouse melanoma and lung carcinoma models by preventing fibroblast growth factor 2 (FGF-2) binding to endothelial cells and also by removing any pre-bound FGF-2 from these cells (IC50 = ~2 μg/ml).

The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formationin vivo[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injuryin vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg kg day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation[3].

BO-264 是一种有口服活性的转化酸性卷曲螺旋 3 抑制剂，可特异性阻断 FGFR3-TACC3融合蛋白的功能。它诱导纺锤体检查点依赖的有丝分裂阻滞，DNA 损伤和细胞凋亡，具有广谱抗肿瘤活性。

SUN11602 是新型的碱性苯胺化合物，具有成纤维细胞生长因子特性。

Tec-IN-14 is a Tec kinase inhibitor. Tec-IN-14 blocks unconventional secretion of fibroblast growth factor 2 (FGF2).

FGFR1 DDR2 inhibitor 1 是一种具有口服活性的成纤维细胞生长因子受体 1 和盘状蛋白域受体 2 的抑制剂，能够抑制 FGFR1 (IC50:31.1 nM) 和 DDR2 (IC50:3.2 nM)，具有抗肿瘤作用。

Rogaratinib (BAY1163877) 选择性抑制成纤维细胞生长因子受体。

Tec-IN-21 is an inhibitor of Tec kinase, it also blocks unconventional secretion of fibroblast growth factor 2 (FGF2).

AS1069562 is an inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake which acts by notably restoring reduced insulin-like growth factor 1 and fibroblast growth factor 2 mRNA levels in dorsal root ganglion and spinal cord, respectively.

BW710 是一种口服活性的成纤维细胞生长因子受体 2 (FGFR2) 抑制剂，具有强效和选择性。其在抑制 BaF3-FGFR2 细胞增殖中的 IC50 为 2.8 nM，能够完全抑制 FGFR2 的酶活性。BW710 选择性地作用于包括 FGFR1、FGFR3 和 FGFR4 在内的其他 75 种酪氨酸激酶，且对 FGFR2 信号传导及其驱动的癌细胞增殖有明显抑制作用。BW710 药代动力学表现优良，在小鼠中口服生物利用度达到 29%。