fibroblast growth factor 1

Brain-derived acidic fibroblast growth factor (brain-derived aFGF) (1-11) is a peptide fragment of brain-derived aFGF. Brain-derived aFGF is an angiogenic vascular endothelial cell mitogen produced in bovine brain that has sequence homology to interleukin-1. aFGF (1-11) corresponds to amino acid residues 1-11 of the full length peptide.

Brain-derived basic fibroblast growth factor (1-24) (brain-derived bFGF) is a peptide fragment of brain-derived bFGF. bFGF is a peptide produced in bovine brain that is protective in a rat model of pressure-induced retinal ischemia. bFGF (1-24) corresponds to amino acid residues 1-24 of the full length peptide.

Brain Derived BasicFibroblast Growth Factor(1-24) (FGF basic 1-24) 是一种合成肽，表现出抗细菌和抗HBV 的活性。Brain Derived BasicFibroblast Growth Factor(1-24) 可用于感染性疾病和免疫性疾病的研究。

Brain-derived acidic fibroblast growth factor (102-111) is a peptide fragment of brain-derived acidic fibroblast growth factor (aFGF). aFGF is an angiogenic vascular endothelial cell mitogen produced in bovine brain that has sequence homology to interleukin-1. It also shares sequence homology with the known neuropeptides neuromedin C , bombesin , neuromedin K , substance K , substance P , physalaemin, and eledoisin. aFGF (102-111) corresponds to amino acid residues 102-111 of the fulllength peptide.

Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂，抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5 2.5 4.2 7 13 22 nM)，具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。

Picropodophyllin (Picropodophyllin (PPP)) 是一种选择性的胰岛素样生长因子-1受体抑制剂，IC50为1 nM。

SU4984 是蛋白质酪氨酸激酶抑制剂，能够抑制成纤维细胞生长因子受体 1 (FGFR1) (IC50:10-20 μM)，还能够抑制血小板衍生的生长因子受体和胰岛素受体的活性。它可用于研究癌症。

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。

PD-161570 是一种有效的 ATP 竞争性人 FGF-1 受体抑制剂，IC50 为 39.9 nM，Ki 为 42 nM。它还是骨形态发生蛋白 (BMPs) 和TGF-β信号抑制剂。它抑制PDGF 刺激的自磷酸化和FGF-1受体磷酸化，IC50分别为 450 和 622 nM。它抑制 PDGFR、EGFR 和 c-Src 酪氨酸激酶，IC50 值分别为 310、240 和 44 nM。

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)。

PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM. PRLX-93936 inhibits tumor growth in PANC-1 and HT-1080 xenograft models when administered at a dose of 50 mg/kg and induces tumor regression when administered at a dose of 100 mg/kg.

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.

CPL304110 是一种口服具有活力的、选择性的、有效的成纤维细胞生长因子受体 FGFR (1-3) 的抑制剂，能够作用于 FGFR1 (IC50: 0.75 nM)、 FGFR2 (IC50: 0.5 nM)、FGFR3 (IC50: 3.05 nM) 。

FIIN-3 是FGFR 的不可逆抑制剂，对FGFR1、FGFR2、FGFR3和FGFR4的IC50值分别为13.1、21、31.4和35.3 nM。

Picropodophyllotoxin (AXL 1717) 是一种环木脂素生物碱，存在于五月树(Podophyllum peltatum) 中，是一种具有潜在抗肿瘤活性的胰岛素样生长因子 1 受体 (IGF1R) 的小分子抑制剂。它特异性抑制 IGF1R 的活性并下调细胞表达，而不干扰其他生长因子受体的活性，例如胰岛素受体、表皮生长因子、血小板衍生生长因子、成纤维细胞生长因子和肥大 干细胞生长因子 (KIT) ）。该药剂在抑制肿瘤细胞增殖和诱导肿瘤细胞凋亡方面显示出有效的活性。 IGF1R 是一种在多种人类癌症中过度表达的受体酪氨酸激酶，在多种癌细胞的生长和存活中起关键作用。

Dovitinib 是一种口服有效的、多靶点的酪氨酸激酶 (RTK) 抑制剂，具有抗肿瘤作用。

Futibatinib（TAS-120） 是口服具有活力的、选择性强的、高生物利用度的、不可逆的 FGFR 抑制剂，对 FGFR1、FGFR2、FGFR3 和 FGFR4 的 IC50 值分别为 3.9、1.3、1.6 和 8.3 nM。[2]

Tyrosine kinase-IN-1是一种多靶点酪氨酸激酶抑制剂，能够抑制KDR (IC50:4 nM)，Flt-1 (IC50:20 nM)，FGFR1 (IC50:4 nM) 和 PDGFRα (IC50:2 nM)。

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].

PD-089828 是受体酪氨酸激酶 FGFR1、PDGFRβ 和 EGFR 的竞争性抑制剂，IC50分别为0.15、1.76 和 5.47 µM。它也是非受体酪氨酸激酶 c-Src 的非竞争性抑制剂，IC50 为 0.18 µM。

Brain Derived Acidic Fibroblast Growth Factor (1-11) 是多肽分子，其序列是 PALPEDGGSGAFPPGHFKDPKRLY。

PRN1371 是一种高效的、选择性的FGFR1-4和CSF1R 抑制剂，对FGFR1，FGFR2，FGFR3，FGFR4 和 CSF1R 的IC50值分别为 0.6，1.3，4.1，19.3 和 8.1 nM。

FGFR-IN-1 is a highly effective inhibitor targeting the Fibroblast Growth Factor Receptor (FGFR) group, comprising FGFR1, FGFR2, and FGFR3, with an impressive inhibitory concentration (IC 50) of less than 100 nM (US20130338134A1, example 219).