pdgf-receptor

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) (PDGF Receptor Tyrosine Kinase Inhibitor III)是一种多激酶抑制剂，可抑制 PDGFR、EGFR、FGFR、PKA 和 PKC 等。PDGFR Tyrosine Kinase Inhibitor III 可用于肌萎缩侧索硬化症的研究。

KN1022是血小板衍生生长因子（PDGF）受体磷酸化抑制剂，IC50为0.26μM。

CYM50260 是有效的、强选择性的鞘氨醇-1-磷酸 4 受体 (S1P4-R) 激动剂 (EC50= 45 nM)，对 S1P1-R，S1P2-R，S1P3-R 和 S1P5-R 无活性。

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。

AG-494 (Tyrphostin B48) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂，IC50为0.7 μM。它阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。它抑制 EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化，IC50为 1.1、39、45 和 6 μM。

Tyrphostin AG1296 (Tyrphostin AG 1296) 抑制人PDGF α和β受体以及相关干细胞因子受体的信号传导，是一种选择性血小板衍生生长因子受体抑制剂，IC50值为 0.8 μM。

AG 1295 是选择性血小板衍生生长因子受体酪氨酸激酶抑制剂。它能抑制 PDGFR 的自磷酸化，对 EGF 受体的自磷酸化无影响。

AG 370 是一种吲哚 tyrphostin，是一种有效的PDGF 诱导的有丝分裂抑制剂，IC50值为 20 μM。AG 370 对 EGF 受体的抑制作用较弱。

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].

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).

Ansornitinib (ANG-3070) 是一种具有口服活性的 KDR 和 PDGF 受体抑制剂，具有抗纤维化活性，抑制血小板衍生生长因子受体 (PDGFR) 和血管内皮生长因子受体 (VEGFR2)，可用于研究异常或过度纤维化引起的疾病。

SU 5402 是多靶点受体酪氨酸激酶抑制剂，能够抑制VEGFR2 (IC50:20 nM)，FGFR1 (IC50:30 nM)，PDGFRβ (IC50:510 nM)。