Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T62653 |
FGFR-IN-2
|
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FGFR-IN-2 (compound 1) 是一种有效的 FGFR 抑制剂,能够作用于 FGFR1 (IC50: 7.3 nM)、FGFR2 (IC50: 4.3 nM)、FGFR3 (IC50: 7.6 nM) 和 FGFR4 (IC50: 11 nM)。FGFR-IN-2 具有潜力进行癌症研究。 | |||
T1948 |
AZD4547
|
VEGFR; FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
AZD4547 是FGFR 家族抑制剂,能够作用于FGFR1 (IC50:0.2 nM),FGFR2 (IC50:2.5 nM),FGFR3 (IC50:1.8 nM) 和FGFR4 (IC50:165 nM)。 | |||
T4425 |
JK-P3
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
JK-P3 是广谱 VEGFR2抑制剂。它能够抑制 VEGF-A 刺激的 VEGFR2 激活和细胞内信号转导,也可阻碍内皮单层细胞迁移和血管生成,影响成纤维细胞生长因子受体激酶在体外的活性。它具有抗血管生成的作用。 | |||
T3714 |
SUN11602
SUN 11602 |
ERK; FGFR | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
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。 | |||
T79880 |
FGFR4-IN-16
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR4-IN-16 (CY-15-2)为FGFR-4选择性共价抑制剂,适用于癌症研究领域。 | |||
T10372 |
ARQ 069
|
Others | Others |
ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in K | |||
T63967 |
Multi-kinase-IN-2
|
||
Multi-kinase-IN-2 是口服具有活力的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 能够显著抑制血管激酶的活性,如 VEGFR-1/2/3、PDGFRα/β、FGFR-1、LYN 和 c-KIT 激酶。Multi-kinase-IN-2 能够明显减弱 AKT 和 ERK 蛋白的磷酸化,并可诱导细胞凋亡 (apoptosis),具有抗癌作用。 | |||
T36292 |
NSC 12
|
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NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 μM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs). NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 μM, preventing them from forming HSPG/FGF/FGFR ternary complexes. NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduc... | |||
T3512 |
S49076 HCl
S-49076 Hydrochloride |
FGFR; c-Met/HGFR; TAM Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
S49076 HCl (S-49076 Hydrochloride) 是 MET、AXL/MER 和 FGFR1/2/3 的有效抑制剂。S49076 HCl 在体外和体内有效阻断 MET、AXL 和 FGFR 的细胞磷酸化并抑制下游信号传导。在细胞模型中,S49076 HCl (S-49076 Hydrochloride) 抑制 MET 和 FGFR2 依赖性胃癌细胞的增殖,阻断 MET 驱动的肺癌细胞迁移,并抑制表达 FGFR1/2 和 AXL 的肝癌细胞的集落形成。在肿瘤异种移植模型中,建立了口服 S49076 HCl (S-49076 Hydrochloride) 后 MET 和 FGFR2 抑制的良好药代动力学/药效学关系,并与对肿瘤生长的影响密切相关。 |