Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0256 |
FGFR4-IN-1
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR4-IN-1 是一种 FGFR4 抑制剂 (IC50:0.7 nM)。 | |||
T39001 |
FGFR-IN-1
|
||
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). | |||
T5044 |
Futibatinib
TAS120,FGFR-IN-1 |
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Futibatinib (FGFR-IN-1) 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。它抑制突变型和野生型 FGFR2,且 IC50相似(wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM)。 | |||
T5466 |
Tyrosine kinase-IN-1
|
VEGFR; FGFR; FLT; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
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)。 | |||
T11279 |
FGFR1/DDR2 inhibitor 1
|
Discoidin Domain Receptor (DDR); FGFR; Others | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
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。 | |||
T39992 |
FGFR1 inhibitor-2
FGFR1 inhibitor-2 |
||
FGFR1 inhibitor-2 (with an IC50 of 4.55 μM in MDA-MB-231 cells) is a potent inhibitor of FGFR1. It is specifically useful for studying metastatic triple-negative breast cancer. | |||
T64107 |
FGFR3-IN-1
|
||
FGFR3-IN-1 (compound 1) 是一种成纤维细胞生长因子受体 (FGFR) 抑制剂,可抑制FGFR1 (IC50: 40 nM),FGFR2 (IC50: 5.1 nM) 和 FGFR3 (IC50: 12 nM)。FGFR3-IN-1 能够用于研究膀胱癌。 | |||
T78845 |
FGFR1/VEGFR2-IN-1
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR1/VEGFR2-IN-1 (compound 2b) 为FGFR1/VEGFR2抑制剂,适用于癌症研究。 | |||
T78830 |
FGFR1 inhibitor 7
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR1 inhibitor7(compound 5),作为一种FGFR1络氨酸激酶抑制剂,具有0.33 nM的IC50。它对多种人癌细胞系显示出广谱的细胞毒性,能在2.1 μM的IC50抑制MOLT3细胞系。 | |||
T63816 | FGFR1 inhibitor-6 | ||
FGFR1 inhibitor-6 是 FGFR1 的有效抑制剂 (IC50: 16.31 nM),具有细胞毒活性。FGFR1 inhibitor-6 能够将细胞周期阻滞在前 G1 和 G2/M 期并诱导细胞凋亡 (apoptosis) 。 | |||
T78832 |
FGFR1 inhibitor-9
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR1inhibitor-9(Compound 9),一种FGFR1抑制剂(IC50为0.85 nM),可与FGFR1的ATP结合袋发生结合,并展现出抗癌活性。 | |||
T79686 | FGFR1 inhibitor-10 | FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR1inhibitor-10 (Compound 4i)为一种选择性的FGFR1抑制剂,其IC50值为28 nM。该化合物有效阻断FGFR1磷酸化,并展现出了明显的抗血管生成和抗侵袭特性,具有潜在的抗肿瘤效果。 | |||
T78831 |
FGFR1 inhibitor-8
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR1inhibitor-8(化合物9)是一种高效的FGFR1抑制剂,其IC50s为0.5 nM,能够与FGFR1的ATP结合口袋发生相互作用,并显示出抗癌活性。 | |||
T61304 |
FGFR2-IN-1
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR2-IN-1是一种 FGFR 抑制剂,对 FGFR1、FGFR2和FGFR3具有抑制作用, IC50 分别为460、140和2200 nM。FGFR2-IN-1 可用于研究与 FGFR2 相关的癌症。 | |||
T2041 |
PD153035
NSC 669364,SU-5271,ZM 252868,AG1517 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
PD153035 (NSC-669364) 是一种EGFR 抑制剂,Ki 和IC50值分别为6和25 pM。 | |||
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。 | |||
T61528 |
FGFR-IN-7
|
||
FGFR-IN-7 (compound 17) is an orally active, potent FGFR modulator with the ability to penetrate the blood-brain barrier. It exhibits neuroprotective properties, enhancing brain exposure and decreasing the likelihood of phospholidosis. FGFR-IN-7 proves valuable for research on neurodegenerative diseases [1]. | |||
T62653 |
FGFR-IN-2
|
||
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。 | |||
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。 | |||
T79020 | ALK2-IN-5 | ||
ALK2-IN-5为一种吡唑并嘧啶化合物,具有抑制ALK2及FGFR活性的作用。该抑制剂常用于癌症等疾病的研究,这些疾病与ALK2及/或FGFR的活性有关。 | |||
T61660 | FGFR-IN-3 | ||
FGFR-IN-3 (compound 6) is a highly potent and orally active modulator of FGFR (fibroblast growth factor receptor). It has the ability to penetrate the blood-brain barrier (BBB). Additionally, FGFR-IN-3 exhibits significant neuroprotective properties. Therefore, it holds potential for research on neurodegenerative diseases [1]. | |||
T82404 | FGFR3-IN-7 | FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR3-IN-7为高选择性FGFR3抑制剂,显示出小于350 nM 的IC50效价,主要用于癌症相关研究。 | |||
T79257 | FGFR-IN-11 | FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR-IN-11(compound I-5)是一款具备口服活性的共价pan-FGFR抑制剂,对FGFR1至FGFR4的IC50值分别为9.9 nM、3.1 nM、16 nM和1.8 nM。该化合物能够在纳摩尔水平有效抑制多种肿瘤细胞的增殖,并在荷瘤小鼠模型中显著地抑制肿瘤生长。 | |||
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。 | |||
T82405 |
FGFR3-IN-6
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
FGFR3-IN-6为FGFR3选择性抑制剂,具有低于350 nM 的IC50,适用于癌症研究领域。 | |||
T68286 |
CE-245677 mesylate
|
||
CE-245677 is a selective, orally active Tie2 kinase inhibitor identified by Pfizer previously in development for the treatment of certain cancers. CE-245,677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, resp., displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR) and gene family panels, and demonstrates good oral absorption in in vivo rat PK studies (F=80%). | |||
T79850 |
Irpagratinib
ABSK011 |
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Irpagratinib (ABSK011)是一种靶向FGFR4(IC50<10 nM)的口服活性酪氨酸激酶抑制剂,可抑制FGFR4自磷酸化并阻断其信号转导至下游途径。在小鼠、大鼠和狗的PK研究中,Irpagratinib表现出高暴露量,并在皮下异种移植肿瘤模型中展示抗肿瘤活性。 |