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Cat. No. Product Name Target Signaling Pathways
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).
TQ0256 FGFR4-IN-1

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
FGFR4-IN-1 是一种 FGFR4 抑制剂 (IC50:0.7 nM)。
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)。
T61304 FGFR2-IN-1

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
FGFR2-IN-1是一种 FGFR 抑制剂,对 FGFR1FGFR2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。
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].
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。
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。
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FGFR1FGFR4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。

化合物

FGFR-IN-1
Cat.No: T39001
Synonym:
Target:
FGFR4-IN-1
Cat.No: TQ0256
Synonym:
Target: FGFR
Futibatinib
Cat.No: T5044
Synonym: TAS120,FGFR-IN-1
Target: FGFR
Tyrosine kinase-IN-1
Cat.No: T5466
Synonym:
Target: VEGFR, FGFR, FLT, PDGFR
FGFR2-IN-1
Cat.No: T61304
Synonym:
Target: FGFR
PD153035
Cat.No: T2041
Synonym: NSC 669364,SU-5271,ZM 252868,AG1517
Target: EGFR
JK-P3
Cat.No: T4425
Synonym:
Target: VEGFR
FGFR-IN-7
Cat.No: T61528
Synonym:
Target:
FGFR-IN-2
Cat.No: T62653
Synonym:
Target:
FGFR4-IN-16
Cat.No: T79880
Synonym:
Target: FGFR
FGFR-IN-3
Cat.No: T61660
Synonym:
Target:
ALK2-IN-5
Cat.No: T79020
Synonym:
Target:
FGFR3-IN-1
Cat.No: T64107
Synonym:
Target:
FGFR3-IN-7
Cat.No: T82404
Synonym:
Target: FGFR
FGFR-IN-11
Cat.No: T79257
Synonym:
Target: FGFR
Multi-kinase-IN-2
Cat.No: T63967
Synonym:
Target:
FGFR3-IN-6
Cat.No: T82405
Synonym:
Target: FGFR
CE-245677 mesylate
Cat.No: T68286
Synonym:
Target:
Irpagratinib
Cat.No: T79850
Synonym: ABSK011
Target: FGFR
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