FGFR1 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S1490 Ponatinib (AP24534)

Ponatinib (AP24534)是一种新型有效的多靶点抑制剂,在无细胞试验中作用于Abl,PDGFRα,VEGFR2,FGFR1和Src,IC50分别为0.37 nM,1.1 nM,1.5 nM,2.2 nM和5.4 nM。

Selective FGFR1, IC50: 2.2 nM
S0487 Sulfatinib

Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50 of ranging between 1 and 24 nM.

Selective FGFR1, IC50: 15 nM
S1264 PD173074

PD173074是一种有效的FGFR1抑制剂,在无细胞试验中IC50约为25 nM,也能抑制VEGFR2,IC50为100-200 nM,作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。

Selective FGFR1, IC50: ~25 nM
S8161 ON123300

ON123300是有效的多靶点激酶抑制剂,对CDK4, Ark5, PDGFRβ, FGFR1, RET, Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。

Selective FGFR1, IC50: 26 nM; FGFR1, IC50: 260 nM
S7667 SU5402

SU5402是一种有效的多靶点受体激酶抑制剂,对VEGFR2,FGFR1,和PDGF-Rβ的IC50分别为20 nM,30 nM,和510 nM。

Selective FGFR1, IC50: 30 nM
S1164 Lenvatinib (E7080)

Lenvatinib (E7080)是一种多靶点抑制剂,无细胞试验中,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。Phase 3。

Selective FGFR1, IC50: 46 nM
S5240 Lenvatinib (E7080) Mesylate

Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.

Selective FGFR1, IC50: 46 nM
S1107 Danusertib (PHA-739358)

Danusertib (PHA-739358)是一种Aurora kinase抑制剂,作用于Aurora A/B/C,无细胞试验中IC50为13 nM/79 nM/61 nM,适度有效作用于Abl,TrkA,c-RET和FGFR1,对Lck,VEGFR2/3,c-Kit,CDK2等作用效果稍弱。Phase 2。

Selective FGFR1, IC50: 47 nM
S8493 PD-166866 (PD166866)

PD-166866是一种合成类小分子,抑制FGFR1的酪氨酸激酶作用,对FGFR1具有高度选择性并抑制FGFR1的自我磷酸化活性。

Selective FGFR1, IC50: 52.4 nM
S1084 Brivanib (BMS-540215)

Brivanib (BMS-540215)是一种ATP竞争性的VEGFR2抑制剂,IC50为25 nM,对VEGFR-1和FGFR-1抑制作用适中,但比作用于PDGFR-β效果强240多倍。Phase 3。

Selective FGFR1, IC50: 148 nM
S1138 Brivanib Alaninate (BMS-582664)

Brivanib Alaninate (BMS-582664)是BMS-540215的前体药物,是一种ATP竞争性的VEGFR2抑制剂,IC50为25 nM。

Selective FGFR1, IC50: 148 nM
S1040 Sorafenib (BAY 43-9006) tosylate

Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)RAF/MEK/ERK级联抑制剂,同时作用于Raf-1,wtBRAF和V599EBRAF,IC50分别为6 nM, 22 nM和38 nM。

Selective FGFR1, IC50: 580 nM
S7167 SSR128129E

SSR128129E是口服效果较好的变构FGFR抑制剂,IC50为1.9μM,对别的关联RTKs无效果。

Selective FGFR1, IC50: 1.9 μM
S2801 AZD4547

AZD4547是一种新型选择性的FGFR抑制剂,靶向作用于FGFR1/2/3,在无细胞试验中IC50为0.2 nM/2.5 nM/1.8 nM,对FGFR4, VEGFR2(KDR)具有微弱的作用活性,对IGFR, CDK2和p38几乎没有作用活性。Phase 2/3。

Pan FGFR1, IC50: 0.2 nM
S0088 Pemigatinib (INCB054828)

Pemigatinib is an orally active, selective FGFR inhibitor with IC50 of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has potential antineoplastic activity.

Pan FGFR1, IC50: 0.4 nM
S6539 ASP5878

ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.

Pan FGFR1, IC50: 0.47 nM
S8578 PRN1371

PRN1371是FGFR1-4的不可逆性共价抑制剂,对于FGFR1, 2, 3, 4和CSF1R的IC50分别为0.6、1.3、4.1、19.3、和8.1 nM。

Pan FGFR1, IC50: 0.6 nM
S2183 Infigratinib (BGJ398)

BGJ398 (NVP-BGJ398)是一种有效的,选择性FGFR抑制剂,作用于FGFR1/2/3,在无细胞试验中IC50为0.9 nM/1.4 nM/1 nM,作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上,对Abl, Fyn, Kit, Lck, Lyn和Yes几乎没有抑制活性。Phase 2。

Pan FGFR1, IC50: 0.9 nM
S8848 Futibatinib (TAS-120)

Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

Pan FGFR1, IC50: 1.8 nM
S7057 LY2874455

LY2874455是一个泛FGFR的抑制剂,对FGFR1,FGFR2, FGFR3, 和FGFR4的IC50值分别为2.8 nM, 2.6 nM, 6.4 nM,以及6 nM。并且也能抑制VEGFR2的活性,IC50为7 nM。Phase 1。

Pan FGFR1, IC50: 2.8 nM
S7714 FIIN-2

FIIN-2是一种不可逆的泛-FGFR抑制剂,对FGFR1/2/3/4的IC50分别为3.09 nM,4.3 nM,27 nM 和 45.3 nM。

Pan FGFR1, IC50: 3.09 nM
S8609 Derazantinib(ARQ-087)

Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.

Pan FGFR1, IC50: 4.5 nM
S1018 Dovitinib (TKI-258)

Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂,在无细胞试验中对III型(FLT3/c-Kit)作用最强,IC50为1 nM/2 nM,同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs,IC50为8-13 nM,但对InsR,EGFR,c-Met,EphA2,Tie2,IGF-1R和HER2作用较弱。Phase 4。

Pan FGFR1, IC50: 8 nM
S7765 Dovitinib (TKI258) Lactate

Dovitinib (TKI258) Lactate是Dovitinib的乳酸盐,Dovitinib是一种多靶点的PTK抑制剂,主要对第III类(FLT3/c-Kit)发挥作用,IC50为1 nM/2 nM,对第IV 类(FGFR1/3)和第V 类(VEGFR1-4) RTKs也有效,IC50为8-13 nM,对InsR,EGFR,c-Met,EphA2,Tie2,IGFR1 和HER2作用较差。Phase 4。

Pan FGFR1, IC50: 8 nM
S7665 Zoligratinib (Debio-1347)

CH5183284 是一种选择性口服有效的FGFR抑制剂,对FGFR1,FGFR2,FGFR3,和 FGFR4的IC50分别为 9.3 nM,7.6 nM,22 nM,和 290 nM 。Phase 1。

Pan FGFR1, IC50: 9.3 nM
S8882 ODM-203

ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.

Pan FGFR1, IC50: 11 nM
S7647 Lucitanib (E3810) hydrochloride

Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

Pan FGFR1, IC50: 17.5 nM
S8404 S49076

S49076是一种新型的、有效的MET, AXL/MERFGFR1/2/3抑制剂,IC50低于20 nM。

Pan FGFR1, IC50: 18 nM
S2774 MK-2461

MK-2461是一种有效的,多靶点抑制剂,作用于c-Met(WT/mutants)IC50为0.4-2.5 nM,对Ron,和Flt1作用效果稍弱;作用于c-Met比作用于FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA和TrkB选择性高8到30倍。Phase 1/2。

Pan FGFR1, IC50: 65 nM
S5234 Nintedanib Ethanesulfonate Salt

Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively.

Pan FGFR1, IC50: 69 nM
S1010 Nintedanib (BIBF 1120)

Nintedanib (BIBF 1120)是一种有效的三重血管激酶抑制剂,作用于VEGFR1/2/3FGFR1/2/3PDGFRα/β,在无细胞试验中IC50分别为34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。

Pan FGFR1, IC50: 69 nM
S1181 ENMD-2076

ENMD-2076选择性作用于Aurora AVEGFR(Flt3)IC50分别为14 nM和1.86 nM,作用于Aurora A比作用于Aurora B选择性高25倍,对VEGFR2/KDR和VEGFR3, FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。

Pan FGFR1, IC50: 92.7 nM
S2300 Ferulic Acid

Ferulic Acid 是一种羟基肉桂酸,是在Ferula assafoetida L或Ligusticum chuanxiong中发现的一种有机化合物。

Pan FGFR1, IC50: 3.78 μM