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FGFR4 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Fgfr4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Fgfr4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Fgfr4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Fgfr4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases . FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC) .
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4V550L, FGFR4V550M and FGFR4C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
FGFR4-IN-11 (Compound 30) is a potent, selective, covalent FGFR4 inhibitor with an IC50 of 2.1 nM. FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and shows antitumor activity .
FGFR4-IN-9 (Compound 6O) is a selective FGFR4 inhibitor with an IC50 of 75.3 nM. FGFR4-IN-9 effectively inhibits both the growth and angiogenesis of HCC .
FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research .
FGFR4-IN-14 (Compound 27i) is a FGFR4 inhibitor (IC50: 2.4 nM. FGFR4-IN-14 inhibits the proliferation of V550L and N535K mutant strains, with IC50s of 21 nM, 2.5 nM, 171 nM against huh7, BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells respectively. FGFR4-IN-14 has potent antitumor efficacy in the Huh7 xenograft model. FGFR4-IN-14 can be used for research of hepatocellular carcinoma (HCC) .
FGFR4-IN-17 (Compound (S)-23) is a piperazinyl diflurindan derivative containing pyridinyl. FGFR4-IN-17 is a FGFR inhibitor with IC50 values of 24.2, 16.1, 78.0, and 68.0 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. FGFR4-IN-17 has antitumor activity .
FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3 .
CXF-009 is a selective and covalent FGFR4 inhibitor, with the IC50 of 48 nM. CXF-009 targeting Cys477 and Cys552 of FGFR4, and can be used for the study of hepatocellular carcinoma .
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4(FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling .
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively .
BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4(FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity .
E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively .
Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Infigratinib (BGJ-398; NVP-BGJ398) is a potent inhibitor of the FGFR family with IC50s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma .
FGFR-IN-2 (compound 1) is a potent FGFR inhibitor with IC50s of 7.3 nM, 4.3 nM, 7.6 nM, 11 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-2 has the potential for cancer research .
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively .
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity .
FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively .
The leptin R/LEPR protein is a receptor protein that binds to the hormone leptin. It plays a vital role in regulating energy balance and body weight. FGFR-4 Protein, Human (HEK293, Fc) is the recombinant human-derived FGFR-4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of FGFR-4 Protein, Human (HEK293, Fc) is 348 a.a., with molecular weight of 95-112 kDa.
The FGFR-4 protein is a tyrosine protein kinase and cell surface receptor for fibroblast growth factor that regulates diverse cellular processes such as proliferation, differentiation, migration, lipid metabolism, and bile acid biosynthesis. Notably, it contributes to the downregulation of the bile acid synthase CYP7A1 in response to FGF19. FGFR-4 Protein, Human (HEK293, His) is the recombinant human-derived FGFR-4 protein, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-4 Protein, Human (HEK293, His) is 369 a.a., with molecular weight of ~60 kDa.
FGFR-4 protein is a tyrosine protein kinase that serves as a cell surface receptor for fibroblast growth factor and controls proliferation, differentiation, migration, lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism, and phosphate and other cellular processes homeostasis. It significantly downregulates CYP7A1 in response to FGF19. FGFR-4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived FGFR-4 protein, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-4 Protein, Mouse (HEK293, His) is 196 a.a., with molecular weight of 58-80 kDa.
The FGFR-4 protein is a tyrosine-protein kinase receptor for fibroblast growth factor that regulates cellular processes, lipid metabolism, bile acid biosynthesis, and more. Its effects include downregulation of CYP7A1 in response to FGF19. FGFR-4 Protein, Rat (HEK293, His) is the recombinant rat-derived FGFR-4 protein, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-4 Protein, Rat (HEK293, His) is 367 a.a., with molecular weight of 64-68 kDa.
FGFR-4 protein is a tyrosine protein kinase that serves as a cell surface receptor for fibroblast growth factor and controls proliferation, differentiation, migration, lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism, and phosphate and other cellular processes homeostasis. It significantly downregulates CYP7A1 in response to FGF19. FGFR-4 Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived FGFR-4 protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of FGFR-4 Protein, Mouse (HEK293, His-Fc) is 366 a.a., with molecular weight of 100-110 kDa.
The FGFR-4 protein is a tyrosine-protein kinase receptor for fibroblast growth factor that regulates cellular processes, lipid metabolism, bile acid biosynthesis, and more. Its effects include downregulation of CYP7A1 in response to FGF19. FGFR-4 Protein, Rat (HEK293, Fc, Solution) is the recombinant rat-derived FGFR-4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of FGFR-4 Protein, Rat (HEK293, Fc, Solution) is 351 a.a., with molecular weight of ~110 kDa.
The FGFR-4 protein is a cell surface receptor for tyrosine kinase and fibroblast growth factor. FGFR4, a receptor for FGF-1 and FGF-3 highly expressed in cancer cells, promotes tumor progression in colon cancer by activating Mek/Erk and MMP-7. FGFR-4 Protein, Rhesus Macaque (HEK293, Fc) is the recombinant Rhesus Macaque-derived FGFR-4 protein, expressed by HEK293 , with C-mFc labeled tag. The total length of FGFR-4 Protein, Rhesus Macaque (HEK293, Fc) is 369 a.a., with molecular weight of ~65.6 KDa.
The FGFR-4 protein is a cell surface receptor for tyrosine kinase and fibroblast growth factor. FGFR4, a receptor for FGF-1 and FGF-3 highly expressed in cancer cells, promotes tumor progression in colon cancer by activating Mek/Erk and MMP-7. FGFR-4 Protein, Rhesus Macaque (HEK293, His) is the recombinant Rhesus Macaque-derived FGFR-4 protein, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-4 Protein, Rhesus Macaque (HEK293, His) is 348 a.a., with molecular weight of ~60-80 KDa.
The FGFR-4 protein is a tyrosine protein kinase and cell surface receptor for fibroblast growth factor that regulates diverse cellular processes such as proliferation, differentiation, migration, lipid metabolism, and bile acid biosynthesis. Notably, it contributes to the downregulation of the bile acid synthase CYP7A1 in response to FGF19. FGFR-4 Protein, Human (Biotinylated, HEK293, His) is the recombinant human-derived FGFR-4 protein, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-4 Protein, Human (Biotinylated, HEK293, His) is 369 a.a., with molecular weight of ~60.8 kDa.
The FGFR-4 protein is a tyrosine protein kinase and cell surface receptor for fibroblast growth factor that regulates diverse cellular processes such as proliferation, differentiation, migration, lipid metabolism, and bile acid biosynthesis. Notably, it contributes to the downregulation of the bile acid synthase CYP7A1 in response to FGF19. FGFR-4 Protein, Human (HEK293, His-Avi) is the recombinant human-derived FGFR-4 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of FGFR-4 Protein, Human (HEK293, His-Avi) is 348 a.a., with molecular weight of 60-75 kDa.
The FGFR-4 protein is a tyrosine protein kinase and cell surface receptor for fibroblast growth factor that regulates diverse cellular processes such as proliferation, differentiation, migration, lipid metabolism, and bile acid biosynthesis. Notably, it contributes to the downregulation of the bile acid synthase CYP7A1 in response to FGF19. FGFR-4 Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived FGFR-4 protein, expressed by HEK293 , with C-His, C-Avi labeled tag. The total length of FGFR-4 Protein, Human (Biotinylated, HEK293, His-Avi) is 348 a.a., with molecular weight of 55-72 kDa.
The FGFR-4 protein is a tyrosine-protein kinase receptor for fibroblast growth factor that regulates cellular processes, lipid metabolism, bile acid biosynthesis, and more. Its effects include downregulation of CYP7A1 in response to FGF19. FGFR-4 Protein, Rat (HEK293, C-hFc) is the recombinant rat-derived FGFR-4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of FGFR-4 Protein, Rat (HEK293, C-hFc) is 351 a.a., with molecular weight of ~110 kDa.
Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
