fgfr

FGFR-IN-4 is a potent inhibitor of FGFR. FGFR-IN-4 has potential for cancer disease studies.

FGFR-IN-6 (Compound 5) is an FGFR inhibitor.

FGFR-IN-8 is a potent, orally active FGFR inhibitor that inhibits both wild-type and mutant FGFR. FGFR-IN-8 acts on FGFR1 (IC50<0.5 nM), V564F-FGFR2 (IC5016: 189.1 nM), N549H-FGFR2 (IC50<0.5 nM), V555M-FGFR3 (IC50: 22.6 nM), FGFR3 (IC50<0.5 nM) and FGFR 4 (IC50: 7.30 nM), V555M-FGFR3 (IC50: 22.6 nM), FGFR3 (IC50<0.5 nM) and FGFR 4 (IC50: 7.30 nM). FGFR-IN-8 induces apoptosis and exhibits anti-cancer effects.

FGFR-IN-9 is a potent, reversible, and orally active inhibitor of the fibroblast growth factor receptor (FGFR) family, demonstrating IC50 values of 17.1 nM for FGFR4 WT, 29.6 nM for FGFR3, 30.7 nM for FGFR4 V550L, 46.7 nM for FGFR2, and 64.3 nM for FGFR1, respectively.

FGFR-IN-2 (compound 1) is a potent inhibitor of FGFR, acting on FGFR1 (IC50: 7.3 nM), FGFR2 (IC50: 4.3 nM), FGFR3 (IC50: 7.6 nM) and FGFR4 (IC50: 11 nM).

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].

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).

FGFR-IN-5 is a potent inhibitor of FGFR. FGFR-IN-5 has potential for research in cancer diseases.

FGFR-IN-11 (compound I-5) is an orally active, covalent inhibitor of FGFR, exhibiting IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4). This compound demonstrates nanomolar potency in inhibiting proliferation of various cancer cells and significantly hinders tumor growth in xenograft mouse models [1].

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].

FGFR2-IN-1 is an FGFR inhibitor that inhibits FGFR1, FGFR2, and FGFR3 with IC50s of 460, 140, and 2200 nM, respectively.FGFR2-IN-1 can be used for the study of cancers associated with FGFR2.CAS 번호13460-73-81-1

Futibatinib (FGFR-IN-1) is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.

FGFR3-IN-7 is a potent, selective inhibitor of FGFR 3, demonstrating an IC50 value of less than 350 nM , and is utilized in cancer research [1].

FGFR3-IN-6 is a potent, selective inhibitor of FGFR 3, exhibiting an IC50 value of less than 350 nM , and is utilized in cancer research [1].

FIIN-1 (FGFR irreversible inhibitor-1) is an irreversible and selective FGFR inhibitor with Kd of 2.8, 6.9, 5.4, 120, 32 and 120 nM for FGFR1, FGFR2, FGFR3, FGFR4, Flt1, Flt14, respectively.FIIN-1 inhibited FGFR1, FGFR2, FGFR3, FGFR4, with IC50 of 9.2, 6.2, 11.9 and 189 nM. FIIN-1 inhibited FGFR1, FGFR2, FGFR3 and FGFR4, with IC50s of 9.2, 6.2, 11.9 and 189 nM, respectively.

FGFR4-IN-16 (CY-15-2) is a covalent inhibitor targeting FGFR-4, utilized in cancer research [1].

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoindin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

FGFR4-IN-10 (compound 5a) is a selective and potent inhibitor of FGFR4 (IC50: 70.7 nM).FGFR4-IN-10 does not inhibit other FGFR family members (i.e., FGFR1, FGFR2, and FGFR3).

FGFR4-IN-1 is a potent FGFR4 inhibitor (IC50: 0.7 nM).

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.

FGFR3-IN-1 (compound 1) is a fibroblast growth factor receptor (FGFR) inhibitor that inhibits FGFR1 (IC50: 40 nM), FGFR2 (IC50: 5.1 nM) and FGFR3 (IC50: 12 nM).

FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].

FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].

FGFR2-IN-2 is a specific FGFR2 inhibitor that inhibits FGFR1, FGFR2, and FGFR3, and can be used in the study of cancer and cardiovascular disease.

FGFR4-IN-7 is a covalent, reversible FGFR4 inhibitor (IC50: 0.42 μM) that blocks the FGFR4 signaling pathway, thereby inducing apoptosis.

FGFR3-IN-4 is a selective inhibitor targeting FGFR3, demonstrating an IC50 value of under 50 nM. This compound exhibits at least a tenfold greater selectivity for FGFR3 compared to FGFR1.

FGFR1 inhibitor-6 is a potent inhibitor of FGFR1 (IC50: 16.31 nM) with cytotoxic activity. fGFR1 inhibitor-6 is capable of blocking the cell cycle in pro-G1 and G2/M phases and inducing apoptosis.

FGFR1 inhibitor-10 (Compound 4i), with an IC50 of 28 nM, effectively inhibits FGFR1 phosphorylation. This compound demonstrates anti-angiogenic and anti-invasion properties, as well as a significant anti-tumor effect [1].

FGFR2-IN-3 hydrochloride is a selective, orally active FGFR2 inhibitor.

FGFR1 Inhibitor 7 (compound 5), a potent FGFR1 tyrosine kinase inhibitor, exhibits an IC50 of 0.33 nM against its target and demonstrates broad-spectrum cytotoxicity against human cancer cell lines. Additionally, it inhibits MOLT3 cells with an IC50 of 2.1 μM [1].

FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM. It targets the ATP-binding pocket of FGFR1 and demonstrates anticancer activity [1].

FGFR4-IN-14 (Compound 27i) is a selective FGFR4 inhibitor with an IC50 of 2.4 nM, showing potent inhibition of cell proliferation in the V550L and N535K mutant strains. Specifically, it registers IC50 values of 21 nM against Huh7 cells, 2.5 nM against BaF3/ETV6-FGFR4-V550L cells, and 171 nM against BaF3/ETV6-FGFR4-N535K cells. Demonstrating significant antitumor efficacy in the Huh7 xenograft model, FGFR4-IN-14 is utilized in the research of hepatocellular carcinoma (HCC) [1].

FGFR3-IN-2 (compound 18b) is a potent and selective FGFR3 inhibitor that inhibits FGFR3 (IC50: 4.1 nM) and VEGFR2 (IC50: 570 nM).

FGFR4-IN-9 is a selective inhibitor of FGFR4 (IC50: 75.3 nM) that effectively inhibits the growth and angiogenesis of hepatocellular carcinoma cells.

FGFR4-IN-11 is a selective, potent, covalently bound FGFR4 inhibitor (IC50: 2.1 nM). FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and exhibits anticancer effects.

FGFR1 inhibitor-8 (Compound 9), an FGFR1 inhibitor with an IC50 of 0.5 nM, binds to the ATP-binding pocket of FGFR1 and exhibits anticancer activity [1].

FGFR2-IN-3 is an orally active selective FGFR2 inhibitor[1].

FGFR3-IN-5 is a potent, selective FGFR3 inhibitor, exhibiting IC50 values of 3 nM (FGFR3), 44 nM (FGFR2), and 289 nM (FGFR1), respectively. This compound is utilized in cancer research.

FGFR4-IN-8 (Compound 7v) is an ATP-competitive inhibitor that covalently and highly selectively targets both the wild-type and gatekeeper mutant forms of FGFR4. It shows excellent inhibitory potency with IC50s of 0.5 nM for FGFR4, 0.25 nM for FGFR4 V550L, 1.6 nM for FGFR4 V550M, and 931 nM for FGFR4 C552S. Additionally, FGFR4-IN-8 has a potent antiproliferative effect on Hep3B hepatocellular carcinoma cells, with an IC50 of 29 nM, and demonstrates moderate antitumor efficacy in vivo in a Huh-7 xenograft model in nude mice [1].

FGFR4-IN-6 is a covalent, reversible FGFR4 inhibitor (IC50: 5.4 nM) that exhibits good oral pharmacokinetic properties. In a xenograft mouse model of the Hep3B2.1-7 HCC cell line, FGFR4-IN-6 was able to significantly induce tumour regression without significant toxicity.

Aprutumab (BAY 1179470) is a human FGFR2 monoclonal antibody with affinity to FGFR2 isoforms FGFR2-IIIB and FGFR2-IIIC. Aprutumab is commonly used to synthesize antibody-drug conjugates.

AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays).

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.

Erdafitinib (JNJ-42756493) is a quinoxaline derivative compound, acts on FGFR1/2/3/4.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Fisogatinib (BLU-554) is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).

Derazantinib (ARQ-087) (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5 nM/1.8 nM/4.5 nM).

Ferulic Acid (Coniferic acid) is a highly abundant phenolic phytochemical and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.It can be absorbed by the small intestine and excreted through the urine.

Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.