FGFR

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.

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively.

FGFR-IN-1 is a potent FGFR inhibitor with an IC50 of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219).

FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor with IC50s of 389, 29, and 758 nM for FGFR1, FGFR2, and FGFR3, respectively.

Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer.

ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment.

MAX-40279 is a dual and potent inhibitor of FLT3 kinase and FGFR kinase.

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.

Aprutumab?(BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has?the?potential?for?solid tumors research.

Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has the potential for cancer research.

E7090 is an effective selective FGFR inhibitor with oral activity, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4 respectively.

FGFR3-IN-5 is an effective selective inhibitor of FGFR3, with IC50 values of 3, 44, and 289 nM for FGFR3, FGFR2, and FGFR1 respectively. It can be used in cancer research.

Vofatamab (B-701) is a monoclonal antibody (mAb) that targets FGFR3. Vofatamab blocks the activation of both wild-type and mutated receptors. It is being studied for its potential use in metastatic urothelial carcinoma (MUC).

Vosoritide (BMN 111) acetate is a natriuretic peptide receptor 2 (NPR2) agonist that can stimulate the proliferation and differentiation of chondrocytes, promoting bone growth.

FGFR2-IN-1 is a selective FGFR2 inhibitor with an IC50 of 140 nM.

Fazpilodemab (BFKB8488A) is a humanized, agonistic, bispecific antibody targeting fibroblast growth factor receptor 1c (FGFR1c) and Klothoβ.

Recifercept (TA-46) is a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule.

Efruxifermin is an Fc-FGF21 fusion protein (human IgG1 Fc domain linked to a modified human FGF21).

Pazopanib-13C,d3 (drochloride) is the deuterium and 13C labeled Pazopanib drochloride.

LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM.

FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM).

Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM).

Resigratinib (KIN-3248) is a FGFR tyrosine kinase inhibitor, with antineoplastic effect.