SNIPER(TACC3)-11 is a potent FGFR3-TACC3 degrader. SNIPER(TACC3)-11 reduces FGFR3-TACC3 protein levels and suppressed the growth of FGFR3-TACC3 positive cancer cells.

SUN11602 is a novel aniline compound, which mimics the neuroprotective mechanisms of basic fibroblast growth factor.

FGFR4-IN-2 is a potent, selective, covalent FGFR4 inhibitor with cellualr IC50 of 8.8 nM, 100-fold selectivity over FGFR2.FGFR4-IN-2 potently and selectively inhibit FGFR4 signaling through covalent modification of Cys552.FGFR4-IN-2 induces tumor regression in preclinical models of orthotopic and sorafenib-resistant HCC.

CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.CXF-009 forms covalent bonds with FGFR4(C477A) and FGFR4(C552A), respectively; display weak inhibition against FGFR1-3 with IC50 of 2579 nM, 2408 nM, and 977 nM.CXF-009 shows inhibitory effect agaginst FGFR4 muntants FGFR4(C477A), FGFR4(C552A), and FGFR4(C477A, C552A) with IC50 of 193 nM, 602 nM, and 1528 nM, respectively.CXF-009 inhibited the growth of Ba/F3 cells transformed with FGFR1-4 with IC50 values of 1562 nM, 1971 nM, 777 nM, and 38 nM, respectively.CXF-009 is slightly more reactive to GSH than PRN1371.

Alphastatin-C is a 14-amino acids peptide consisting of a C-terminal fragment of the α-chain of Fgn, is a potent inhibitor of bFGF induced endothelial cell (HUVEC-CS) activation in vitro.Alphastatin-C inhibits tumor angiogenesis and reduces melanoma tumor growth, inhibits the chorioallantoic membrane (CAM) angiogenesis in chick model.Alphastatin-C efficiently reduces tumor number and volume in a melanoma mice model, due to the impairment of tumor neovascularization in treated mice.Alphastatin-C is an efficient new antiangiogenic FGF-associated agent in vitro, and inhibitor of embryonic and tumor vascularization in vivo, also is an arteriogenic agent

EMI1 (EGFR MaMTH Inhibitor 1) is a novel EGFR ex19del/T790M/C797S inhibitor.EMI1, while potently reducing the interaction of EGFR triple mutant with Shc1 in our MaMTH-DS assay, did not behave as a TKI and displayed no inhibition of the kinase activity of EGFR triple-mutant protein invitro.EMI1 did, however, more strongly inhibit the viability and increase the caspase 3/7 activ-ity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells, as well as potently reduce PC9 EGFR ex19del/T790M/C797S organ-oid viability.EMI1 had a similar inhibi-tory effect on microtubule plus-end growth in both EGFR-WT and EGFR-C797S triple-mutant cells at 50–100 nM concentration. At 1 µM concentration, EMI1 strongly depolymerized inter-phase microtubules, perturbed spindle formation and induced strong mitotic block in PC9 EGFR ex19del/T790M/C797S cells after 20 h of treatment. EMI1 inhibited interaction of both proteins with EGFR at a level similar to that observed with Shc1, indicating it is not a specific inhibitor of the EGFR-Shc1 PPI interface. Rather, the loss of interaction mediated by EMI1 appears to be due to a more general alteration in EGFR activity.EMI1 induced EGFR degradation, and inhibited the activation of EGFR, ERK, AKT and S6 in PC9-ex19del and PC9-ex19del/T790M cells.

Derazantinib (Derazantinib) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.

FGFR2-IN-2 is a selective FGFR2 inhibitor with an IC50 of 29 nM.

PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, 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).

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.

FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer.

SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer.

FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1.

NSC12 is a PTX3-derived anti-FGF small molecule, inhibits FGF-dependent tumor growth, angiogenesis, and metastases,acts as a small-molecule FGF trap in cancer therapy.

FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.

Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.