FGFR Inhibitor

ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC₅₀s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC₅₀s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner.

FGFR1 inhibitor 7 (compound 5) is an inhibitor of FGFR1 Tyrosine Kinase with IC₅₀ value of 0.33 nM. FGFR1 inhibitor 7 shows broad-spectrum cytotoxicity agasinst human cancer cell lines, and inhibits MOLT3 cells with IC₅₀ of 2.1 μM.

FGFR4-IN-22 (compound 10f) is a potent inhibitor of FGFR4, with the IC₅₀ of 5.4 nM. FGFR4-IN-22 serve as a potential lead compound targeting FGFR4 for anti-HCC agent development.

FGFR3-IN-6 is a potent and selective FGFR3 inhibitor with IC₅₀ value less than 350 nM. FGFR3-IN-6 can be used in research of cancer.

Lenvatinib-d₅ is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. FGFR-IN-14 inhibits FGFR1, FGFR2, FGFR3 and FGFR2 V564F gatekeeper mutant with IC₅₀s of 46, 41, 99, and 62 nM, respectively. FGFR-IN-14 strongly suppresses NCI-H520 lung cancer cells, SNU-16 and KATO III gastric cancer cells proliferation with IC₅₀s of 19, 59, and 73 nM, respectively.

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.

PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).

FGFR1 inhibitor-11 (compound 5g) binds to FGFR1, inactivation of its downstream ERK1/2 and IκBα/NF-κB signaling inhibited RANKL-induced osteoclastogenesis. FGFR1 inhibitor-11 has oral bioactivity.

Multi-kinase-IN-15 is an orally active multi-kinase inhibitor. Multi-kinase-IN-15 inhibits the kinase activity of MNK1, MNK2, ABL1, ABL1 T315I, FLT3, VEGFR2, RET, cKIT, FGFR2, PDGFRα, and PDGFRβ. Multi-kinase-IN-15 dose-dependently reduces phosphorylation of eIF4E and phosphorylated Crkl in tumor cells, and decreases phosphorylation of eIF4E in tumor tissues. Multi-kinase-IN-15 inhibits tumor growth. Multi-kinase-IN-15 can be used for research on chronic myeloid leukemia.

FGFR3-IN-10 is a FGFR3 inhibitor with an IC₅₀ of <350 nM. FGFR3-IN-10 is applicable to research related to cancer, systemic sclerosis, fibrosis, achondroplasia, thanatophoric dysplasia, and Muenke syndrome.

FGFR2 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

FGFR3-IN-4 is a selective FGFR3 inhibitor, with an IC₅₀ value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1.

Dabogratinib (GMP) is the GMP-grade version of Dabogratinib (HY-159642). Dabogratinib (TYRA-300) is an orally active, selective FGFR3 inhibitor with an IC₅₀ of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia.

IONIS-FGFR4Rx sodium scrambled negative control is the sequence scrambled negative control of IONIS-FGFR4Rx sodium.

Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with K_D of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models.

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 FGFR4^WT, FGFR3, FGFR4^V550L, FGFR2 and FGFR1, respectively.

BMS-645737 is an orally active, selective FGF receptor-1 and VEGF receptor-2 inhibitor. BMS-645737 selectively and competitively inhibits both VEGFR-2 and FGFR-1 tyrosine kinases. BMS-645737 has anti-angiogenic activity. BMS-645737 induces lesions in the incisor teeth.

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.

(S)-N-trans-feruloyloctopamine is an isomer of N-trans-feruloyloctopamine (HY-N2232). N-trans-feruloyloctopamine is a natural hydroxycinnamic acid amide compound derived from garlic husk, possessing tyrosinase inhibitory, FGF2 inhibitory, anti-melanogenic, and anti-tumor activities, and is used in research related to hepatocellular carcinoma, pigmentation disorders, and UVB-induced skin damage.