FGFR Inhibitor

Formononetin-d₃-1 is the deuterium-labeled Formononetin (HY-N0183).

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.

Nintedanib-¹³C,d₃ is the ¹³C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

PDK1-IN-1 (Compound 2-11) is a PDK1 inhibitor. PDK1-IN-1 is also useful as inhibitor of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. PDK1-IN-1 selectively inhibits microtubule affinity regulating kinase (MARK). PDK1-IN-1 can be used for researches of myeloproliferative disorders, cancer and Alzheimer's disease.

Fgfr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Fgfr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC₅₀s of 4.5, 1.8, and 4.5 nM, respectively.

MAX-40279 hemiadipate is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate is also effective against the FLT3 mutants such as FLT3^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hemiadipate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemiadipate can be used for the research of acute myelogenous leukemia (AML).

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.

OM-RCA-01 is an anti-FGFR1 monoclonal antibody with a K_d of 1.59 nM for human FGFR1. OM-RCA-01 inhibits the phosphorylation of FGFR1, blocks FGF-mediated signaling pathways, and suppresses the proliferation of downstream tumor cells. OM-RCA-01 delays tumor growth in lung cancer and renal cancer xenograft models expressing FGFR1. When combined with Nivolumab, OM-RCA-01 enhances the release of IFN-γ and IL-2. OM-RCA-01 is applicable for the research of lung cancer and renal cell carcinoma.

Umedaptanib pegol sodium is a pegylated aptamer, which can target fibroblast growth factor-2 (FGF2). It is used for the study of neovascular age-related macular degeneration (nAMD).

Nintedanib-d₃ is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.

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

IONIS-FGFR4Rx (ISIS 463588) sodium is an antisense inhibitor of fibroblast growth factor receptor 4 (FGFR4), which is promising for research of renal diseases.

Pazopanib-d₆ is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

Fgfr1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Fgfr1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ponatinib-d₈ (AP24534-d₈) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

Erdafitinib (Standard) is the analytical standard of Erdafitinib. This product is intended for research and analytical applications. Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

Nintedanib (Standard) is the analytical standard of Nintedanib. This product is intended for research and analytical applications. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC₅₀s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.