FGFR Inhibitor

FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, with the IC₅₀s of 8 nM, 4 nM and 3.8 nM, respectively. FGFR-IN-16 plays an important role in cancer research^1].

FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4^V550L, FGFR4^V550M and FGFR4^C552S with IC₅₀s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC₅₀ value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model.

ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC₅₀ = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC₅₀ = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations.

FGFR1/VEGFR2-IN-1 (compound 2b) is an FGFR1/VEGFR2 inhibitor. FGFR1/VEGFR2-IN-1 can be used for cancer research.

FGFR3-IN-3 (compound 40a) is a potent and pan-FGFR inhibitor, with IC₅₀s of 2.1 nM, 3.1 nM, 4.3 nM and 74 nM for FGFR1, 2, 3, and 4, respectively. FGFR3-IN-3 can be used for the research of bladder cancer.

PNU-145156E (FCE26644) is an angiogenesis inhibitor with anti-tumor activity. PNU-145156E inhibits the binding of bFGF to its receptor and inhibits bFGF-induced endothelial cell proliferation and motility.

FGFR3-IN-1 (compound 1) is a fibroblast growth factor receptor (FGFR) inhibitor, with IC₅₀s of 40 nM, 5.1 nM, and 12 nM for FGFR1, 2, and 3, respectively. FGFR3-IN-1 can be used for the research of bladder cancer.

MPT0L145 is a PIK3C3/FGFR inhibitor, with a K_d value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC.

CXF-007 is a potent and specific FGFR4 inhibitor with a IC₅₀ value of 7 nM. CXF-007 has antitumor activity.

Ferulic acid-¹³C₃ is the ¹³C-labeled Ferulic acid. Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.

FGFR1 inhibitor-14 (compound 28) is a FGFR1 inhibitor, which can be used in anti-cancer research.

Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

GP369 is a humanized FGFR2-IIIb-specific antibody. GP369 significantly inhibits the proliferation of tumor cells. GP369 can significantly inhibit phosphorylation of FGFR2 and downstream signaling pathways. GP369 can be used for research on cancer such as gastric cancer and breast cancer.

FGFR2/3-IN-2 (compound 10) is an orally active FGFR2 and FGFR3 inhibitor. FGFR2/3-IN-2 inhibits FGFR2 and FGFR3 with IC₅₀s of 3.7 nM and 31.2 nM (preincubation time 1 h), respectively. FGFR2/3-IN-2 spares FGFR1/4 and other kinases without causing diarrhea and serum phosphate elevation in vivo. FGFR2/3-IN-2 induces tumor stasis or regression in the SNU-16 gastric cancer model.

PRN1371 (Standard) is the analytical standard of PRN1371 (HY-101768). This product is intended for research and analytical applications. PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC₅₀s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.

Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.

PD-166866 (Standard) is the analytical standard of PD-166866 (HY-101296). This product is intended for research and analytical applications. PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.

Si5-N14 is a key component of siloxane-incorporated lipid nanoparticles (SiLNP), possessing pro-vascular repair and anti-tumor activities. In the transgenic GFP mouse model, Si5-N14 can mediate CRISPR-Cas9 editing. In the Lewis lung carcinoma (LLC) tumor-bearing mouse model, Si5-N14 can knock out the expression of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) to exert an anti-tumor effect. In a mouse model of lung injury induced by viral infection, the delivery of Fibroblast Growth Factor-2 (FGF-2) mRNA via Si5-N14 can promote vascular repair, increase blood oxygen levels, and improve lung function. Si5-N14 shows promise for research in the fields of oncology, pneumonia, and cardiovascular diseases.

EphB1-IN-2 is a mutant-selective kinase inhibitor of ABL and FGFR4, with an IC₅₀ of 14 nM against ABL^G321C mutant and 163 nM against FGFR4^G556C mutant. EphB1-IN-2 shows selectively over wild-type ABL and FGFR4.

Orantinib (Standard) is the analytical standard of Orantinib (HY-10517). This product is intended for research and analytical applications. Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.