fgfr1 inhibitor-16

FGFR1inhibitor-16 (Compound 89) functions as an FGFR1 inhibitor, demonstrating an inhibition rate of 53.00% at a concentration of 50 μM and 24.95% at 10 μM. It is utilized in tumor research.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(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).

TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(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).

TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src,

FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, exhibiting IC50 values of 8 nM, 4 nM, and 3.8 nM respectively. It plays a crucial role in cancer research.

FGFR2/3-IN-2 (compound 10) is an orally active inhibitor targeting FGFR2 and FGFR3. It exhibits IC50 values of 3.7 nM for FGFR2 and 31.2 nM for FGFR3, with a pre-incubation time of 1 hour. FGFR2/3-IN-2 demonstrates selectivity over FGFR1/4 and other kinases, and does not cause diarrhea or increased serum phosphate in vivo. In the SNU-16 gastric cancer model, FGFR2/3-IN-2 can induce tumor stasis or regression.

FGFR1 inhibitor-18 (compound 16) is a potent inhibitor of FGFR1 with an IC50 of 1.31 nM. It effectively occupies the ATP binding site of the target FGFR1.

FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. It effectively inhibits FGFR1, FGFR2, FGFR3, and the FGFR2V564F gatekeeper mutant, with IC50 values of 46, 41, 99, and 62 nM, respectively. Additionally, FGFR-IN-14 demonstrates strong antiproliferative effects on NCI-H520 lung cancer cells and SNU-16 and KATO III gastric cancer cells, with IC50 values of 19, 59, and 73 nM, respectively.

FGFR-IN-11 (compound I-5) is an orally active, covalent inhibitor of FGFR, with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4). This compound demonstrates nanomolar potency in inhibiting the proliferation of various cancer cells and significantly hinders tumor growth in xenograft mouse models [1].