snu-16

LY3405105 (1-Piperidinecarboxylic acid, 4-[[5-methyl-3-(1-methylethyl)pyrazolo[1,5-a]pyrimidin-7-yl]amino]-, 1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-3-pyrrolidinyl ester) is a novel CDK7 inhibitors.

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

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.

LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR, with IC50 values of 71.6 nM and 8.9 nM, respectively. It blocks FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation, and also inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). Furthermore, LC-SF-14 exhibits antitumor activity in SNU-16 xenograft mouse models, making it suitable for research on FGFR2-driven gastric cancer.

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.

5,7,4'-Trimethoxyflavone (4',5,7-Trimethoxyflavone) is isolated from Kaempferia parviflora (KP) which is a medicinal plant from Thailand.

LC-MB12 is an orally active, selective and potent PROTAC FGFR2 complex that degrades FGFR2.LC-MB12 has antiproliferative and antitumor activity.LC-MB12 is used in the study of gastric cancer because of its inhibition of FGFR2 signaling.LC-MB12 has been shown to have antiproliferative and antitumor activity.LC-MB12 has been shown to have antiproliferative and antitumor activity.