ly2874455

Description: LY2874455 (LY-2874455; LY 2874455) is a novel and highly potent pan-FGFR inhibitor with potential anticancer activity. It inhibits FGFR1, FGFR2, FGFR3, and FGFR4 with IC50 values of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM, respectively. It also inhibits VEGFR2 activity with an IC50 of 7 nM. LY2874455 exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines. It shows an excellent broad spectrum of antitumor activity in several tumor xenograft models representing the major FGF/FGFR relevant tumor histologies including lung, gastric, and bladder cancers and multiple myeloma, and with a well-defined pharmacokinetic/pharmacodynamic relationship.

References: Mol Cancer Ther. 2011 Nov; 10(11):2200-10.

Chemical Name: (R, E)-2-(4-(2-(5-(1-(3, 5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol.

InChi Key: GKJCVYLDJWTWQU-CXLRFSCWSA-N

InChi Code: InChI=1S/C21H19Cl2N5O2/c1-13(21-17(22)10-24-11-18(21)23)30-15-3-5-20-16(8-15)19(26-27-20)4-2-14-9-25-28(12-14)6-7-29/h2-5, 8-13, 29H, 6-7H2, 1H3, (H, 26, 27)/b4-2+/t13-/m1/s1

SMILES Code: C[CH](C1=C(Cl)C=NC=C1Cl)OC2=CC3=C(NN=C3/C=C/C4=CN(CCO)N=C4)C=C2