WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205527
CAS#: 1254473-64-7
Description: LY2874455 is a novel and potent FGF/FGFR Inhibitor. It exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines and 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.
MedKoo Cat#: 205527
Name: LY2874455
CAS#: 1254473-64-7
Chemical Formula: C21H19Cl2N5O2
Exact Mass: 443.09158
Molecular Weight: 444.31
Elemental Analysis: C, 56.77; H, 4.31; Cl, 15.96; N, 15.76; O, 7.20
Synonym: LY2874455; LY 2874455; LY-2874455.
IUPAC/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[C@H](C1=C(Cl)C=NC=C1Cl)OC2=CC3=C(NN=C3/C=C/C4=CN(CCO)N=C4)C=C2
LY2874455 is active against all 4 FGFRs, with a similar potency in biochemical assays. It exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines and 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. LY2874455 also exhibits a 6- to 9-fold in vitro and in vivo selectivity on inhibition of FGF- over VEGF-mediated target signaling in mice. Furthermore, LY2874455 did not show VEGF receptor 2-mediated toxicities such as hypertension at efficacious doses. Currently, this molecule is being evaluated for its potential use in the clinic.[source: Mol Cancer Ther; 10(11); 2200-10.]
1. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K, Peng SB, McCann DJ. A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. Mol Cancer Ther. 2011 Nov;10(11):2200-10. Epub 2011 Sep 7. PubMed PMID: 21900693.
