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LY2874455

Chemical Structure : LY2874455

CAS No.: 1254473-64-7

LY2874455 (LY 2874455;LY-2874455)

Catalog No.: PC-43480Not For Human Use, Lab Use Only.

LY2874455 is a potent, selective pan-FGFR inhibitor with IC50 of 2.8/2.6/6.4/6 nM for FGFR1/2/3/4, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LY2874455 is a potent, selective pan-FGFR inhibitor with IC50 of 2.8/2.6/6.4/6 nM for FGFR1/2/3/4, respectively.
LY2874455 inhibits FGFR2 phosphorylation in SNU-16 and KATO-III cells with IC50 of 0.8 and1.5 nM, also inhibits the phosphorylation of FRS2, an immediate downstream target of FGFR, with a similar potency of 0.8 to 1.5 nM.
LY2874455 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.

Physicochemical Properties

M.Wt 444.31
Formula C21H19Cl2N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Pyrazole-1-ethanol, 4-[(1E)-2-[5-[(1R)-1-(3,5-dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-

References

1. Zhao G, et al. Mol Cancer Ther. 2011 Nov;10(11):2200-10.

2. Kim SY, et al. Oncotarget. 2017 Feb 28;8(9):15014-15022.

3. Michael M, et al. Target Oncol. 2017 Aug;12(4):463-474.

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