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Home > Products > Protein Tyrosine Kinase > FGFR Inhibitor > LY2874455 1254473-64-7

LY2874455 1254473-64-7

Product Description

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Molecular Weight:

444.31 LY2874455 is a Pan-FGFR Inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.


Biological Activity


In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455
inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows
FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and
KATO-III cells.


LY2874455 exhibits a potent inhibition of FGF-induced Erk
phosphorylation in the heart tissues of mice with TED50 and TED90 values
of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2
(DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results
in dose-dependent inhibition of the tumor growth.


Biochemical filter-binding assays for detection of FGFR phosphorylation activities


Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2,
150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL
poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5,
7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are
incubated at room temperature for 30 minutes followed by termination
with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)







Chemical Information




Molecular Weight (MW) 444.31
Formula

C21H19Cl2N5O2

CAS No. 1254473-64-7

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms N/A



Solubility (25°C) * In vitro DMSO 88 mg/mL (198.05 mM)
Water <1 mg/mL (
Ethanol 88 mg/mL heating (198.05 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.




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







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Product Categories : Protein Tyrosine Kinase > FGFR Inhibitor