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LY2874455

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Purity:99.46%

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COA HNMR HPLC

LY2874455

Catalog No. T2361Cas No. 1254473-64-7

LY2874455 has been used in trials studying the treatment of Advanced Cancer.

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Pack Size	Price	Availability
1 mg	$58	In Stock
2 mg	$84	In Stock
5 mg	$130	In Stock
10 mg	$207	In Stock
25 mg	$369	In Stock
50 mg	$549	In Stock
100 mg	$788	In Stock
1 mL x 10 mM (in DMSO)	$143	In Stock

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Product Introduction

Bioactivity

Description	LY2874455 has been used in trials studying the treatment of Advanced Cancer.
In vitro	In mice carrying xenografts of RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460, LY2874455 (3 mg/kg, orally administered) demonstrated dose-dependent inhibition of tumor growth. Additionally, LY2874455 effectively inhibited FGF-induced Erk phosphorylation in mouse cardiac tissue, with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively.
In vivo	LY2874455 exhibits FGFR-dependent anti-proliferative effects in KMS-11, OPM-2, SNU-16, and KATO-III cells. In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activity.
Kinase Assay	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.
Cell Research	Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). (Only for Reference)
Alias	LY 2874455, LY-2874455

Chemical Properties

Molecular Weight	444.31
Formula	C21H19Cl2N5O2
Cas No.	1254473-64-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 82 mg/mL (184.6 mM)

Ethanol: 53 mg/mL (119.3 mM)

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.2507 mL	11.2534 mL	22.5068 mL	112.5340 mL
5 mM	0.4501 mL	2.2507 mL	4.5014 mL	22.5068 mL
10 mM	0.2251 mL	1.1253 mL	2.2507 mL	11.2534 mL
20 mM	0.1125 mL	0.5627 mL	1.1253 mL	5.6267 mL
50 mM	0.0450 mL	0.2251 mL	0.4501 mL	2.2507 mL
100 mM	0.0225 mL	0.1125 mL	0.2251 mL	1.1253 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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