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LY3009120

Catalog No. T6882 CAS 1454682-72-4

Synonyms: DP-4978

LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.

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LY3009120, CAS 1454682-72-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 30.00
5 mg	In stock	$ 46.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 174.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 555.00
1 mL * 10 mM (in DMSO)	In stock	$ 51.00

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Purity: 99.54%

Purity: 99.08%

Purity: 98%

Purity: 96.96%

Biological Description

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Storage & Solubility Information

Description	LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.
Targets&IC50	C-Raf:4.3 nM, B-Raf (V600E):5.8 nM, B-Raf (WT):15 nM
In vitro	LY3009120 inhibits the cell growth of A375 and HCT116 cells with the IC50 of 9.2 and 220 μM, respectively. LY3009120 inhibits the tyrosine kinase KDR with the IC50 of 3.9 μM.[1]
In vivo	In rats bearing BRAF V600E ST019VR PDX tumors, LY3009120 (15 or 30 mg/kg, p.o.) shows a dose-dependent tumor growth inhibition. In nude rats bearing A375 xenograft, single dose oral treatment with LY3009120 (3 to 50 mg/kg, p.o.) shows a dose dependent inhibition of phospho-ERK, with a dose for 50% inhibition of phospho-ERK (EC50) of 4.36 mg/kg, with plasma concentration to achieve 50% inhibition of phospho-ERK (EC50) of 68.9 ng/mL or 165 nM.[1]
Kinase Assay	Kinase activity measurement using KiNativ assays: Compounds are screened in A375 cell lysates using the ATP-based probe at 5 μM. IC50 values are reported in micromolar units. Cell pellets are resuspended in four volumes of lysis buffer [25 mM Tris pH 7.6, 150 mM NaCl, 1% CHAPS, 1% Tergitol NP-40 type, 1% v/v phosphatase inhibitor cocktail II], sonicated using a tip sonicator, and dounce homogenized. Lysates are cleared by centrifugation at 100,000 g for 30 min. The cleared lysates are filtered through a 0.22 μM syringe filter, and gel filtered into reaction buffer [20 mM Hepes pH 7.8, 150 mM NaCl, 0.1% triton X-100, 1% v/v phosphatase inhibitor cocktail II]. MnCl2 is then added to the lysate to a final concentration of 20 mM prior to inhibitor treatment and probe labeling. Final inhibitor concentrations used for IC50 determinations are 10, 1, 0.1, and 0.01 μM. ATP competition experiments are performed at 1,000, 100, 10, and 1 μM ATP. All inhibitor treatments are performed at room temperature.
Cell Research	Brie?y, cells are grown in DMEM high glucose supplemented with 10% characterized fetal bovine serum and 1% penicillin/streptomycin/L -glutamine at 37℃, 5% CO2, and 95% humidity. Cells are allowed to expand until 70-95% con?uency. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate. 625 cells are added per well in 50 μL of complete growth medium. Plates are incubated for 67 h at 37℃, 5% CO2 , and 95% humidity. Then, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37℃, 5% CO2, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism software to calculate IC 50 values.(Only for Reference)
Animal Research	Animal Models: Female NIH nude rats bearing BRAF V600E ST019VR PDX tumorsFormulation: 20% cyclodextrin, 25 mM phosphate, pH2.0Dosages: 30 mg/kgAdministration: p.o.[1]

Synonyms	DP-4978
Molecular Weight	424.51
Formula	C23H29FN6O
CAS No.	1454682-72-4

Storage

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

Solubility Information

DMSO: 10 mg/mL (23.56 mM)

References and Literature

1. Henry JR, et al. J Med Chem. 2015, 58(10), 4165-4179. 2. Patricelli MP, et al. Chem Biol.2011, 18(6), 699-710.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Covalent Inhibitor Library Bioactive Compound Library Target-Focused Phenotypic Screening Library

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Keywords

LY3009120 1454682-72-4 Autophagy MAPK Raf Raf kinases DP 4978 inhibit LY 3009120 LY-3009120 DP4978 DP-4978 Inhibitor inhibitor

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