LY3009120

Catalog No.S7842

LY3009120 Chemical Structure

Molecular Weight(MW): 424.51

LY03009120 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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Cited by 2 Publications

2 Customer Reviews

  • (a) INA-6, MM.1S, KMS11 or U266 cells were treated for 24 h either with 50 μm of the pan-Raf inhibitor MLN-2480, or 20 μm (INA-6 and MM.1S) or 25 μm (KMS11 or U266) of the pan-Raf inhibitor LY3009120 before western analyses of MEK1/2 and ERK1/2 activation with phosphorylation-specific antibodies.

    Leukemia, 2017, 31(4):922-933. LY3009120 purchased from Selleck.

    Treatment of two PDXs (M048R2.X2 and M063R.X2) that express the BRAFV600E/DK with 30 mg/kg dabrafenib or 15 mg/kg LY3009120 (n=8 tumors/group). Graphs represent tumor volume and dashed lines indicate start of treatment. Unpaired t test was performed at the last time point (*p < 0.05 and ***p < 0.005). Error bars indicate SD. Lower part depicts the immunoblotting for p-ERK and BRAF on M048R2.X2 and M063R.X2, treated with either dabrafenib or LY3009120 (each lane represents a tumor derived from an individual mouse).

    Cell Rep, 2016, 16(1):263-77.. LY3009120 purchased from Selleck.

Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Description LY03009120 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
C-Raf [1]
(Cell-free assay)		 BRAF(V600E) [1]
(Cell-free assay)		 BRAF WT [1]
(Cell-free assay)
4.3 nM 5.8 nM 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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A375 cells Mm\aVJJwdGmoZYLheIlwdiCjc4PhfS=> NU\0UY9SPzJiaB?= NXjlc4RlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDy[ZNignW{aX6gZZN{[XluIFnDOVA:QS5{IH7N NF3MfnUzPTl4NUiwOC=>
human A375 cells NXewelRGTnWwY4Tpc44h[XO|YYm= NXLzT2ZVOTVibXnudy=> M1LE[GNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iRYDoRVIhcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlAzKM7:TR?= MlvHNlU6PjV6MES=
human A375 cells MmTISpVv[3Srb36gZZN{[Xl? M{nDTFE2KG2rboO= MULDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEKUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkCzNUDPxE1? MWqyOVk3PThyNB?=
human A375 cells NF64eJdHfW6ldHnvckBie3OjeR?= MUG3NkBp NIf1NI9KdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFGzO|Uh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDFVmsheGixc4Doc5J6dGG2aX;uJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDFUGlUSSCjc4PhfUwhUUN3ME2wMlA{PyEQvF2= NVLLTGxmOjV7NkW4NFQ>
human A375 cells M2LyT2Z2dmO2aX;uJIF{e2G7 NVL2VWNoOTVibXnudy=> MmDoR49ueGW2aYTpeoUh[mmwZHnu[{Bi\m[rbnn0fUB1dyCcQVugbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkCzPUDPxE1? MYGyOVk3PThyNB?=
human A375 cells MYjGeY5kfGmxbjDhd5NigQ>? MYixOUBucW6| MlXqR49ueGW2aYTpeoUh[mmwZHnu[{Bi\m[rbnn0fUB1dyCyM{igbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkC2NUDPxE1? MXmyOVk3PThyNB?=
human HCT116 cells M{X5PWZ2dmO2aX;uJIF{e2G7 M13scGlvcGmkaYTpc44hd2ZiS2LBV{BIOTOGIH31eIFvfCCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDFVmsheGixc4Doc5J6dGG2aX;uJIJ6KEWOSWPBMEBKSzVyPUCuNVUh|ryP MmLuNlU6PjV6MES=
human HCT116 cells M3rJWnBzd2yrZnXyZZRqd25iYYPzZZk> MWG2O{Bp NHvKc|VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC2O{BpenNiYomgdoV{[Xq3cnnuJIF{e2G7LDDJR|UxRTBwMkKg{txO M3fqe|I2QTZ3OEC0

... Click to View More Cell Line Experimental Data
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]

Protocol

Kinase Assay:[2]
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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:[1]
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  • Cell lines: A375 and HCT116 cells
  • Concentrations: 0.51 μM
  • Incubation Time: 67 h
  • Method: Briefly, 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% confluency. 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:[1]
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  • Animal Models: Female NIH nude rats bearing BRAF V600E ST019VR PDX tumors
  • Formulation: 20% cyclodextrin, 25 mM phosphate, pH2.0
  • Dosages: 30 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL warmed (7.06 mM)
Water Insoluble
Ethanol Insoluble warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC Na
For best results, use promptly after mixing. 		30mg/mL

* 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 Information

Molecular Weight 424.51
Formula

C23H29FN6O
CAS No. 1454682-72-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02014116 Active not recruiting Neoplasms|Neoplasm Metastasis|Melanoma|Carcinoma Non-Small-Cell Lung|Colorectal Neoplasms Eli Lilly and Company November 26 2013 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    I am trying to figure out solubility of the drug LY3009120 Catalog #7842 for in vivo studies. I need some details on the formulation and how it is made to dissolve the chemical?

  • Answer:

    It can dissolve in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 1 mg/ml clearly, and in 0.5% CMC Na at 30 mg/ml as a suspension.

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID