LY3009120

For research use only.

Catalog No.S7842

26 publications

LY3009120 Chemical Structure

CAS No. 1454682-72-4

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. LY03009120 induces autophagy. Phase 1.

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Selleck's LY3009120 has been cited by 26 publications

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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. LY03009120 induces autophagy. 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 MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NV3EN3ZFPzJiaB?= NEC4UpJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IILld4F7fXKrbjDhd5NigSxiSVO1NF06NjJibl2= M{O5OlI2QTZ3OEC0
human A375 cells M2W3ZWZ2dmO2aX;uJIF{e2G7 MYGxOUBucW6| M{T2UWNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iRYDoRVIhcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlAzKM7:TR?= NIfoOoszPTl4NUiwOC=>
human A375 cells MmPrSpVv[3Srb36gZZN{[Xl? M{XRPVE2KG2rboO= M4jSXGNwdXCndHn0bZZmKGKrbnTpcoch[W[oaX7peJkhfG9iQmLBSkBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNFMyKM7:TR?= MYCyOVk3PThyNB?=
human A375 cells NH;LV5dHfW6ldHnvckBie3OjeR?= NEHxWVk4OiCq NHvOdI5KdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFGzO|Uh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDFVmsheGixc4Doc5J6dGG2aX;uJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDFUGlUSSCjc4PhfUwhUUN3ME2wMlA{PyEQvF2= M17zclI2QTZ3OEC0
human A375 cells MULGeY5kfGmxbjDhd5NigQ>? MXWxOUBucW6| NF\xc5lEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIGrBT{BqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNFM6KM7:TR?= MXeyOVk3PThyNB?=
human A375 cells MlHMSpVv[3Srb36gZZN{[Xl? M3fjTlE2KG2rboO= MX3Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKHB|ODDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwME[xJO69VQ>? MkS3NlU6PjV6MES=
human HCT116 cells MVnGeY5kfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKEuUQWOgS|E{TCCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRWLLJJBpd3OyaH;yfYxifGmxbjDifUBGVEmVQTygTWM2OD1yLkG1JO69VQ>? NHexVoUzPTl4NUiwOC=>
human HCT116 cells M{HGcHBzd2yrZnXyZZRqd25iYYPzZZk> NXHTT4tyPjdiaB?= M3;TWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IE[3JIhzeyCkeTDy[ZNignW{aX6gZZN{[XluIFnDOVA:OC5{MjFOwG0> NHjIeFkzPTl4NUiwOC=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-EGFR / EGFR / p-BRAF / BRAF / p-CRAF / CRAF / p-MEK / MEK / p-AKT / AKT; 

PubMed: 27999210     


CRC cell lines were treated with DMSO or 1 μM LY3009120 for 24 and 48 hrs. Whole cell lysates were analyzed by Western blot using antibodies against the proteins indicated.

Beclin-1 / Mcl-1 / LC3 / p62 ; 

PubMed: 28382170     


LY3009120 treatment of K1 cells increased the conversion of LCⅠ to LC3Ⅱ without influencing the expression of Beclin-1.

27999210 28382170
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
  • 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
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
Smiles CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02014116 Terminated Drug: LY3009120 capsule Neoplasms|Neoplasm Metastasis|Melanoma|Carcinoma Non-Small-Cell Lung|Colorectal Neoplasms Eli Lilly and Company November 26 2013 Phase 1

Tech Support

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