RO5126766 (CH5126766)

Catalog No.S7170

RO5126766 (CH5126766) Chemical Structure

Molecular Weight(MW): 471.46

RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.

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Biological Activity

Description RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.
Targets
BRAF V600E [1]
(cell-free assay)
BRAF [1]
(cell-free assay)
CRAF [1]
(cell-free assay)
MEK1 [1]
(cell-free assay)
8.2 nM 19 nM 56 nM 160 nM
In vitro

In HCT116 KRAS-mutant colorectal cancer cells, CH5126766 significantly reduces the levels of phospho-MEK and phospho-ERK. CH5126766 inhibits RAF kinase by binding to MEK1, and causes MEK to become a dominant negative inhibitor of RAF. [1] In Raf or RAS-mutant cell lines SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, HCT116, and PC3 cells, CH5126766 inhibits cell growth with IC50 of 65, 28, 40, 46, and 277 nM, respectively. In two melanoma cell lines with the BRAF V600E or NRAS mutation, RO5126766 induces G1 cell cycle arrest accompanied by up-regulation of the CDK inhibitor p27 and down-regulation of cyclinD1. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cell NXH0[ldkTnWwY4Tpc44h[XO|YYm= M4K4Slk3KGh? M3fmfmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGxiZ4Lve5RpKGGodHXyJFk3KGi{czDifUBkd3WwdHnu[{BscXRvODDhcoFtgXOrczygTWM2OD1yLkC0JO69VQ>? NIexSXgzPDlyMEizNi=>
human C32 cells NY[ybFl6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWnEZmxpT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSzN{IHPlcIx{KGijcnLvdolv\yCULWLh[kBXPjByRTDteZRidnRuIFnDOVA:OC5yNEeg{txO Mmm3NlQ6ODB6M{K=
human PANC1 cells M{Hpd2Z2dmO2aX;uJIF{e2G7 MlvZNVAh|ryP MmrMNUBp M3S1dWlvcGmkaYTpc44hd2ZiTVXLNUBqdiCqdX3hckBRSU6FMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heEW{a{GvNkBt\X[nbDDheEAyOCC3TTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> MnnKNlU4PjZ4M{O=
human A549 cells MmHkSpVv[3Srb36gZZN{[Xl? NYHpbnpoOTBizszN NInJVmwyKGh? MWjJcohq[mm2aX;uJI9nKE2HS{GgbY4hcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gdGVzczFxMjDs[ZZmdCCjdDCxNEB2VSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYO= MmTTNlU4PjZ4M{O=

... Click to View More Cell Line Experimental Data

In vivo In an HCT116 (G13D KRAS) mouse xenograft model, CH5126766 (25 mg/kg, p.o.) inhibits ERK signaling output more effectively than a standard MEK inhibitor that induces MEK phosphorylation and has potent antitumor activity. [1] In the HCT116 (K-ras) and COLO205 (B-raf) mutant xenografts, CH5126766 (0.3 mg/kg) causes significant decreases in [18 F]FDG uptake. [2] In the SK-MEL-2 xenograft model, RO5126766 also suppresses the tumor growth. [3]

Protocol

Kinase Assay:[1]
+ Expand

MEK and RAF kinase enzyme assays:

The inhibitory activities against CRAF, BRAF, or BRAF V600E enzymes are measured by quantification of phosphorylation of inactive K97R MEK1 [MEK1] by recombinant RAF proteins [BRAF: B-RAF wt, BRAF V600E: B-RAF V600E or CRAF: Raf-1] with Europium-anti-MEK1/2 (pSer218/222) antibody and SureLight allophycocyanine-anti-6his antibody by measuring time-resolved fluorescence (TRF). Alternatively, the inhibitory activities against the RAF enzymes are measured by quantification of phosphorylation of a fluorescein-labeled peptide corresponding to human MEK1 212-224 and human MEK2 217-229 (5-Fl-SGQLIDSMANSFV-NH2, MEKtide) by using the IMAP fluorescence polarization (FP) Screening Express Kit. Inhibition of MEK1 is evaluated by a coupled assay with active MEK1 (MEK1 S218E/S222E) and unactive dephosphorylated ERK2 (MAP kinase 2/Erk 2). The phosphorylation of a fluorescent-labeled peptide substrate (FAM-Erktide, IPTTPITTTYFFFK-5FAM-COOH) by ERK2 is quantified by using the IMAP FP Screening Express Kit.
Cell Research:[3]
+ Expand
  • Cell lines: SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, A549, HCT15, HCT116, and PC3 cells
  • Concentrations: ~10 μM
  • Incubation Time: 72 h
  • Method: The number of viable cells is determined using the Cell Counting Kit-8 assay according to the manufacturer's instructions. After the incubation of cells for 72 h with the indicated concentrations of various agents, kit reagent WST-8 is added to the medium and incubated for a further 4 h. The absorbance of samples (450 nm) is determined using a scanning multiwell spectrophotometer that serves as an ELISA reader. Cell numbers and viability are also measured using the ViaCount Assay according to the manufacturer's instructions.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female BALB-nu/nu mice bearing HCT116, Calu-6 or COLO205 tumors
  • Formulation: 5% DMSO and 10% 2-hydroxypropyl-β-cyclodextrin (HPCD) solution in distilled water
  • Dosages: ~25 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (199.38 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
20mg/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 471.46
Formula

C21H18FN5O5S

CAS No. 946128-88-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03681483 Not yet recruiting Advanced Non-small Cell Lung Cancer Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|Chugai Pharma USA October 2018 Phase 1
NCT02407509 Unknown status Solid Tumours|Multiple Myeloma Royal Marsden NHS Foundation Trust|Institute of Cancer Research United Kingdom|Chugai Pharmaceutical May 2013 Phase 1
NCT00773526 Completed Neoplasms Hoffmann-La Roche November 2008 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.

Handling Instructions

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID