[CAS NO. 946128-88-7] RO5126766 (CH5126766)

Name: RO5126766 (CH5126766)
Brand: Arctom Scientific
SKU: SLK-S7170

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PRODUCTS SPECIFICATIONS [946128-88-7]

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Catalog

SLK-S7170

Brand

Selleck

CAS

946128-88-7

DESCRIPTION [946128-88-7]

Overview

MDL	MFCD27987901
Molecular Weight	471.46
Molecular Formula	C21H18FN5O5S
SMILES	O=S(NC)(NC1=NC=CC(CC2=C(C)C3=CC=C(OC4=NC=CC=N4)C=C3OC2=O)=C1F)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1211 mL	10.6054 mL	21.2107 mL
5 mM	0.4242 mL	2.1211 mL	4.2421 mL
10 mM	0.2121 mL	1.0605 mL	2.1211 mL
50 mM	0.0424 mL	0.2121 mL	0.4242 mL

Description

RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304) is a dual inhibitor with 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. 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.

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. In the HCT116 (K-ras) and COLO205 (B-raf) mutant xenografts, CH5126766 (0.3 mg/kg) causes significant decreases in [18 F]FDG uptake. In the SK-MEL-2 xenograft model, RO5126766 also suppresses the tumor growth.

References

[1] Ishii N, et al. Cancer Res. 2013, 73(13), 4050-4060.
[2] Miller CR, et al. Gynecol Oncol. 2014, 133(1), 128-137.
[3] Wada M, et al. PLoS One. 2014, 9(11), e113217.