[CAS NO. 1951483-29-6]  Temuterkib (LY3214996)

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PRODUCTS SPECIFICATIONS [1951483-29-6]

Catalog
SLK-S8534
Brand
Selleck
CAS
1951483-29-6

DESCRIPTION [1951483-29-6]

Overview

MDL-
Molecular Weight453.56
Molecular FormulaC22H27N7O2S
SMILESO=C1C(C=C(C2=NC(NC3=CC=NN3C)=NC=C2)S4)=C4C(C)(C)N1CCN5CCOCC5

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

1 mg5 mg10 mg
1 mM2.2048 mL11.0239 mL22.0478 mL
5 mM0.4410 mL2.2048 mL4.4096 mL
10 mM0.2205 mL1.1024 mL2.2048 mL
50 mM0.0441 mL0.2205 mL0.4410 mL

Description

Temuterkib (LY3214996) is a selective and novel inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

Targets

ERK1 [1]
(Cell-free assay)
ERK2 [1]
(Cell-free assay)
5 nM5 nM

In vitro

In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY3214996.LY3214996 possesses an optimal balance of potency (hERK1 IC50 5 nM, hERK2 IC50 5nM, pRSK IC50 0.43 µM) and solubility.