Temuterkib

Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.

Product Specifications

CAS Number

[1951483-29-6]

Product Name Alternative

LY3214996

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

ERK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LY3214996.html

Purity

99.94

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C(C=C(C1=NC(NC2=CC=NN2C)=NC=C1)S3)=C3C4(C)C)N4CCN5CCOCC5

Molecular Formula

C22H27N7O2S

Molecular Weight

453.56

Precautions

H302, H315, H319, H335

References & Citations

[1]Shripad V. Bhagwat, et al. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Research. July 2017.