Temuterkib

• Description:

  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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  ERK1; ERK2

• CAS Number:

  [1951483-29-6]