A MEK1 inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Tunlametinib

Item No. 45050

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-fluoro-5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-6-benzothiazolecarboxamide
CAS Number
1801756-06-8
Synonyms
  • HL 085
Molecular Formula
C16H12F2IN3O3S
Formula Weight
491.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO
InChi Code
InChI=1S/C16H12F2IN3O3S/c17-10-5-8(19)1-2-11(10)21-14-9(16(24)22-25-4-3-23)6-12-15(13(14)18)20-7-26-12/h1-2,5-7,21,23H,3-4H2,(H,22,24)
InChi Key
UFZJUVFSSINETF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $39

    Add

    5 mg

    $117

    Add

    10 mg

    $215

    Add

    25 mg

    $390

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    Tunlametinib is a MEK1 inhibitor (IC50 = 1.9 nM).1 It is selective for MEK1 over a panel of other kinases at 10 µM. Tunlametinib selectively reduces proliferation in a panel of cancer cell lines expressing mutant K-Ras or B-RAF (IC50s = 0.67-59.89 nM) over H1975 cells expressing wild-type K-Ras and B-RAF (IC50 = >1,000 nM). It also inhibits the phosphorylation of ERK in A375 melanoma cells (IC50 = 1.16 nM). In vivo, tunlametinib (1, 3, and 9 mg/kg) inhibits intratumoral ERK phosphorylation in an A375 mouse xenograft model and reduces tumor growth in the same model when administered at doses of 3 and 9 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, Y., Cheng, Y., Huang, G., et al. Preclinical characterization of tunlametinib, a novel, potent, and selective MEK inhibitor. Front. Pharmacol. 14, 1271268 (2023).