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Tunlametinib

Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1) . Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells) . Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011) . Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) [1][2].

Product Specifications

CAS Number

[1801756-06-8]

Product Name Alternative

HL-085

UNSPSC

12352005

Target

MEK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Concentration

10mM

Purity

99.53

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO

Molecular Formula

C16H12F2IN3O3S

Molecular Weight

491.25

References & Citations

[1]Liu Y, et al. Preclinical characterization of tunlametinib, a novel, potent, and selective MEK inhibitor. Front Pharmacol. 2023 Sep 21;14:1271268.|[2]Sari MHM, et al. Editorial: Advances in molecular and pharmacological mechanisms of novel targeted therapies for melanoma. Front Oncol. 2024 Apr 4;14:1403778.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

MEK1; MEK2

Available Sizes

Curated Selection

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