1801756-06-8
Chemical Structure
Tunlametinib
Synonym(s): HL-085
- CAS No.: 1801756-06-8
- Formula:C16H12F2IN3O3S
- Molecular Weight:491.25
IUPAC Name: 4-fluoro-5-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)benzo[d]thiazole-6-carboxamide
InChIKey: UFZJUVFSSINETF-UHFFFAOYSA-N
SMILES: O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Tunlametinib | 99.53% | 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). | ||||||||||||||||||||
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- [1]. Liu Y, et al. Preclinical characterization of tunlametinib, a novel, potent, and selective MEK inhibitor. Front Pharmacol. 2023 Sep 21;14:1271268. [Content Brief]
- [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. [Content Brief]
Keywords
