Avutometinib, Dual MEK/RAF inhibitor (TBI4112)

Description

Product Details

Formal Name: 3-[[3-Fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one

Alternate Names: RO5126766; CH5126766

Molecular Formula: C₂₁H₁₈FN₅O₅S

Formula Weight: 471.5

CAS Number: 946128-88-7

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years

Applications

Dual MEK/RAF inhibitor

Functions

Dual MEK/RAF inhibitor (IC₅₀s: MEK = 160 nM; CRAF = 56 nM; BRAF = 19 nM; BRAF V600E = 8nM). It directly inhibits unphosphorylated MEK without causing induction of MEK phosphorylation by RAF. The avutemetinib-MEK adduct is a dominant-negative inhibitor of RAF, stabilizing the MEK/RAF complex and locking in an inactive form. Displayed efficacy across multiple RAS-mutated cancer cell lines and an SK-MEL-2 xenograft model. It displayed synergistic effects with eribulin against triple-negative breast cancer cell lines. Avutometinib also displayed efficacy in combination with the FAK inhibitor Defactinib in KRAS-mutated NSCLC cells.

Application Procedures

First dissolved in DMSO (> 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4112_Avutometinib_datasheet

MSDS:

TBI4112_Avutometinib_MSDS

Research use only.