BRAFV600E/ABL2-IN-1

BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM) /ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest at the G1 phase, inhibiting progression to the S phase and subsequent phases and G2/M phase. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Bcr-Abl; PERK; P-glycoprotein; Raf

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C(N/N=C(C1=CC=C(Br)C=C1)\C)CN2C(C3=CC=C(S(=O)(C)=O)C=C3)=NC4=CC(Cl)=CC=C24

Molecular Formula

C24H20BrClN4O3S

Molecular Weight

559.86

References & Citations

[1]Badawy MAS, et al. Targeting melanoma resistance: Novel oxindole and non-oxindole-based benzimidazole derivatives as potent dual inhibitors of BRAFV600E and ABL2 kinases. Eur J Med Chem. 2025 Dec 15;300:118096.