R428, Potent and selective AXL inhibitor

Product Details

Formal Name: 1-(3,4-Diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine

Alternate Names: Bemcentinib; BGB324

Molecular Formula: C₃₀H₃₄N₈

Formula Weight: 506.64

CAS Number: 1037624-75-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Potent and selective AXL inhibitor

Functions

R428 (1037624-75-1) is a potent and selective inhibitor of AXL kinase (IC50 = 1.4nM). R428 has been shown to overcome chemotherapy resistance to various agents in multiple cancer models. AXL has been shown to suppress myeloid cell activation and function – combined AXL inhibition with R428 and PD-1 blockade showed potent synergistic antitumor effects.

Application Procedures

First dissolved in DMSO (up to at least 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.

Documents

• Datasheet (PDF)
• MSDS (PDF)