R428 (BGB324), AXL Inhibitor

Cat. No.
CLIA-0130098
Product Size
5 mg 25 mg Custom Size

Product Overview

Description
Potent and selective AXL kinase inhibitor.
Purity
> 98%
Form
Solid
Target
AXL
Biological Description
Potent and selective inhibitor of AXL kinase (IC50 = 14 nM). Overcomes chemotherapy resistance to various agents in multiple cancer models. Suppresses myeloid cell activation and function.  AXL inhibition combined with PD-1 blockade shows potent synergistic anti-tumor effects. Greater than 100-fold selective for AXL versus ABL. Selective (50-100-fold) versus Mer and Tyro3 in cell-based assays. Highly selective for AXL versus InsR, EGFR, HER2, and PDGFRbeta in cell-free assays.
Source
Synthetic
CAS Number
1037624-75-1
Solubility Overview
Soluble in DMSO to 25 mM.

Chemical Properties

Chemical 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
Molecular Weight (Da)
506.64
Molecular Formula
C30H34N8
PubChem Identifier
SMILES
c1ccc-2c(c1)CCCc3c2nnc(c3)n4c(nc(n4)Nc5ccc6c(c5)CC[C@H](CC6)N7CCCC7)N

Storage & Handling

Storage Instructions
Shipped at room temperature. Store at -20 °C. Store under desiccating conditions.

For Research Use Only. Not For Clinical Use.

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