1037624-75-1

Product Details:

CasNo： 1037624-75-1

Molecular Formula： C30H34N8

Purity： 99%

Synonyms: (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine; BGB-324; BGB-324,CPDB1725; (S)-1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8; R428; R428(BGB324); 1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine; EOS-62006
Melting point: >211°C (dec.)
Boiling point: 799.6±70.0°C
Density: 1.41±0.1 g/cm3
Solubility: Soluble in DMSO (up to at least 25 mg/ml)
Form: Yellow powder
Pka: 10.34±0.20
Color: Yellow

Description:
Bemcentinib (R428, BGB324), a selective small-molecule inhibitor of AXL, is currently being evaluated in phase II trials for the treatment of non-small-cell lung cancer (NSCLC) and acute myelocytic leukemia (AML). It has been found to induce apoptosis in cancer cells and to block tumor spread in models of metastatic breast cancer. The therapeutic potential of Bemcentinib has also been demonstrated in highly invasive esophageal adenocarcinoma cells and in ESCC cells.
Bemcentinib is a selective, small molecule inhibitor of Axl that blocks its catalytic and precancerous activities. Bemcentinib treatment reduced Axl-induced AKT phosphorylation, cancer cell invasion, angiogenesis, and the production of pro-inflammatory cytokines. It also reduced the expression of the cytokine granulocyte macrophage colony-stimulating factor and Snail in a dosage-dependent manner. Interestingly,using Bemcentinib to inhibit Axl-mediated cellular and molecular functions during cisplatin treatments achieved an enhanced suppression of liver metastases. Axl knockdowns in RAC cell lines reduced migration, invasion, and in vivo engraftment, accompanied by a downregulation in the activity of the Ral GTPase proteins (RalA and RalB). Similar effects were obtained using an A428 inhibitor. Blocking Axl functions also abrogated the phosphorylation of ERBB2 (Her-2/neu) at the Tyr877 residue, which reveals the cross-functional effects of Bemcentinib on different receptor signaling axes.
Cabozantinib (XL184) and Bemcentinib (R428, BGB324) Inhibit the Growth of Esophageal Squamous Cell Carcinoma (ESCC)

Uses:
Bemcentinib (R428, BGB324) is an AXL tyrosine kinase inhibitor shown to be used as an anti-cancer agent.