Dubermatinib
AXL inhibitor / Potent (IC50 = 27 nM) inhibitor of the TAM family kinase AXL.1 It displayed potent activity against the pancreatic tumor cell line PSN-1 (IC50 = 6 nM). Dubermatinib also strongly inhibited the kinases Aurora A/B, JAK2, ABL1, and CHEK1. It induced apoptosis in chronic lymphocytic leukemia (CLL) cells and acted synergistically with BTK inhibitors against CLL cells.2 It inhibited neuroblastoma cell growth and enhanced sensitivity to conventional chemotherapy.3 Dubermatinib was also active in a drug-resistant acute myeloid leukemia model4 and reduced metastasis and therapy resistance in pancreatic cancer models5.
Biochemicals & reagents
1341200-45-0
TP-0903
1 Mollard et al. (2011), Design, Synthesis, and Biological Evaluation of a Series of Novel AXL Kinase Inhibitors; ACS Med. Chem. Lett. 2 907 2 Sinha et al. (2015); Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors; Clin. Cancer Res. 21 115 3 Aveic et al. (2018); TP-0903 inhibits neuroblastoma cell growth and enhances the sensitivity to conventional chemotherapy; Eur. J. Pharmacol. 818 435 4 Jeon et al. (2020); TP-0903 is active in models of drug-resistant acute myeloid leukemia; JCI Insight 5 e140169 5 Zhang et al. (2022); Axl Inhibitor TP-0903 Reduces Metastasis and Therapy Resistance in Pancreatic Cancer; Mol. Cancer Ther. 21 38
-20°C
TARGET: Kinase -- DISEASE AREA: Cancer