Dubermatinib, AXL inhibitor

Product Details

Formal Name: 2-[[5-Chloro-2-[4-[(4-methylpiperazine-1-yl)methyl]pyrimidine-4-yl]amino]-N,N-dimethylbenzenesulfonamide

Alternate Names: TP-0903

Molecular Formula: C₂₄H₃₀ClN₇O₂S

Formula Weight: 516.10

CAS Number: 1341200-45-0

Purity: >98%

Formulation: powder

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

Storage: -20°C

Stability: ≥ 2 years.

Applications

AXL inhibitor

Functions

Potent (IC50 = 27 nM) inhibitor of the TAM family kinase AXL. 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. It inhibited neuroblastoma cell growth and enhanced sensitivity to conventional chemotherapy. Dubermatinib was also active in a drug-resistant acute myeloid leukemia model and reduced metastasis and therapy resistance in pancreatic cancer models.

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° for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)