Alectinib, ALK inhibitor, potent (TBI4793)

Description

Product Details

Formal Name: 9-Ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile

Alternate Names: CH5424802; RO5424802

Molecular Formula: C₃₀H₃₄N₄O₂

Formula Weight: 482.60

CAS Number: 1256580-46-7

Purity: >99%

Formulation: powder

Solubility: Soluble in DMSO (up to 5 mg/ml) with warming

Storage: -20°C

Stability: ≥ 1 year.

Applications

ALK inhibitor, potent

Functions

Potent inhibitor of wild-type and fusion ALK (IC50 = 1.9 nM) and RET (IC50 = 4.8 nM), but not ROS1 tyrosine kinase activity. Significantly reduces proliferation and induces apoptosis in NSCLC, however these tumors can become resistant by activating Yes-associated protein 1 (YAP1). Causes cell death in glioblastoma cells via inhibition of STAT3, and prolongs the survival of mice harboring intracerebral GBM xenografts. Has been used to enable allogeneic stem cell transplantation in a patient with ALK-positive anaplastic large-cell lymphoma. Clinically useful anticancer agent.

Application Procedures

First dissolved in DMSO (up to 5 mg/ml) with warming, then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 2 months.