Belizatinib, also known as TSR-011, is an orally available inhibitor of both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases (TRK) TRKA, TRKB, and TRKC, with potential antineoplastic activity. Upon administration, ALK/TRK inhibitor TSR-011 binds to and inhibits both ALK and TRK kinases. The inhibition leads to disruption of ALK- and TRK-mediated signaling and impedes tumor cell growth in ALK/TRK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors.
MedKoo Cat#: 206430
Name: Belizatinib
CAS#: 1357920-84-3
Chemical Formula: C33H44FN5O3
Exact Mass: 577.3428
Molecular Weight: 577.75
Elemental Analysis: C, 68.61; H, 7.68; F, 3.29; N, 12.12; O, 8.31
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMF | 30.0 | 51.93 | |
DMSO | 143.3 | 248.08 | |
Ethanol | 65.0 | 112.50 |
The following data is based on the product molecular weight 577.75 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |