Entrectinib

Datasheet MSDS
Catalog Number
SALK10025
Product Name
Entrectinib
CAS Number
1108743-60-7
Synonyms
RXDX-101, NMS-E628
Molecular Formula
C31H34F2N6O2
Molecular Weight
560.64
Purity
99.61%
Solubility
DMSO: 100 mg/mL (178.36 mM) Ethanol: 67 mg/mL (119.5 mM) Water: <1 mg/mL ( < 1 mg/ml refers to the product slightly soluble or insoluble )
Storage
Powder: -20°C for 3 years In solvent: -80°C for 6 months
Description
Entrectinib is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
Target
ALK, ROS1, TrkA, TrkB, TrkC
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