An inhibitor of TrkA (IC50 = 1.7 nM)

Entrectinib – 10 mg

Brand:
Cayman
CAS:
1108743-60-7
Storage:
-20
UN-No:
Non-Hazardous - /

Entrectinib is an inhibitor of TrkA (IC50 = 1.7 nM), TrkB (IC50 = 0.1 nM), and TrkC (IC50 = 0.1 nM), as well as C-ros oncogene 1 (ROS1; IC50 = 0.2 nM) and anaplastic lymphoma kinase (ALK; IC50 = 1.6 nM).{31678,31677} Entrectinib blocks proliferation of ALK-dependent cell lines, including those with L1196M or C1156Y resistance mutations, and inhibits ALK‐dependent signaling.{31677,31679} It has been shown to inhibit the growth of a non-small cell lung cancer cell line bearing an EML4-ALK rearrangement.{31677,31679} In mice bearing various Trk, ROS1, or ALK-driven xenografts, entrectinib has been shown to induce tumor regression.{31677,31679}  

 

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Description

An inhibitor of TrkA (IC50 = 1.7 nM), TrkB (IC50 = 0.1 nM), and TrkC (IC50 = 0.1 nM), as well as ROS1 (IC50 = 0.2 nM) and ALK (IC50 = 1.6 nM); blocks proliferation of ALK-dependent cell lines, including those with L1196M or C1156Y resistance mutations; induces tumor regression in mice bearing various Trk, ROS1, or ALK-driven xenografts

Formal name: N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-benzamide

Synonyms:  NMS-E628|RXDX-101

Molecular weight: 560.6

CAS: 1108743-60-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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