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Entrectinib

Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice[1][2][3].

Product Specifications

CAS Number

[1108743-60-7]

Product Name Alternative

NMS-E628; RXDX-101

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Anaplastic lymphoma kinase (ALK) ; Autophagy; ROS Kinase; Trk Receptor

Type

Reference compound

Related Pathways

Autophagy; Neuronal Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Entrectinib.html

Purity

99.87

Solubility

DMSO : ≥ 31 mg/mL

Smiles

O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=C(NC5CCOCC5)C=C(N6CCN(C)CC6)C=C4

Molecular Formula

C31H34F2N6O2

Molecular Weight

560.64

Precautions

H302, H315, H319, H335

References & Citations

[1]Ardini E, et al. Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications. Mol Cancer Ther. 2016 Apr;15 (4) :628-39.|[2]Iyer R, et al. Entrectinib is a potent inhibitor of Trk-driven neuroblastomas in a xenograft mouse model. Cancer Lett. 2016 Mar 28;372 (2) :179-86.|[3]Miao Y, et al. Entrectinib ameliorates bleomycin-induced pulmonary fibrosis in mice by inhibiting TGF-β1 signaling pathway. Int Immunopharmacol. 2022 Dec;113 (Pt B) :109427.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Available Sizes

Curated Selection

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