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Entrectinib

CAT: 0804-HY-12678-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12678-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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

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