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Entrectinib-d4

Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib. Entrectinib 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

Product Name Alternative

NMS-E628-d4; RXDX-101-d4

UNSPSC

12352005

Target

Anaplastic lymphoma kinase (ALK) ; Autophagy; Isotope-Labeled Compounds; ROS Kinase; Trk Receptor

Type

Isotope-Labeled Compounds

Related Pathways

Autophagy; Neuronal Signaling; Others; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=C(NC5C([2H])([2H])COCC5([2H])[2H])C=C(N6CCN(C)CC6)C=C4

Molecular Formula

C31H30D4F2N6O2

Molecular Weight

564.66

References & Citations

[1]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.|[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]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.

Shipping Conditions

Room temperature

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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