Entrectinib-d₈  (Synonyms: NMS-E628-d₈; RXDX-101-d₈)

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice^[1][2][3][4].

568.69

C₃₁H₂₆D₈F₂N₆O₂

2251773-94-9

O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=C(NC5CCOCC5)C=C(N6C([2H])([2H])C([2H])([2H])N(C)C([2H])([2H])C6([2H])[2H])C=C4

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• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. 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.  [Content Brief]

  [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.  [Content Brief]

  [4]. 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.  [Content Brief]