MedChemExpress LLC (MCE)

MedChemExpress - Model Entrectinib - 1108743-60-7

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].

Entrectinib

MCE China：Entrectinib

Brand：MedChemExpress (MCE)

Cat. No.HY-12678

CAS：1108743-60-7

Synonyms：NMS-E628; RXDX-101

Purity：99.79%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

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.

In Vitro：Entrectinib (100, 200, 400 nM; 24 h) alleviates TGF-β1-induced activation of mouse lung fibroblasts[1]. Entrectinib(100, 200, 400 nM; 24 h) inhibits TGF-β1-induced epithelial to mesenchymal transition of mouse lung epithelial cells[1]. Entrectinib (10, 50, 250 nM; 2 h) abolishes autophosphorylation of TPM3-TRKA, concomitant with complete inhibition of the phosphorylation of PLCg1, AKT, and MAPK in KM12 cells[2]. Entrectinib (10, 50, 250 nM; 24, 48 h) induce KM12 cells cycle arrest (24 h) and apoptosis (48 h)[2].

In Vivo：Entrectinib (20, 40, 60 mg/kg; i.g.; single daily for 7 days) attenuates bleomycin-induced pulmonary fibrosis in mice[1]. Entrectinib (30, 60 mg/kg; p.o.; twice daily for 10 consecutive days) induces regression of xenograft tumors in tumor-bearing mice, including TRKA-dependent colorectal cancer KM12, ROS1-driven tumors, and several ALK-dependent models of different tissue origins, including brain-localized lung model cancer metastasis[2].

IC50 & Target：IC50: 1 nM (TrkA), 3 nM (TrkB), 5 nM (TrkC), 12 nM (ROS1), 7 nM (ALK)[2]. Cellular Effect Cell Line Type Value Description References

References：

[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. [Content Brief]

[2]. 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]

[3]. 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]

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