Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Storage Temp
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
ALK tyrosine kinase receptor inhibitor
Product Description
Information
Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C,ROS1andALKinhibitor withIC50ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) inducesautophagy. Phase 2. In vitro
Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement.
In vivo
In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. Cell Data
cell lines：Tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, DU145, A498, and HCT116
