Catalog No.S7998 Synonyms: NMS-E628
Molecular Weight(MW): 560.64
Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.
2 Customer Reviews
(A) We transfected the EGFP/Eluc gene into KM12SM cells to establish KM12SM/Eluc cells. KM12SM/Eluc cells were inoculated into the brain of SCID mice. The mice were treated daily with or without entrectinib (15 mg/kg) for 37 days until the bioluminescence increased. Mean ± SE of total flux are shown in the lower panel. Then, the entrectinib-treated brain tumor was harvested at the point indicated by the orange triangle and cultured in vitro. The expanded tumor cells were named KM12SM-ER. (B) The sensitivity of KM12SM-ER and KM12SM cells to entrectinib was determined through cell viability assays, using a CCK-8 kit. The data (mean ± standard deviation [SD] of triplicate cultures) shown are representative of three independent experiments with similar results. (C) Tumor cells were treated with entrectinib (10 nmol/L) for 4 h or c-PARP for 48 h, and harvested lysates were assessed by western blotting. Data shown are representative of three independent experiments with similar results.
Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-17-1623. Entrectinib (RXDX-101) purchased from Selleck.
KM12C and KM12SM cells were treated with crizotinib (1 μmol/L) or entrectinib (1 μmol/L) for 2 h. Immunoblots of cell lysates from these treated cell lines are shown. The data are representative of three independent experiments, showing similar results.
Cancer Med, 2017, 6(12):2972-2983. Entrectinib (RXDX-101) purchased from Selleck.
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Choose Selective Trk receptor Inhibitors
|Description||Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.|
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. |
|In vitro||DMSO||100 mg/mL (178.36 mM)|
|Ethanol||75 mg/mL (133.77 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02587650||Active, not recruiting||Melanoma||Adil Daud|University of California, San Francisco||May 2016||Phase 2|
|NCT02650401||Recruiting||Solid Tumors|CNS Tumors|Neuroblastoma||Ignyta, Inc.||December 2015||Phase 1|
|NCT02568267||Recruiting||Breast Cancer|Cholangiocarcinoma|Colorectal Cancer|Head and Neck Neoplasms|Lymphoma, Large-Cell, Anaplastic|Melanoma|Neuroendocrine Tumors|Non-Small Cell Lung Cancer|Ovarian Cancer|Pancreatic Cancer|Papillary Thyroid Cancer|Primary Brain Tumors|Renal Cell Carcinoma|Sarcomas|Salivary Gland Cancers|Adult Solid Tumor||Ignyta, Inc.||October 2015||Phase 2|
|NCT02097810||Recruiting||Locally Advanced Solid Tumors|Metastatic Solid Tumors||Ignyta, Inc.||June 2014||Phase 1|
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