Entrectinib (RXDX-101)

Catalog No.S7998 Synonyms: NMS-E628

Entrectinib (RXDX-101) Chemical Structure

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.

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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

Biological Activity

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.
TrkA [1] TrkB [1] TrkC [1] ROS1 [1] ALK [1]
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. [2]

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. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3]


Solubility (25°C)

In vitro DMSO 100 mg/mL (178.36 mM)
Ethanol 75 mg/mL (133.77 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 560.64


CAS No. 1108743-60-7
Storage powder
in solvent
Synonyms NMS-E628

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02650401 Recruiting Solid Tumors|CNS Tumors|Neuroblastoma Hoffmann-La Roche May 3 2016 Phase 1
NCT02097810 Active not recruiting Locally Advanced Solid Tumors|Metastatic Solid Tumors Hoffmann-La Roche July 28 2014 Phase 1
NCT02587650 Recruiting ALK Fusion Protein Expression|BRAF wt Allele|Invasive Skin Melanoma|MET Fusion Gene Positive|NRAS wt Allele|NTRK1 Fusion Positive|NTRK2 Fusion Positive|NTRK3 Fusion Positive|RET Fusion Positive|ROS1 Fusion Positive|Stage III Cutaneous Melanoma AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7 University of California San Francisco|National Cancer Institute (NCI) March 26 2015 Phase 2
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 Hoffmann-La Roche November 19 2015 Phase 2
NCT03330990 Completed Advanced Solid Tumor Hoffmann-La Roche November 14 2017 Phase 1
NCT03066661 Temporarily not available Cancers With NTRK ROS1 or ALK Gene Fusions Ignyta Inc. null --

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID