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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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.
Targets
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]

Protocol

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
Formula

C31H34F2N6O2

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

Bio Calculators

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Related Antibodies

Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID