Entrectinib

Catalog No.S7998 Batch:S799801

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Technical Data

Formula

C31H34F2N6O2
Molecular Weight 560.64 CAS No. 1108743-60-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (178.36 mM)
Ethanol 100 mg/mL (178.36 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Entrectinib 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.
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 (from reference)

Customer Product Validation

Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(10):2357-2369]

Data from [Data independently produced by , , Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-17-1623]

Data from [Data independently produced by , , Cancer Med, 2017, 6(12):2972-2983]

Data from [Data independently produced by , , Cancer Med, 2017, 6(12):2972-2983]

Selleck's Entrectinib has been cited by 59 publications

Clinical efficacy and identification of factors confer resistance to afatinib (tyrosine kinase inhibitor) in EGFR-overexpressing esophageal squamous cell carcinoma [ Signal Transduct Target Ther, 2024, 9(1):153] PubMed: 38937446
Pharmacological inhibition of PDGF-C/neuropilin-1 interaction: A novel strategy to reduce melanoma metastatic potential [ Biomed Pharmacother, 2024, 176:116766] PubMed: 38788599
Acquired NF2 mutation confers resistance to TRK inhibition in an ex vivo LMNA::NTRK1-rearranged soft-tissue sarcoma cell model [ J Pathol, 2024, 263(2):257-269] PubMed: 38613194
Acquired NF2 mutation confers resistance to TRK inhibition in an ex vivo LMNA::NTRK1-rearranged soft-tissue sarcoma cell model [ J Pathol, 2024, 10.1002/path.6282] PubMed: 38613194
LTK mutations responsible for resistance to lorlatinib in non-small cell lung cancer harboring CLIP1-LTK fusion [ Commun Biol, 2024, 7(1):412] PubMed: 38575808
Molecular Characterization and Inhibition of a Novel Stress-Induced Mitochondrial Protecting Role for Misfolded TrkAIII in Human SH-SY5Y Neuroblastoma Cells [ Int J Mol Sci, 2024, 25(10)5475] PubMed: 38791513
Molecular Characterization and Inhibition of a Novel Stress-Induced Mitochondrial Protecting Role for Misfolded TrkAIII in Human SH-SY5Y Neuroblastoma Cells [ Int J Mol Sci, 2024, 25(10)5475] PubMed: 38791513
Inhibition of human UDP-glucuronosyltransferase enzyme by entrectinib: Implications for drug-drug interactions [ Chem Biol Interact, 2024, 395:111023] PubMed: 38677539
Novel insight into mechanisms of ROS1 catalytic activation via loss of the extracellular domain [ Sci Rep, 2024, 14(1):22191] PubMed: 39333184
Induction of resistance to neurotrophic tropomyosin-receptor kinase inhibitors by HMGCS2 via a mevalonate pathway [ Cancer Med, 2024, 13(12):e7393] PubMed: 38923428

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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