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Entrectinib

Catalog No. T3678   CAS 1108743-60-7
Synonyms: RXDX-101, NMS-E628

Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.

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Entrectinib Chemical Structure
Entrectinib, CAS 1108743-60-7
Pack Size Availability Price/USD Quantity
2 mg In stock $ 35.00
5 mg In stock $ 54.00
10 mg In stock $ 81.00
25 mg In stock $ 113.00
50 mg In stock $ 171.00
100 mg In stock $ 297.00
500 mg In stock $ 728.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.61%
Purity: 99.49%
Purity: 98.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
Targets&IC50 TrkA:1.7 nM, TrkB:0.1 nM, TrkC:0.1 nM, ALK:1.6 nM
In vitro Entrectinib effectively inhibits ALK‐dependent signaling and specificity blocks proliferation of ALK-dependent cell lines. Entrectinib also significantly inhibits cell growth of the NCI‐H2228 cell line 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. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3]
Cell Research NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol[2].
Synonyms RXDX-101, NMS-E628
Molecular Weight 560.64
Formula C31H34F2N6O2
CAS No. 1108743-60-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 67 mg/mL(119.5 mM)

DMSO: 100 mg/mL (178.36 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Rolfo C, et al. Expert Opin Investig Drugs. 2015, 24(11), 1493-1500. 2. Ardini E, et al. Mol Cancer Ther. 2009, 8, A244. 3. Lyer R, et al. Cancer Res. 2015, 75, 5390.

TargetMolCitations

1. Shi S, Ma B, Sun F, et al. Zafirlukast inhibits the growth of lung adenocarcinoma via inhibiting TMEM16A channel activity. Journal of Biological Chemistry. 2022, 298(3). 2. Qin Q, Fu Q, Wang X, et al.Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.European Journal of Medicinal Chemistry.2023: 115291. 3. Jin X, Liu D, Zhou X, et al.Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7.Cell Reports Medicine.2023, 4(12).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Antioxidant Compound Library Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library Fluorochemical Library

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Keywords

Entrectinib 1108743-60-7 Angiogenesis Autophagy Immunology/Inflammation Tyrosine Kinase/Adaptors Trk receptor ROS ALK ROS Kinase ALK tyrosine kinase receptor Inhibitor Cluster of differentiation 246 RXDX-101 Anaplastic lymphoma kinase (ALK) RXDX 101 RXDX101 Trk Receptor inhibit NMS-E628 Tropomyosin related kinase receptor Anaplastic lymphoma kinase CD246 NMS-E-628 NMS-E 628 inhibitor

 

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