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Repotrectinib

Catalog No. T4071 CAS 1802220-02-5

Synonyms: TPX-0005, TPX 0005, TPX0005

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Repotrectinib, CAS 1802220-02-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 172.00
25 mg	In stock	$ 312.00
50 mg	In stock	$ 498.00
100 mg	In stock	$ 725.00
1 mL * 10 mM (in DMSO)	In stock	$ 102.00

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Purity: 100%

Purity: 99.86%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
Targets&IC50	ALK (WT):1.01 nM, ALK (G1202R):1.26 nM, ALK (L1196M):1.08 nM, Src:5.3 nM

Synonyms	TPX-0005, TPX 0005, TPX0005
Molecular Weight	355.37
Formula	C18H18FN5O2
CAS No.	1802220-02-5

Storage

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

Solubility Information

DMSO: 83.3 mg/mL

References and Literature

1. Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016 2. Li W, Perpinioti N, Schinkel A H, et al. Bioanalytical assay for the new-generation ROS1/TRK/ALK inhibitor repotrectinib in mouse plasma and tissue homogenate using liquid chromatography-tandem mass spectrometry[J]. Journal of Chromatography B. 2020: 122098.

Citations

1. Li W, Sparidans R W, Lebre M C, et al. ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, while OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability[J. Pharmaceutics. 2021, 13(11): 1761 2. Li W, Perpinioti N, Schinkel A H, et al. Bioanalytical assay for the new-generation ROS1/TRK/ALK inhibitor repotrectinib in mouse plasma and tissue homogenate using liquid chromatography-tandem mass spectrometry. Journal of Chromatography B. 2020: 122098 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：

Membrane Protein-targeted Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library FDA-Approved Kinase Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library

Related Products

Related compounds with same targets

Crizotinib Taletrectinib APG-2449 Lorlatinib Salvigenin ROS kinases-IN-1 Merestinib Methyl 12-methyltridecanoate

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Repotrectinib 1802220-02-5 Angiogenesis Immunology/Inflammation Tyrosine Kinase/Adaptors ROS Src ALK ROS Kinase Trk receptor ALK tyrosine kinase receptor Trk Receptor inhibit Cluster of differentiation 246 CD246 Anaplastic lymphoma kinase (ALK) Tropomyosin related kinase receptor TPX-0005 Anaplastic lymphoma kinase Inhibitor TPX 0005 TPX0005 inhibitor

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