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Entrectinib (RXDX-101)
Catalog No.S7998 Synonyms: NMS-E628
For research use only.
Entrectinib (RXDX-101, NMS-E628) 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.
CAS No. 1108743-60-7
Selleck's Entrectinib (RXDX-101) has been cited by 29 publications
Purity & Quality Control
Choose Selective Trk receptor Inhibitors
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Biological Activity
| Description | Entrectinib (RXDX-101, NMS-E628) 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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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)
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Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 560.64 | ||
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| Formula | C31H34F2N6O2 |
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| CAS No. | 1108743-60-7 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6 | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04551495 | Recruiting | Drug: Entrectinib|Drug: Letrozole|Drug: Goserelin | Invasive Lobular Breast Carcinoma|ER+ Breast Cancer|HER2-negative Breast Cancer | Jules Bordet Institute|Hoffmann-La Roche | January 14 2021 | Phase 2 |
| NCT04226833 | Completed | Drug: entrectinib | Hepatic Insufficiency | Hoffmann-La Roche | February 11 2020 | Phase 1 |
| NCT03796013 | Completed | Drug: Entrectinib Form A|Drug: Entrectinib Form C | Healthy Volunteers | Genentech Inc. | January 10 2019 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-08-01)
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