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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 28 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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| Targets |
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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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| Assay |
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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)
| References |
|
|---|
Solubility (25°C)
|
In vitro |
DMSO |
100 mg/mL
(178.36 mM) |
| Ethanol |
75 mg/mL
(133.77 mM) |
|
| Water |
Insoluble
|
Chemical Information
| Molecular Weight | 560.64 | ||
|---|---|---|---|
| Formula | C31H34F2N6O2 |
||
| 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 | ||
In vivo Formulation Calculator (Clear solution)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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 2022-01-17)
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