Entrectinib (RXDX-101)
Catalog No.S7998 Synonyms: NMS-E628
Molecular Weight(MW): 560.64
Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.
2 Customer Reviews
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(A) We transfected the EGFP/Eluc gene into KM12SM cells to establish KM12SM/Eluc cells. KM12SM/Eluc cells were inoculated into the brain of SCID mice. The mice were treated daily with or without entrectinib (15 mg/kg) for 37 days until the bioluminescence increased. Mean ± SE of total flux are shown in the lower panel. Then, the entrectinib-treated brain tumor was harvested at the point indicated by the orange triangle and cultured in vitro. The expanded tumor cells were named KM12SM-ER. (B) The sensitivity of KM12SM-ER and KM12SM cells to entrectinib was determined through cell viability assays, using a CCK-8 kit. The data (mean ± standard deviation [SD] of triplicate cultures) shown are representative of three independent experiments with similar results. (C) Tumor cells were treated with entrectinib (10 nmol/L) for 4 h or c-PARP for 48 h, and harvested lysates were assessed by western blotting. Data shown are representative of three independent experiments with similar results.
Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-17-1623. Entrectinib (RXDX-101) purchased from Selleck.
KM12C and KM12SM cells were treated with crizotinib (1 μmol/L) or entrectinib (1 μmol/L) for 2 h. Immunoblots of cell lysates from these treated cell lines are shown. The data are representative of three independent experiments, showing similar results.
Cancer Med, 2017, 6(12):2972-2983. Entrectinib (RXDX-101) purchased from Selleck.
Purity & Quality Control
Choose Selective Trk receptor Inhibitors
Biological Activity
| Description | Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. 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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| 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
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (178.36 mM) |
|---|---|---|
| Ethanol | 75 mg/mL (133.77 mM) | |
| Water | 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.
Chemical Information
| Molecular Weight | 560.64 |
|---|---|
| Formula | C31H34F2N6O2 |
| CAS No. | 1108743-60-7 |
| Storage | powder |
| in solvent | |
| Synonyms | NMS-E628 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02650401 | Recruiting | Solid Tumors|CNS Tumors|Neuroblastoma | Hoffmann-La Roche | May 3 2016 | Phase 1 |
| NCT02097810 | Active not recruiting | Locally Advanced Solid Tumors|Metastatic Solid Tumors | Hoffmann-La Roche | July 28 2014 | Phase 1 |
| NCT02587650 | Recruiting | ALK Fusion Protein Expression|BRAF wt Allele|Invasive Skin Melanoma|MET Fusion Gene Positive|NRAS wt Allele|NTRK1 Fusion Positive|NTRK2 Fusion Positive|NTRK3 Fusion Positive|RET Fusion Positive|ROS1 Fusion Positive|Stage III Cutaneous Melanoma AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7 | University of California San Francisco|National Cancer Institute (NCI) | March 26 2015 | Phase 2 |
| NCT02568267 | Recruiting | Breast Cancer|Cholangiocarcinoma|Colorectal Cancer|Head and Neck Neoplasms|Lymphoma Large-Cell Anaplastic|Melanoma|Neuroendocrine Tumors|Non-Small Cell Lung Cancer|Ovarian Cancer|Pancreatic Cancer|Papillary Thyroid Cancer|Primary Brain Tumors|Renal Cell Carcinoma|Sarcomas|Salivary Gland Cancers|Adult Solid Tumor | Hoffmann-La Roche | November 19 2015 | Phase 2 |
| NCT03330990 | Completed | Advanced Solid Tumor | Hoffmann-La Roche | November 14 2017 | Phase 1 |
| NCT03066661 | Temporarily not available | Cancers With NTRK ROS1 or ALK Gene Fusions | Ignyta Inc. | null | -- |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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