Entrectinib (RXDX-101)

Catalog No.S7998 Synonyms: NMS-E628

Entrectinib (RXDX-101) Chemical Structure

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.

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Cited by 5 Publications

4 Customer Reviews

  • Tumor cells were treated with entrectinib (10 nmol/L) for 4 hours or c-PARP for 48 hours, and harvested lysates were assessed by Western blotting. Data shown are representative of three independent experiments with similar results.

    Clin Cancer Res, 2018, 24(10):2357-2369. Entrectinib (RXDX-101) purchased from Selleck.

    (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.

    The effect of kinase inhibitors on signal transduction in human cancer cell lines in vitro. H1975 cells were treated with osimertinib (1 μmol/L) for 2 h. NUGC4 cells were treated with crizotinib (1 μmol/L) for 2 h, and then stimulated with HGF (50 ng/mL) for 10 min. 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.

    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.
Targets
TrkA [1] TrkB [1] TrkC [1] ROS1 [1] ALK [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV411 MWfQdo9tcW[ncnH0bY9vKGG|c3H5 MV[3NkBp M1rXWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0NVEh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYpvwKxKSzVyPUCuNFgyKM7:TR?= MWKyO|AxOzd4MR?=
KM12 MmT2VJJwdGmoZYLheIlwdiCjc4PhfS=> M1\yflczKGh? NYPRbnExSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIV5eHKnc4PpcochXFKNQTDwdo91\WmwIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxRTBwMEG3JO69VQ>? MV2yO|AxOzd4MR?=
SU-DHL1 NVnaTIVLWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYi3NkBp M3naWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2WtSGhNOSClZXzsd{BmgHC{ZYPzbY5oKEGOSzDwdo91\WmwIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxRTBwMEK0JO69VQ>? MXGyO|AxOzd4MR?=
SUP-M2 MkPRVJJwdGmoZYLheIlwdiCjc4PhfS=> MkiyO|IhcA>? M4LFc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2XQMW0zKGOnbHzzJIV5eHKnc4PpcochSUyNIIDyc5RmcW5iaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVA:OC5yNEGg{txO MYWyO|AxOzd4MR?=
NCI-H2228 NFPNUmFRem:uaX\ldoF1cW:wIHHzd4F6 MlzqO|IhcA>? NFjINndCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOjJ{ODDj[YxteyCneIDy[ZN{cW6pIFHMT{Bxem:2ZXnuJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG|c3H5 NUWxRZkxOjdyMEO3OlE>
KARPAS299 MWHQdo9tcW[ncnH0bY9vKGG|c3H5 M370WlczKGh? MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuDUmDBV|I6QSClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2wMlA{OSEQvF2= NVPqbFNmOjdyMEO3OlE>
SR786 M2LsTnBzd2yrZnXyZZRqd25iYYPzZZk> MYm3NkBp NGf6Tm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSO|g3KGOnbHzzJIV5eHKnc4PpcochSUyNIIDyc5RmcW5iaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVA:OC5yOEGg{txO M1vUblI4ODB|N{[x

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin A1 / Cyclin E1 / p27 / p21; 

PubMed: 26735175     


Expression of cell cycle regulatory proteins (p21, p27, Cyclin A1, and Cyclin E1) was validated by Western Blot 24h after treatment with entrectinib. Gapdh was used as a control of proper protein loading. Numbers indicate concentration of entrectinib (e; 䲧疝Ỵ疞㧀疜膉痘 

p-ALK / ALK / p-ERK / ERK / p-STAT3 / STAT3; 

PubMed: 26735175     


Using entrectinib (e) IC50 defined for 48h, Eventual change of ALK downstream pathway after treatment with entrectinib was validated by Western blot. 

pTrkA-Y490 / TrkA / p-PLCγ-Y783 / PLCγ ; 

PubMed: 28903424     


Western blot analysis of the changes in phosphorylation levels of TRKA and its downstream transducer PLCγ 2 hours post entrectinib and crizotinib treatment in Ba/F3-SCYL3-NTRK1 cells.

pAKT / AKT; 

PubMed: 26172300     


Western blot demonstrating Inhibition of the phosphorylation of the ALK protein and other downstream signal molecules in the EML4-ALK CRC patient tumor derived cell line after inhibition by crizotinib or entrectinib.

26735175 28903424 26172300
Growth inhibition assay
Cell viability ; 

PubMed: 26172300     


Inhibition of the growth of the EML4-ALK CRC patient derived tumor cells with 1 μM crizotinib or 1 μM entrectinib.

26172300
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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03796260 Recruiting Healthy Volunteers Genentech Inc. January 9 2019 Phase 1
NCT03796013 Completed Healthy Volunteers Genentech Inc. January 10 2019 Phase 1
NCT03796260 Recruiting Healthy Volunteers Genentech Inc. January 9 2019 Phase 1
NCT03796013 Completed Healthy Volunteers Genentech Inc. January 10 2019 Phase 1
NCT03330990 Completed Advanced Solid Tumor Hoffmann-La Roche November 14 2017 Phase 1
NCT03330990 Completed Advanced Solid Tumor Hoffmann-La Roche November 14 2017 Phase 1

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.

Handling Instructions

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID