Entrectinib (RXDX-101)

For research use only.

Catalog No.S7998 Synonyms: NMS-E628

16 publications

Entrectinib (RXDX-101) Chemical Structure

CAS No. 1108743-60-7

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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Selleck's Entrectinib (RXDX-101) has been cited by 16 publications

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  • 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, 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.
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
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NCI-H2228 MmO1RY51cXS3bX;yJIF{e2G7 M1f1Z|MxKHSxIE[wJI1oN2up NGn5WW0yOCCmYYnz NWL0cFg{SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{MkK4JINmdGy|IIjlco9oemGodHXkJIlvKGG2aIntbYMhdnVxboWgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgN|AhfG9iNkCgcYcwc2duIIDvJIJq\CCjZH3pcol{fGW{ZXSg[o9zKDFyIHThfZM> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228 MVXGeY5kfGmxbjDhd5NigQ>? MV:2NEBu\y:tZx?= NXfrVXllOTJiaILz NHn4UXhGgCC4aY\vJIlvcGmkaYTpc44hd2ZiRV3MOE1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCQQ1mtTFIzOjhiY3XscJMh[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ Mn\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 M2XvXWZ2dmO2aX;uJIF{e2G7 NGHoXXM3OCCvZz;r[y=> NFLLVm8yQCCqcoO= NWHRcGczTXhidnn2c{BqdmirYnn0bY9vKG:oIFXNUFQuSUyNIIDoc5NxcG:{eXzheIlwdiCrbjDheIh6dWmlIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGG2IE[wJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNVghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NES3SJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
NCI-H2228 M2jWPWZ2dmO2aX;uJIF{e2G7 MUm2NEBu\y:tZx?= NY\RR5VvOTJiaILz MYPFfEB3cX[xIHnubIljcXSrb36gc4YhTU2OND3BUGsheGixc4Doc5J6dGG2aX;uJIlvKGG2aIntbYMhdnVxboWgcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBPS0lvSEKyNlgh[2WubIOgZZN{\XO|ZXSgZZMhe3WycILld5Nqd25ib3[gRWtVKHCqb4PwbI9zgWyjdHnvckBifCB4MDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGG|IIPpcodt\SCmb4PlJI1m[XO3cnXkJIFnfGW{IEGyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MonCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 NYHFRmxqTnWwY4Tpc44h[XO|YYm= MoDGOlAhdWdxa3e= M3nPV|E5KGi{cx?= MljuSZghfmm4bzDpcohq[mm2aX;uJI9nKEWPTEStRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCjdHj5cYlkKG63L371JI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hVkOLLViyNlI5KGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGFMXCCyaH;zdIhwenmuYYTpc44h[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxPEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ Mm\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KARPAS299 MkX0RY51cXS3bX;yJIF{e2G7 NG[ydpg{OCC2bzC2NEBu\y:tZx?= NF3RTm4yOCCmYYnz NV7PeVRrSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT2FTWEGVMkm5JINmdGy|IIjlco9oemGodHXkJIlvKFOFSVSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgN|AhfG9iNkCgcYcwc2duIIDvJIJq\CCjZH3pcol{fGW{ZXSg[o9zKDFyIHThfZM> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299 NXXwR4Y{SW62aYT1cY9zKGG|c3H5 NWHzUok5OzBidH:gOlAhdWdxa3e= NVvEPHpGOTBiZHH5dy=> M2\QfWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBUS0mGIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKG[{ZXWgZ5Vz\WRibX;1d4Uh[XRiM{CgeI8hPjBibXevb4ctKHCxIHLp[EBi\G2rbnnzeIVz\WRiZn;yJFExKGSjeYOgcYVie3W{ZXSgc44h\GG7IEmw M2DG[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 MnKzSpVv[3Srb36gZZN{[Xl? M2njTFIhcHK| M4PrbmlvcGmkaYTpc44hd2ZiTmDNM2FNUyCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjdDD2[ZJ6KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NU\6XHRKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 M2TJWGZ2dmO2aX;uJIF{e2G7 NHnUT3gzKGi{cx?= M2PaUWlvcGmkaYTpc44hd2ZiTmDNM2FNUyCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF7DTU1JOjJ{ODDj[YxteyCjdDD2[ZJ6KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MmDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=

... 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
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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04551495 Not yet recruiting Drug: Entrectinib|Drug: Letrozole|Drug: Goserelin Invasive Lobular Breast Carcinoma|ER+ Breast Cancer|HER2-negative Breast Cancer Jules Bordet Institute|Hoffmann-La Roche November 2020 Phase 2
NCT04226833 Recruiting 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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID