Entrectinib (RXDX-101)

For research use only.

Catalog No.S7998 Synonyms: NMS-E628

12 publications

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. Entrectinib (RXDX-101) induces autophagy. Phase 2.

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Selleck's Entrectinib (RXDX-101) has been cited by 12 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

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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. 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
MV411 MXLQdo9tcW[ncnH0bY9vKGG|c3H5 NHPrTYg4OiCq MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YNEGxJINmdGy|IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G778{MTWM2OD1yLkC4NUDPxE1? MmPMNlcxODN5NkG=
KM12 M4HzU3Bzd2yrZnXyZZRqd25iYYPzZZk> MlPGO|IhcA>? MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPMUKgZ4VtdHNiZYjwdoV{e2mwZzDUVmtCKHC{b4TlbY4hcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUC9NE4xOTdizszN MVWyO|AxOzd4MR?=
SU-DHL1 MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NELGc|A4OiCq NXLUOlYySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWU1FUExzIHPlcIx{KGW6cILld5NqdmdiQVzLJJBzd3SnaX6gbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTB;MD6wNlQh|ryP NFm0O3MzPzByM{e2NS=>
SUP-M2 NFyxdYNRem:uaX\ldoF1cW:wIHHzd4F6 NILRZog4OiCq MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXUD3NNkBk\WyuczDlfJBz\XO|aX7nJGFNUyCycn;0[YlvKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwQVAvODRzIN88US=> Mnj3NlcxODN5NkG=
NCI-H2228 Ml7UVJJwdGmoZYLheIlwdiCjc4PhfS=> MlHKO|IhcA>? MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlIzQCClZXzsd{BmgHC{ZYPzbY5oKEGOSzDwdo91\WmwIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7 MV2yO|AxOzd4MR?=
KARPAS299 M13TfnBzd2yrZnXyZZRqd25iYYPzZZk> MkLYO|IhcA>? M{LCSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwQVAvODNzIN88US=> MmPFNlcxODN5NkG=
SR786 M36zbXBzd2yrZnXyZZRqd25iYYPzZZk> NIHxUoM4OiCq MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUN{i2JINmdGy|IHX4dJJme3OrbnegRWxMKHC{b4TlbY4hcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUC9NE4xQDFizszN MVKyO|AxOzd4MR?=

... 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)
Water Insoluble
Ethanol ''75 mg/mL

* 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(=O)NC3=N[NH]C4=C3C=C(CC5=CC(=CC(=C5)F)F)C=C4)C(=C2)NC6CCOCC6

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04226833 Suspended 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
NCT02097810 Active not recruiting Drug: Entrectinib Locally Advanced Solid Tumors|Metastatic Solid Tumors Hoffmann-La Roche July 28 2014 Phase 1

Tech Support

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID