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    Entrectinib (NMS-E 628; RXDX101; ROZLYTREK)
    Entrectinib (NMS-E 628; RXDX101; ROZLYTREK)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0609
    CAS #: 1108743-60-7Purity ≥98%

    Description: Entrectinib (formerly also known as NMS-E628; RXDX-101; trade name ROZLYTREK) is a potent and orally bioavailable small molecule inhibitor of TrkA, TrkB, TrkC, ROS1 and ALK with potential antitumor activity. It inhibits the above mentioned kinases with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. In 2019, Entrectinib was approved by US FDA to treat ROS1-positive non-small cell lung cancer (NSCLC) and NTRK fusion-positive solid tumors. It was also approved for NSCLC in Australia in May 2020, and in the European Union in July 2020.

    References: Expert Opin Investig Drugs. 2015;24(11):1493-500.

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    Molecular Weight (MW)560.64
    FormulaC31H34F2N6O2
    CAS No.1108743-60-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (178.4 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (178.4 mM)
    Other infoChemical Name: N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide
    SMILES Code: O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=CC=C(N5CCN(C)CC5)C=C4NC6CCOCC6
    SynonymsEntrectinib, RXDX-101, NMS-E628; RXDX101; RXDX 101; RXDX-101; NMS E628; NMS-E-628; trade nameROZLYTREK



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    In Vitro

    In vitro activity: 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.


    Kinase Assay: Entrectinib is a potent and orally available Trk, ROS1, and ALK inhibitor; inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively.


    Cell Assay: NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol. 

    In VivoIn 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. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy.
    Animal model Mice bearing Karpas-299 and SR-786 xenograft models
    Formulation & Dosage p.o. and i.v.; Entrectinib is reconstituted in 0.5% methylcellulose containing 1% Tween 80 at a final dosing volume of 10 mL/kg (e.g., 0.2 mL for a 20 gm mouse). Treatment with entrectinib, Irino and TMZ started about 15–17 days after tumor inoculation when the average tumor size is 0.2 cm3. Mice are sacrificed when tumor volume reached 3 cm3.  
    ReferencesExpert Opin Investig Drugs. 2015;24(11):1493-500; Cancer Res 2013;73(8 Suppl): Abstract nr 2092. doi:10.1158/1538-7445.AM2013-2092.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Entrectinib

    Mechanism of action and in vivo activity of entrectinib in ALK-driven ALCL cell lines and xenograft models.  2016 Apr;15(4):628-39.

    Entrectinib

    In vivo activity of entrectinib in an NPM-ALK transgenic model.  2016 Apr;15(4):628-39.

    Entrectinib

    Activity of entrectinib against NCI-H2228 NSCLC tumors.  2016 Apr;15(4):628-39.


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