A pan-Trk, ROS1, and ALK inhibitor
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Entrectinib

Item No. 19476

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-benzamide
CAS Number
1108743-60-7
Synonyms
  • NMS-E628
  • RXDX-101
Molecular Formula
C31H34F2N6O2
Formula Weight
560.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
302, 348 nm
SMILES
O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=CC=C(N5CCN(C)CC5)C=C4NC6CCOCC6
InChi Code
InChI=1S/C31H34F2N6O2/c1-38-8-10-39(11-9-38)25-3-4-26(29(19-25)34-24-6-12-41-13-7-24)31(40)35-30-27-17-20(2-5-28(27)36-37-30)14-21-15-22(32)18-23(33)16-21/h2-5,15-19,24,34H,6-14H2,1H3,(H2,35,36,37,40)
InChi Key
HAYYBYPASCDWEQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Entrectinib is an inhibitor of TrkA (IC50 = 1.7 nM), TrkB (IC50 = 0.1 nM), and TrkC (IC50 = 0.1 nM), as well as C-ros oncogene 1 (ROS1; IC50 = 0.2 nM) and anaplastic lymphoma kinase (ALK; IC50 = 1.6 nM).1,2 Entrectinib blocks proliferation of ALK-dependent cell lines, including those with L1196M or C1156Y resistance mutations, and inhibits ALK‐dependent signaling.2,3 It has been shown to inhibit the growth of a non-small cell lung cancer cell line bearing an EML4-ALK rearrangement.2,3 In mice bearing various Trk, ROS1, or ALK-driven xenografts, entrectinib has been shown to induce tumor regression.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Siena, S., Drilon, A.E., Ou, S.H.I., et al. Enrectinib (RXDX-101), an oral pan-Trk, ROS1, and ALK inhibitor in patients with advanced solid tumors harboring gene rearrangements. (2015).

    2. Ardini, E., Menichincheri, M., De Ponti, C., et al. Characterization of NMS-E628, a small molecule inhibitor of anaplastic lymphoma kinase with antitumor efficacy in ALK-dependent lymphoma and non-small cell lung cancer models. Mol. Cancer Res. 8(12 suppl), A244 (2009).

    3. Sullivan, I., and Planchard, D. ALK inhibitors in non-small cell lung cancer: The latest evidence and developments. Ther. Adv. Med. Oncol. 8(1), 32-47 (2016).