TargetMol

Entrectinib

Product Code:
 
TAR-T3678
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
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TAR-T3678-2mg2mg£99.00
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TAR-T3678-5mg5mg£114.00
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TAR-T3678-1mL1 mL * 10 mM (in DMSO)£121.00
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TAR-T3678-10mg10mg£136.00
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TAR-T3678-25mg25mg£161.00
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TAR-T3678-50mg50mg£208.00
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TAR-T3678-100mg100mg£309.00
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Further Information

Bioactivity:
Entrectinib is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK?dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
CAS:
1108743-60-7
Formula:
C31H34F2N6O2
Molecular Weight:
560.65
Pathway:
Tyrosine Kinase/Adaptors; Angiogenesis; Immunology/Inflammation; Autophagy
Purity:
0.9961
SMILES:
CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1
Target:
Trk receptor; ROS; ALK; Autophagy; ROS Kinase

References

Ardini E, et al. Mol Cancer Ther. 2009, 8, A244. Rolfo C, et al. Expert Opin Investig Drugs. 2015, 24(11), 1493-1500. Lyer R, et al. Cancer Res. 2015, 75, 5390. Shi S, Ma B, Sun F, et al. Zafirlukast inhibits the growth of lung adenocarcinoma via inhibiting TMEM16A channel activity. Journal of Biological Chemistry. 2022, 298(3). Qin Q, Fu Q, Wang X, et al.Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.European Journal of Medicinal Chemistry.2023: 115291.