TargetMol

Repotrectinib

Product Code:
 
TAR-T4071
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
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CodeSizePrice
TAR-T4071-2mg2mg£125.00
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TAR-T4071-5mg5mg£148.00
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TAR-T4071-1mL1 mL * 10 mM (in DMSO)£152.00
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TAR-T4071-10mg10mg£210.00
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TAR-T4071-25mg25mg£321.00
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TAR-T4071-50mg50mg£470.00
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Further Information

Bioactivity:
TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
CAS:
1802220-02-5
Formula:
C18H18FN5O2
Molecular Weight:
355.373
Pathway:
Tyrosine Kinase/Adaptors; Immunology/Inflammation; Angiogenesis
Purity:
0.9986
SMILES:
C[C@H]1CNC(=O)c2cnn3ccc(N[C@H](C)c4cc(F)ccc4O1)nc23
Target:
Trk receptor; ROS; Src; ALK; ROS Kinase

References

Li W, Perpinioti N, Schinkel A H, et al. Bioanalytical assay for the new-generation ROS1/TRK/ALK inhibitor repotrectinib in mouse plasma and tissue homogenate using liquid chromatography-tandem mass spectrometry. Journal of Chromatography B. 2020: 122098 Li W, Sparidans R W, Lebre M C, et al. ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, while OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability[J. Pharmaceutics. 2021, 13(11): 1761 Li W, Perpinioti N, Schinkel A H, et al. Bioanalytical assay for the new-generation ROS1/TRK/ALK inhibitor repotrectinib in mouse plasma and tissue homogenate using liquid chromatography-tandem mass spectrometry[J]. Journal of Chromatography B. 2020: 122098. Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016