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Active Pharmaceutical Ingredients
Repotrectinib
Repotrectinib
Repotrectinib
Category:
Active Pharmaceutical Ingredients
CAS NO:
1802220-02-5
Standard:
ChP,USP,BP,EP,JP,In-house Standards,IP,Ph. Int,
Price Range:
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Main Sales Markets:
North America,Central/South America,Western Europe,Eastern Europe,Asia,Middle East,Africa
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Shenzhen Tianyuan Pharmaceutical Technology Co., Ltd.
Shenzhen Tianyuan Pharmaceutical Technology Co., Ltd.
2
Years
Standard Member Standard Member
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Basic Info
Grade
Pharmaceutical Grade
Is Manufacturer
YES
Payment Method
L/C
Samples Provided
YES
Product Description

Repotrectinib Biological Activity

Description:Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.

Target:IC50: 5.3 nM (SRC), 1.01 nM (WT ALK), 1.26 nM (ALK G1202R), 1.08 nM (ALK L1196M)

In Vitro:Repotrectinib (TPX-0005) effectively overcomes this primary resistance (IC50 100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50 13 nM) and the SRC substrate paxillin (IC50 107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib.

In Vivo:Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts.

 

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