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Chemical Structure : Repotrectinib
CAS No.: 1802220-02-5
Catalog No.: PC-62298Not For Human Use, Lab Use Only.
Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $78 | In stock | |
| 10 mg | $118 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | $528 | In stock | |
| 250 mg | Get quote |
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Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants.
Repotrectinib (TPX-0005) potently inhibits WT ALK (IC50=1.01 nM) and mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM).
Repotrectinib (TPX-0005) is also a potent SRC inhibitor (IC50=5.3 nM); shows low nano-molar activities against CD74-ROS1 G2032R (IC50=8.4 nM), LMNA-TRKA G595R (IC50=0.4 nM),TEL-TRKB G639R (IC50=1.9 nM) and TEL-TRKC G623R (IC50=0.4 nM) in Ba/F3 cell proliferation assays; dramatically causes tumor growth inhibition and tumor regression in xenograft tumor model.
Repotrectinib (TPX-0005) demonstrates desired druglike properties and good safety profile.
| M.Wt | 355.373 | |
| Formula | C18H18FN5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(7S,13R)-11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one |
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1. Zhai D, et al. DOI: 10.1158/1538-7445.AM2016-2132 Published July 2016
2. J.J. Cui, et al. DOI: http://dx.doi.org/10.1016/S0959-8049(16)32675-2.
3. Drilon A, et al. Cancer Discov. 2018 Aug 9. pii: CD-18-0484.
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