1802220-02-5
1802220-02-5
Chemical Structure
Repotrectinib
Synonym(s): TPX-0005
- CAS No.: 1802220-02-5
- Formula:C18H18FN5O2
- Molecular Weight:355.37
IUPAC Name: (13E,14E,3R,6S)-45-fluoro-3,6-dimethyl-5-oxa-2,8-diaza-1(5,3)-pyrazolo[1,5-a]pyrimidina-4(1,2)-benzenacyclononaphan-9-one
InChIKey: FIKPXCOQUIZNHB-WDEREUQCSA-N
SMILES: O=C1NC[C@H](C)OC2=CC=C(F)C=C2[C@@H](C)NC3=NC4=C1C=NN4C=C3
Biological Activity: Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Repotrectinib | 99.95% | Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity. | ||||||||||||||||||||
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Repotrectinib (Standard) | ≥98% | Repotrectinib (Standard) is the analytical standard of Repotrectinib (HY-103022). This product is intended for research and analytical applications. Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity. | ||||||||||||||||||||
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References
- [1]. 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
- [2]. Karachaliou N, et al. Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis. EBioMedicine. 2018 Mar;29:112-127. [Content Brief]
