Synonyms: BLU451 | compound I [WO2023215431A1] [3] | Example 37 [WO2022094354A1] [4] | LNG-451 | LNG451
Compound class:
Synthetic organic
Comment: Although the name-to-structure for BLU-451 has not been formally published, a focussed review of patents [3-4], declared company pipelines (Blueprint Medicines [1]), published literature, meeting abstracts [6] and other online information leads us to consider the chemical structure presented here as a very strong candidate for BLU-451.
BLU-451 (formerly LNG-451) is a wild-type EGFR-sparing, CNS-penetrant and covalent EGFR Exon 20 insertion (Ex20ins) inhibitor that is in development for anti‑tumour potential, particularly for non-small cell lung cancers that express variant EGFRs with Exon 20 insertions (i.e., resistance mutations) [2,5]. The Ex20ins-targeting drugs amivantamab and mobocertinib are already in clinical use, but their activity within the brain has not been established. Minimising activity at WT EGFRs is propsed to reduce on-target toxicity. |
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Classification | |
Compound class | Synthetic organic |
IUPAC Name |
N-[4-fluoro-3-[[2-[(1-methylpyrazol-4-yl)amino]-5-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl]amino]phenyl]prop-2-enamide |
Synonyms | |
BLU451 | compound I [WO2023215431A1] [3] | Example 37 [WO2022094354A1] [4] | LNG-451 | LNG451 |
Database Links | |
GtoPdb PubChem SID | 491299846 |
PubChem CID | 163280903 |
Search Google for chemical match using the InChIKey | XIMJCWSFLXXQMZ-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | XIMJCWSFLXXQMZ |
UniChem Compound Search for chemical match using the InChIKey | XIMJCWSFLXXQMZ-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | XIMJCWSFLXXQMZ-UHFFFAOYSA-N |