CAS No. 2769954-39-2

Batch: Purity:98.81
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Pebezertinib (BLU-451, LNG-451) Chemical Structure
Chemical Structure
Check the Pebezertinib (BLU-451, LNG-451) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Chemical Information

IUPAC Name N-[4-fluoro-3-[[2-[(1-methylpyrazol-4-yl)amino]-5-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
CAS Number 2769954-39-2
Molecular Formula

C24H19F4N7O
Molecular Weight (MW) 497.45
InChIKey XIMJCWSFLXXQMZ-UHFFFAOYSA-N

Biological Activity

Pebezertinib (BLU-451) is a central nervous system-penetrant, wild-type EGFR-sparing, covalent inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion mutants. By selectively targeting EGFR exon 20 insertions, it suppresses receptor autophosphorylation and downregulates downstream signaling pathways such as AKT/mTOR and MAPK. This targeted inhibition impairs tumor cell proliferation and demonstrates potent anti-tumor efficacy in cell-derived and patient-derived xenograft models of non-small cell lung cancer. [1]

How to Prepare Stock Solution?

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Solubility

Batch:
All in vitro solubility values are batch-tested experimental data (non-literature values).
Solvent Solubility & Note
DMSO 99 mg/mL (199.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.)
Ethanol 6 mg/mL
Water Insoluble
FAQ
Q: Why does a DMSO stock precipitate in media/saline?
A: It is caused by unheated aqueous media (supersaturation), local solvent shock, or incorrect mixing sequence.
How to fix it?
  • Preheat media/saline to 37°C.
  • Mix rapidly (pipette/vortex) upon addition.
  • For complex mixes, always add the aqueous phase last.
  • Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).

Reference

[1] Millet YA, et al. Mol Cancer Ther. 2026.

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Note: Technical data last updated: Sep 1, 2026.