Enozertinib (ORIC-114) is a brain-penetrant, orally bioavailable, irreversible inhibitor targeting EGFR and HER2 exon 20 insertions and atypical EGFR mutations. In preclinical studies, it demonstrated low nanomolar potency against these mutations, with enhanced selectivity over wild-type EGFR, and superior kinome selectivity compared to other inhibitors like firmonertinib and lazertinib . In vivo, ORIC-114 induced over 90% tumor growth inhibition in EGFR exon 20 insertion NSCLC models and showed significant regression of intracranial tumors, outperforming TAK-788 .
MedKoo Cat#: 128491
Name: Enozertinib
CAS#: 2489185-38-6
Chemical Formula: C35H42F2N8O3
Exact Mass: 660.3348
Molecular Weight: 660.77
Elemental Analysis: C, 63.62; H, 6.41; F, 5.75; N, 16.96; O, 7.26
The following data is based on the product molecular weight 660.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
