A dual inhibitor of wild-type and ex20ins mutation-containing EGFR and HER2
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Sevabertinib

Item No. 44586

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(3-chloro-2-methoxyphenyl)amino]-2-[3-[(2S)-1,4-dioxan-2-ylmethoxy]-4-pyridinyl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
CAS Number
2521285-05-0
Synonyms
  • BAY-2927088
Molecular Formula
C24H25ClN4O5
Formula Weight
484.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(NCC1)C2=C1NC(C3=CC=NC=C3OC[C@H]4OCCOC4)=C2NC5=C(C(Cl)=CC=C5)OC
InChi Code
InChI=1S/C24H25ClN4O5/c1-31-23-16(25)3-2-4-18(23)29-22-20-17(6-8-27-24(20)30)28-21(22)15-5-7-26-11-19(15)34-13-14-12-32-9-10-33-14/h2-5,7,11,14,28-29H,6,8-10,12-13H2,1H3,(H,27,30)/t14-/m0/s1
InChi Key
VYQVHWNNPKOJEA-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Sevabertinib is a dual inhibitor of wild-type and exon 20 insertion (ex20ins) mutation-containing EGFR and HER2 (IC50s = <0.5 nM for EGFR, EGFR exon20 D770 insSVD, HER2, and HER2 exon20 A775 insYMVA).1 It is selective for these proteins over HER4 (IC50 = 13.96 nM). Sevabertinib (0.01-1 µM) reduces the viability of A431, NCI-H2170, NCI-H1781, and MDA-MB-175-VII cells endogenously expressing EGFR or HER2 wild-type or insertion mutant gene amplifications. In vivo, sevabertinib (5 and 10 mg/kg) reduces tumor growth in a HER2 exon20 A775 insYMVA mutant-containing CTG-2543 patient-derived xenograft (PDX) mouse model. Formulations containing sevabertinib have been used in the treatment of non-small cell lung cancer (NSCLC).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Siegel, F., Siegel, S., Kotýnková, K., et al. Sevabertinib, a reversible HER2 inhibitor with activity in lung cancer. Cancer Discov. (2025).