A brain-penetrant c-Met inhibitor
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Vebreltinib

Item No. 46227

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-[difluoro(6-fluoro-2-methyl-2H-indazol-5-yl)methyl]-1,2,4-triazolo[4,3-b]pyridazine
CAS Number
1440964-89-5
Synonyms
  • APL 101
  • Beritinib
  • Bozitinib
  • CBI 3103
  • PLB 1001
Molecular Formula
C20H15F3N8
Formula Weight
424.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
FC1=CC2=NN(C)C=C2C=C1C(F)(C3=NN=C4C=CC(C5=CN(C6CC6)N=C5)=NN43)F
InChi Code
InChI=1S/C20H15F3N8/c1-29-9-11-6-14(15(21)7-17(11)27-29)20(22,23)19-26-25-18-5-4-16(28-31(18)19)12-8-24-30(10-12)13-2-3-13/h4-10,13H,2-3H2,1H3
InChi Key
QHXLXUIZUCJRKV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $175

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    10 mg

    $333

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    25 mg

    $569

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    50 mg

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    Product Description

    Vebreltinib is a brain-penetrant inhibitor of c-Met.1 It inhibits MET activity by 95% in an enzyme assay at 2 µM. Vebreltinib (30 µM) inhibits the phosphorylation of MET and STAT3 in primary human astrocytes expressing an exogenous PTPRZ1-MET (ZM) fusion or the MET exon 14 skipping alteration (METex14). It reduces tumor weight in a subcutaneous mouse xenograft model of glioma using U87MG cells expressing the E2-E2 ZM fusion variant. It increases survival in an orthotopic mouse xenograft model using the same cells. Vebreltinib also reduces the viability of MKN45 gastric cancer cells with MET amplification (IC50 = 12 nM) but not KATO III gastric cancer cells with low c-Met expression (IC50 = >1,000 nM).2 Formulations containing vebreltinib have been used in the treatment of non-small cell lung cancer in patients with the METex14 alteration.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hu, H., Mu, Q., Bao, Z., et al. Mutational landscape of secondary glioblastoma guides MET-targeted trial in brain tumor. Cell 175(6), 1665-1678 (2018).

    2. Lin, H., Qu, L., Wei, H., et al. Characterization of Bozitinib as a potential therapeutic agent for MET-amplified gastric cancer. Commun. Biol. 8(1), 134 (2025).