An inhibitor of c-Met
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Savolitinib

Item No. 33332

Technical Information
Formal Name
1-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-1,2,3-triazolo[4,5-b]pyrazine
CAS Number
1313725-88-0
Synonyms
  • AZD6094
  • HMPL-504
  • Volitinib
Molecular Formula
C17H15N9
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml
λmax
225, 348 nm
SMILES
C[C@@H](C1=CN2C(C=C1)=NC=C2)N3C4=NC(C5=CN(C)N=C5)=CN=C4N=N3
InChi Code
InChI=1S/C17H15N9/c1-11(12-3-4-15-18-5-6-25(15)10-12)26-17-16(22-23-26)19-8-14(21-17)13-7-20-24(2)9-13/h3-11H,1-2H3/t11-/m0/s1
InChi Key
XYDNMOZJKOGZLS-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Savolitinib is an inhibitor of c-Met (IC50 = 5 nM).1 It is selective for c-Met over a panel of 274 other kinases at 1 µM. Savolitinib inhibits c-Met autophosphorylation in NCI H441 human non-small cell lung cancer (NSCLC) cells (IC50 = 3 nM). It also inhibits proliferation of NCI H441 cells induced by HGF (Item No. 32052; IC50 = 6 nM) and in a panel of gastric cancer cells with dysregulated c-Met (EC50s = 0.6-14.7 nM).1,2 Savolitinib (3 mg/kg) inhibits intratumor c-Met autophosphorylation by 94% and reduces tumor growth in an Hs 746T human stomach cancer mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jia, H., Dai, G., Weng, J., et alDiscovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer. J. Med. Chem. 57(18), 7577-7589 (2014).

    2. Gavine, P.R., Ren, Y., Han, L., et alVolitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models. Mol. Oncol. 9(1), 323-333 (2015).