Description
Savolitinib is an inhibitor of cMET tyrosine kinase or hepatocyte growth factor receptor (HGFR). It potently inhibits the tyrosine kinase activity of recombinant cMET in vitro with an IC₅₀ value of 4 nM. It inhibits proliferation of cell lines SNU‐5, SNU‐638, Hs746T, SNU‐620, GTL16 and IM95m with 50% effective inhibitory concentrations of 0.6 nM, 0.8 nM, 1.3 nM, 3.5 nM, 5.6 nM and 14.7 nM respectively. It shows dose‐responsive anti‐tumor efficacy in gastric cancer Hs746t xenograft model treated once‐daily (0.3 mg/kg, 1 mg/kg or 2.5 mg/kg) orally, for 16 days.
Savolitinib is an inhibitor of cMET tyrosine kinase or hepatocyte growth factor receptor (HGFR). It potently inhibits the tyrosine kinase activity of recombinant cMET in vitro with an IC₅₀ value of 4 nM. It inhibits proliferation of cell lines SNU‐5, SNU‐638, Hs746T, SNU‐620, GTL16 and IM95m with 50% effective inhibitory concentrations of 0.6 nM, 0.8 nM, 1.3 nM, 3.5 nM, 5.6 nM and 14.7 nM respectively. It shows dose‐responsive anti‐tumor efficacy in gastric cancer Hs746t xenograft model treated once‐daily (0.3 mg/kg, 1 mg/kg or 2.5 mg/kg) orally, for 16 days.
Alternate Name/Synonyms: Volitinib; AZD 6094; HM 5016504; HMPL 504; 3-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine; (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; 4-{1-[(1S)-1-{imidazo[1,2-a]pyridin-6-yl}ethyl]-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl}-1-methyl-1H-pyrazole
Appearance: White to off-white powder
Formulation:
CAS Number: 1313725-88-0
Structure Available?: TRUE
Peptide sequence:
Salt Form: FALSE
Molecular Formula: C₁₇H₁₅N₉
Molecular Weight: 345.4
Cell-Permeable?: TRUE
Purity: >98%
Solubilities: ~16 mg/ml in DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: An inhibitor of cMET tyrosine kinase
MDL Number: MFCD28359096
PubChem CID: 68289010
SMILES: CC(C1=CN2C=CN=C2C=C1)N3C4=NC(=CN=C4N=N3)C5=CN(N=C5)C
InChi: 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
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |