Savolitinib | B3006

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.

B3006 | Savolitinib DataSheet

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