| Identification | Back Directory | [Name]
PF 04217903 mesylate | [CAS]
956906-93-7 | [Synonyms]
PF-04217903.MsOH
PF 04217903 mesylate
HBEMHKVWZJTVOC-UHFFFAOYSA-N
PF-04217903 Methanesulfonate
PF04217903 METHANESULFONATE;PF 04217903 METHANESULFONATE
4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol mesylate
4-[1-(6-QuinolinylMethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol Methanesulfonate
4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol methanesulfonate (1:1)
2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethan-1-ol methanesulfonate | [Molecular Formula]
C20H20N8O4S | [MDL Number]
MFCD17392584 | [MOL File]
956906-93-7.mol | [Molecular Weight]
468.489 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥5mg/mL (warmed) | [form ]
powder | [color ]
white to beige | [InChI]
1S/C19H16N8O.CH4O3S/c28-7-6-26-12-15(9-22-26)17-10-21-18-19(23-17)27(25-24-18)11-13-3-4-16-14(8-13)2-1-5-20-16;1-5(2,3)4/h1-5,8-10,12,28H,6-7,11H2;1H3,(H,2,3,4) | [InChIKey]
HBEMHKVWZJTVOC-UHFFFAOYSA-N | [SMILES]
CS(O)(=O)=O.OCCn1cc(cn1)-c2cnc3nnn(Cc4ccc5ncccc5c4)c3n2 |
| Hazard Information | Back Directory | [Uses]
PF 04217903 is highly selective, high affinity c-Met inhibitor (Ki = 6-7 nM against wild type c-Met). Displays >1000-fold selectivity for c-Met over a panel of 208 kinases. | [Biological Activity]
PF-04217903 is a highly selectivepotent inhibitor of the hepatocyte growth factor receptor c-Met. PF-04217903 inhibits endogenouswild type c-Met in A549 human lung carcinoma cells with an IC50 of 4.8 nM. The compund displays 1000-fold selectivity against a panel of 208 other kinases.''PF-04217903 is an ATP-competitive inhibitor. It elicits antiangiogenic functionality. PF-04217903 inhibits c-Met phosphorylation in xenograft models leading to partial tumor growth suppression. | [in vivo]
PF-04217903 mesylate (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors [1].
PF-04217903 mesylate (5-50 mg/kg, p.o.; once daily for 3 days) dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels. PF-04217903 mesylate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 mesylate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors[1]. | Animal Model: | Female nu/nu mice GTL-16 xenograft model[1] | | Dosage: | 1, 3, 10, 30 mg/kg | | Administration: | Oral; daily for 16 days | | Result: | Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.
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| [storage]
Store at +4°C |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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