PF 04217903 mesylate
- Product Name
- PF 04217903 mesylate
- CAS No.
- 956906-93-7
- Chemical Name
- PF 04217903 mesylate
- Synonyms
- PF-04217903.MsOH;PF 04217903 mesylate;HBEMHKVWZJTVOC-UHFFFAOYSA-N;PF-04217903 Methanesulfonate;PF-04217903 mesylate/PF04217903 mesylate;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
- CBNumber
- CB92535688
- Molecular Formula
- C20H20N8O4S
- Formula Weight
- 468.49
- MOL File
- 956906-93-7.mol
PF 04217903 mesylate Property
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥5mg/mL (warmed)
- form
- powder
- color
- white to beige
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0263
- Product name
- PF-04217903
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $138
- Updated
- 2025/07/31
- Product number
- SML0263
- Product name
- PF-04217903
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $375
- Updated
- 2025/07/31
- Product number
- 4239
- Product name
- PF04217903mesylate
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $284
- Updated
- 2021/12/16
- Product number
- P293990
- Product name
- PF04217903Mesylate
- Packaging
- 10mg
- Price
- $195
- Updated
- 2021/12/16
- Product number
- P293990
- Product name
- PF04217903Mesylate
- Packaging
- 100mg
- Price
- $1540
- Updated
- 2021/12/16
PF 04217903 mesylate Chemical Properties,Usage,Production
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 selective, potent inhibitor of the hepatocyte growth factor receptor c-Met. PF-04217903 inhibits endogenous, wild 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. |
storage
Store at +4°C
PF 04217903 mesylate Preparation Products And Raw materials
Raw materials
Preparation Products
PF 04217903 mesylate Suppliers
- Tel
- --
- Fax
- --
- sales@ajchem.in
- Country
- India
- ProdList
- 6100
- Advantage
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