ChemicalBook > CAS DataBase List > PF 04217903 mesylate

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
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PF 04217903 mesylate Property

storage temp. 
2-8°C
solubility 
DMSO: ≥5mg/mL (warmed)
form 
powder
color 
white to beige
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0263
Product name
PF-04217903
Purity
≥98% (HPLC)
Packaging
5mg
Price
$138
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0263
Product name
PF-04217903
Purity
≥98% (HPLC)
Packaging
25mg
Price
$375
Updated
2025/07/31
Tocris
Product number
4239
Product name
PF04217903mesylate
Purity
≥98%(HPLC)
Packaging
10
Price
$284
Updated
2021/12/16
TRC
Product number
P293990
Product name
PF04217903Mesylate
Packaging
10mg
Price
$195
Updated
2021/12/16
TRC
Product number
P293990
Product name
PF04217903Mesylate
Packaging
100mg
Price
$1540
Updated
2021/12/16
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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

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PF 04217903 mesylate Suppliers

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956906-93-7, PF 04217903 mesylateRelated Search:


  • PF 04217903 mesylate
  • 4-[1-(6-QuinolinylMethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol Methanesulfonate
  • 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 (1:1)
  • PF-04217903.MsOH
  • HBEMHKVWZJTVOC-UHFFFAOYSA-N
  • 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
  • PF-04217903 mesylate/PF04217903 mesylate
  • 956906-93-7
  • C19H16N8OCH4O3S
  • C20H20N8O4S
  • CH4O3SC19H16N8O
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