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About This Item
Empirical Formula (Hill Notation):
C18H14F2N4O
CAS Number:
Molecular Weight:
340.33
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
room temp
SMILES string
FC1=C(C2=C(OC=N2)C(C=C3)=CN4C3=NN=C4C(C)C)C=C(F)C=C1
InChI
1S/C18H14F2N4O/c1-10(2)18-23-22-15-6-3-11(8-24(15)18)17-16(21-9-25-17)13-7-12(19)4-5-14(13)20/h3-10H,1-2H3
InChI key
UACOXBQBNWQWOK-UHFFFAOYSA-N
Biochem/physiol Actions
CP-863187 is a potent p38α (p38α) inhibitor (IC50 = 5.8 nM) with 44-fold selectivity over p38β (p38β) and no inhibitory potency against p38γ (p38γ) and p38δ (p38δ) isoforms. CP-863187 effectively inhibits LPS-stimulated cellular TNF-α production in vitro (IC50 = 259 and 25 nM, using human whole blood and isolated mononuclear cells, respectively) and in rats in vivo (ED50 = 0.3 mg/kg p.o.) with good pharmacokinetic profile and oral availability (F = 87%/dog, 40%/monkey, 30%/rat with 5 mg/kg oral dosage; F = 66%/rat with 50 mg/kg oral dosage).
CP-863187 is a potent p38α (p38α) inhibitor.
Legal Information
Sold for research purposes under agreement from Pfizer Inc.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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