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关于此项目
经验公式(希尔记法):
C18H16FN3O2
化学文摘社编号:
分子量:
325.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
Fc1cc(ccc1)Nc2[nH]nc3c2Cc4c3cc(c(c4)OC)OC
InChI
1S/C18H16FN3O2/c1-23-15-7-10-6-14-17(13(10)9-16(15)24-2)21-22-18(14)20-12-5-3-4-11(19)8-12/h3-5,7-9H,6H2,1-2H3,(H2,20,21,22)
InChI key
ZDNURMVOKAERHZ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 10 mg/mL
methanol: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFR Tyrosine Kinase
PDGFR Tyrosine Kinase
Product competes with ATP.
Reversible: yes
Target IC50: 4.2 nM and 45 nM for -β and -α form of PDGFR, respectively
Disclaimer
Toxicity: Harmful (C)
General description
A cell-permeable indenopyrazole compound that displays potent antiproliferative properties in several human tumor cell lines (IC50<33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC50 = 4.2 nM and 45 nM for -β and -α, respectively) and c-Abl (IC50 = 22 nM). Exhibits less activity towards Lck, c-Src, and Fyn (IC50 = 100 nM, 185 nM and 378 nM, respectively) and exhibits little or no inhibition toward VEGFR, HER-2, Cdk′s-1,-2,-4 &-7, bFGFR-1 and EGFR (IC50 = 3.1 µM, >10 µM, >10 µM, 45.8 µM and >100 µM, respectively).
Other Notes
Ho, C.Y., et al. 2005. J. Med. Chem.48, 8163.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
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