PZ0303
PF-04449913 maleate salt
≥98% (HPLC)
别名:
1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate salt, Glasdegib maleate salt
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关于此项目
经验公式（希尔记法）:
C21H22N6O · C4H4O4
化学文摘社编号:
分子量:
490.51
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
InChI
1S/C21H22N6O.C4H4O4/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20;5-3(6)1-2-4(7)8/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28);1-2H,(H,5,6)(H,7,8)/b;2-1-/t16-,19-;/m1./s1
SMILES string
OC(/C=C\C(O)=O)=O.CN1CC[C@@H](NC(NC2=CC=C(C#N)C=C2)=O)C[C@@H]1C3=NC4=CC=CC=C4N3
InChI key
VJCVKWFBWAVYOC-UIXXXISESA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
room temp
Quality Level
Gene Information
human ... SMO(6608)
Biochem/physiol Actions
PF-04449913 (Glasdegib) is an orally bioavailable Hedgehog pathway inhibitor. PF-04449913 acts by binidng Smoothened (Smo) and blocking signal transduction. PF-04449913 has an IC50 of 5 nM in the Gli-Luciferase assay. In a Phase I clinical trial in patients with advanced solid tumors, PF-04449913 caused disease stabilization in 34% of patients.
PF-04449913 maleate salt is also known as 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea. It increases the differentiation of blood cells from hematopoietic precursors of the lymph gland medullary zone. This human Smo inhibitor protein is now under clinical trials to treat myeloid malignancies.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent drosophila hematopoietic progenitor cells.
Giordani G, et al.
Oncotarget, 7(34), 55313-55313 (2016)
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