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经验公式(希尔记法):
C30H33N3O5S
化学文摘社编号:
分子量:
547.67
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
S1c2c(cccc2C5=CC(=O)C=C(O5)N6CCOCC6)Cc3c1ccc(c3)NC(=O)CN4C[C@H](O[C@H](C4)C)C
InChI
1S/C30H33N3O5S/c1-19-16-32(17-20(2)37-19)18-28(35)31-23-6-7-27-22(13-23)12-21-4-3-5-25(30(21)39-27)26-14-24(34)15-29(38-26)33-8-10-36-11-9-33/h3-7,13-15,19-20H,8-12,16-18H2,1-2H3,(H,31,35)/t19-,20+
InChI key
SCELLOWTHJGVIC-BGYRXZFFSA-N
assay
≥98% (HPLC)
form
solid
potency
6.3 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light beige
solubility
DMSO: 50 mg/mL
Quality Level
General description
A cell permeable thioxanthene based compound that acts as a highly potent inhibitor of Ataxia telangiectasia mutate (ATM) kinase inhibitor (IC50 = 6.3 nM). Displays about 270 and 1600-fold greater selectivity over DNA-PK and ATR kinase (IC50 = 1.7 and >10 µM, respectively). Has only a trivial effect on 229 protein kinases when screened in a panel at 1 µM level. Shown to block Ser15 phosphorylation of p53 and basal and radiation-induced Ser473 phosphorylation of Akt in glioma cells. Blocks radiation-induced DNA damage response and radiosensitizes human glioma cells (U87 and U1242) and mouse glioma stem cells and inhibits glioma cell migration, invasion, and growth. Also radiosensitizes orthotopic glioma xenografts and significantly extends the survival of mice.
ATM kinase inhibitor, KU60019, is a cell permeable, potent inhibitor of ATM kinase inhibitor (IC₅₀ = 6.3 nM). Has 270 & 1600-fold higher selectivity over DNA-PK and ATR kinase.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
ATM
ATM
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Biddlestone-Thorpe, L., et al. 2013. Clin. Cancer Res.19, 3189.
Golding, S., et al. 2009. Mol. Cancer Ther.8, 2894.
Golding, S., et al. 2009. Mol. Cancer Ther.8, 2894.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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