ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >DNA damage >ATM / ATR inhibitor >KU-60019

KU-60019

KU-60019 Suppliers list
Company Name: Capot Chemical Co.,Ltd.
Tel: +86-571-85586718
Email: sales@capotchem.com
Products Intro: Product Name:KU-60019
CAS:925701-49-1
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: ATK CHEMICAL COMPANY LIMITED
Tel: +86 21 5161 9050/ 5187 7795
Email: ivan@atkchemical.com
Products Intro: Product Name:KU-60019
CAS:925701-49-1
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
Company Name: career henan chemical co
Tel: +86-371-86658258
Email: sales@coreychem.com
Products Intro: Product Name:KU-60019
CAS: 925701-49-1
Purity:95%~99% Package:1ASSAYS;1USD
Company Name: Hubei xin bonus chemical co. LTD
Tel: 86-13657291602
Email: linda@hubeijusheng.com
Products Intro: Product Name:KU-60019
CAS:925701-49-1
Purity:0.99 Package:5KG;1KG
Company Name: CONIER CHEM AND PHARMA LIMITED
Tel: 86-18523575427
Email: sales@conier.com
Products Intro: Product Name:ku-60019
CAS:925701-49-1
Purity:0.99 Package:1kg

Lastest Price from KU-60019 manufacturers

  • KU-60019
  • US $1.00 / ASSAYS
  • 2019-09-06
  • CAS: 925701-49-1
  • Min. Order: 1ASSAYS
  • Purity: 95%~99%
  • Supply Ability: per week:100kg
KU-60019 Basic information
Description Features In vitro In vivo
Product Name:KU-60019
Synonyms:KU-60019;(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide;2-((2S,6R)-2,6-dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl)acetamide;KU-60019 (2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide;KU-60019, 925701-49-1;KU-60019;KU60019;KU 60019;2-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-N-[5-(6-morpholin-4-yl-4-oxopyran-2-yl)-9H-thioxanthen-2-yl]acetamide;CS-444
CAS:925701-49-1
MF:C30H33N3O5S
MW:547.66512
EINECS:
Product Categories:Inhibitors
Mol File:925701-49-1.mol
KU-60019 Structure
KU-60019 Chemical Properties
density 1.314
storage temp. -20°C
form powder
color white to beige
Safety Information
MSDS Information
KU-60019 Usage And Synthesis
DescriptionKU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.
FeaturesImproved analog of KU-55933, and is more effective at blocking ATM-mediated DDR events.
In vitroCompared to KU-55933, KU-60019 is an improved more water-soluble inhibitor of the ATM kinase, while displaying similar target selectivity. KU-60019 has little activity against DNA-PKcs and ATR with IC50 values of 1.7 μM and >10 μM, respectively, as well as 229 other protein kinases such as PI3K, mTOR and mTOR/FKBP12. KU-60019 displays 3- to 10-fold more potency than KU-55933 at blocking radiation-induced phosphorylation of key ATM protein targets such as p53, γ-H2AX, and CHK2, in human glioma U87 and U1242 cells, as 1 μM of KU-60019 significantly induces >70% decrease of p53 (S15) phosphorylation to which extent ~10 μM of KU-55933 is required to achieve. KU-60019 effectively radiosensitizes human glioma cells with dose-enhancement ratio of 1.7 and 4.4 at 1 μM and 10 μM, respectively, and also radiosensitizes the normal fibroblasts but not the A-T fibroblasts. KU-60019 treatment (3 μM) blocks basal and insulin-induced AKT S473 phosphorylation by 70% and ~50%, respectively, and completely reduces radiation-induced AKT phosphorylation below the level of control. The effect of KU-60019 on AKT S473 phosphorylation can be seen in glioma cell lines and normal fibroblasts but not in A-T (h-TERT) cells, and can be significantly blocked by phosphatase inhibitor okadaic acid, suggesting a critical role of ATM kinase in regulating AKT phosphorylation via unknown phosphatase. Consistent with the inhibition of prosurvival AKT signaling, KU-60019 at 3 μM significantly inhibits migration and invasion of human glioma U87 cells by >70% and ~60%, respectively, as well as U1242 cells by >50% and ~60% respectively.
In vivoIn orthotopic glioma U1242/luc-GFP xenograft models, the combination of KU-60019 and radiation significantly increases survival of mice than KU-60019 alone, radiation alone, or no treatment. In addition, p53-mutant gliomas is much more sensitive to KU-60019 radiosensitization than wild-type glioma.
KU-60019 Preparation Products And Raw materials
Tag:KU-60019(925701-49-1) Related Product Information
NU7441 (KU-57788) KU-55933 (ATM Kinase Inhibitor) Selumetinib VE-821 N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide Olaparib