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AUZ 454

Product Name
AUZ 454
CAS No.
853299-07-7
Chemical Name
AUZ 454
Synonyms
KO3861;K03861;AUZ 454;CS-2904;KO3861 KO-3861;K0-3861;K0 3861;AUZ 454 (K03861);K03861 (AUZ 454);AUZ454,ACHN,Caki-1,cells,K 03861,K-03861,Cyclin dependent kinase,AUZ-454,AUZ 454,Inhibitor,inhibit,CDK,CDK2;1-[4-[(2-Amino-4-pyrimidinyl)oxy]phenyl]-3-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]urea
CBNumber
CB52627352
Molecular Formula
C24H26F3N7O2
Formula Weight
501.5
MOL File
853299-07-7.mol
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AUZ 454 Property

storage temp. 
Store at -20°C
solubility 
≥50.2 mg/mL in DMSO; insoluble in H2O; ≥45.4 mg/mL in EtOH
form 
solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris
Product number
6789
Product name
K03861
Purity
≥98%(HPLC)
Packaging
10
Price
$189
Updated
2021/12/16
Tocris
Product number
6789
Product name
K03861
Purity
≥98%(HPLC)
Packaging
50
Price
$795
Updated
2021/12/16
ChemScene
Product number
CS-5822
Product name
AUZ454
Purity
99.99%
Packaging
2mg
Price
$120
Updated
2021/12/16
ApexBio Technology
Product number
B6042
Product name
K03861
Packaging
5mg
Price
$140
Updated
2021/12/16
ChemScene
Product number
CS-5822
Product name
AUZ454
Purity
99.99%
Packaging
5mg
Price
$180
Updated
2021/12/16
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AUZ 454 Chemical Properties,Usage,Production

Biological Activity

k03861 is a type ii inhibitor of cdk2. the cyclin-dependent kinase holoenzymes contain a catalytic subunit, the cdk, a family of regulatory subunits, and the cyclins. cdks are the catalytic subunits of the mammalian heterodimeric serine/threonine kinases progression, cyclin-dependent kinases (cdks) play important roles in the cell cycle regulation, transcription, and neuronal function. cdks are frequently deregulated in some human tumours. the inhibitors targeted cdk are thought to prevent cell proliferation regulating cyclin-cdk complexes. the central role of cdks in cell cycle regulation makes them a promising target for studying inhibitory molecules that can modify the cell proliferation [1].k03861 is an aminopyrimidine-phenyl urea inhibitor of cdk2. the type ii inhibitor cdk2 cocrystal structure of cdk2 with the inhibitor k03861 revealed a canonical type ii binding mode. the type ii inhibitors could compete with the binding of cyclins. the residues important for the type ii inhibitors may be distant to the atp binding pockets. the crystal structure of this complex may provide a foundation for the cyclin-competitive cdk2 inhibitors [2].

in vitro

K03861 inhibits CDK2 activity by competitively binding to activated cyclins.

target

TargetValue
CDK2(C118L/A144C)
(Cell-free assay)< /td>
9.7 nM(Kd)
CDK2(A144C)
(Cell-free assay)
15.4 nM( Kd)
CDK2(C118L)
(Cell-free assay)
18.6 nM(Kd)
CDK2(WT)
(Cell-free assay)
50 nM(Kd)

storage

Store at -20°C

References

malumbres m, barbacid m. mammalian cyclin-dependent kinases[j]. trends in biochemical sciences, 2005, 30(11): 630-641.alexander l t, mobitz h, drueckes p, et al. type ii inhibitors targeting cdk2[j]. acs chemical biology, 2015, 10(9): 2116-2125.

AUZ 454 Preparation Products And Raw materials

Raw materials

Preparation Products

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AUZ 454 Suppliers

MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Mashilabs (Shanghai) Co.,Ltd.
Tel
19916721580
Fax
QQ:3154870176
Email
mafarm@126.com
Country
China
ProdList
4301
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4566
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
1005
Advantage
55
Shanghai Rechem science Co., Ltd.
Tel
21-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2988
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
7296
Advantage
58
Shanghai SuperLan Chemcial Technique Centre
Tel
021-2022843681 15618226720
Fax
+86-21-51601218
Email
lucy@atkchemical.com
Country
China
ProdList
9952
Advantage
58
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 4009686088
Email
3193328036@qq.com
Country
China
ProdList
29785
Advantage
68
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58

853299-07-7, AUZ 454Related Search:


  • AUZ 454
  • K03861
  • 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea
  • KO3861
  • AUZ 454 (K03861)
  • K0-3861;K0 3861
  • CS-2904
  • Urea, N-[4-[(2-amino-4-pyrimidinyl)oxy]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-
  • K03861 (AUZ 454)
  • AUZ454,ACHN,Caki-1,cells,K 03861,K-03861,Cyclin dependent kinase,AUZ-454,AUZ 454,Inhibitor,inhibit,CDK,CDK2
  • 1-[4-[(2-Amino-4-pyrimidinyl)oxy]phenyl]-3-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]urea
  • KO3861 KO-3861
  • 853299-07-7
  • C24H26F3N7O2