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
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
N-Bromosuccinimide Price
- Product number
- 6789
- Product name
- K03861
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $189
- Updated
- 2021/12/16
- Product number
- 6789
- Product name
- K03861
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $795
- Updated
- 2021/12/16
- Product number
- CS-5822
- Product name
- AUZ454
- Purity
- 99.99%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-5822
- Product name
- AUZ454
- Purity
- 99.99%
- Packaging
- 25mg
- Price
- $648
- Updated
- 2021/12/16
- Product number
- CS-5822
- Product name
- AUZ454
- Purity
- 99.99%
- Packaging
- 10mg
- Price
- $312
- Updated
- 2021/12/16
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
Target | Value |
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
AUZ 454 Suppliers
- Tel
- 19916721580
- Fax
- QQ:3154870176
- mafarm@126.com
- Country
- China
- ProdList
- 4295
- Advantage
- 58
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- 021-52996696,15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4574
- Advantage
- 55
- Tel
- 021-61350663 13052117465
- Fax
- 021-61350662
- sales@zehanbiopharma.com
- Country
- China
- ProdList
- 1005
- Advantage
- 55
- Tel
- 21-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2990
- Advantage
- 58
- Tel
- 021-QQ:65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 7298
- Advantage
- 58
- Tel
- 021-2022843681 15618226720
- Fax
- +86-21-51601218
- lucy@atkchemical.com
- Country
- China
- ProdList
- 9952
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29764
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- 010-60605840 18892239720
- Fax
- 010-60605840
- psaitong@jm-bio.com
- Country
- China
- ProdList
- 12306
- Advantage
- 58
- Tel
- 028-64971018 18108168130
- Fax
- 86 028-64971018
- Country
- China
- ProdList
- 1781
- Advantage
- 55
- Tel
- 17317130613
- Fax
- QQ3358272972
- 3358272972@qq.com
- Country
- China
- ProdList
- 3254
- Advantage
- 58
- Tel
- 028-85157043 15882256948
- 676046971@qq.com
- Country
- China
- ProdList
- 4398
- Advantage
- 58
- Tel
- 15911056312
- liming@bio-fount.com
- Country
- China
- ProdList
- 9729
- Advantage
- 58
- Tel
- 020-31155029 18902330969
- Fax
- 020-31155029
- sales@tomums.cn
- Country
- China
- ProdList
- 4696
- Advantage
- 58
- Tel
- 0512-65816829 18662214788
- Fax
- 0512-65816829
- info@rovathin.com.cn
- Country
- China
- ProdList
- 9663
- Advantage
- 58
- Tel
- +1-2135480471 +1-2135480471
- sales@sarms4muscle.com
- Country
- China
- ProdList
- 10473
- Advantage
- 58
- Tel
- 0512-0512-13601744364 13601744364
- chemsharker@126.com
- Country
- China
- ProdList
- 927
- Advantage
- 58
- Tel
- 021-58447131 13564518121
- sales@dcchemicals.com
- Country
- China
- ProdList
- 9409
- Advantage
- 58
- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3600
- Advantage
- 58
- Tel
- 63313187 15358055255
- Fax
- QQ:63313187
- 63313187@qq.com
- Country
- China
- ProdList
- 1987
- Advantage
- 58
- Tel
- 021-61998551 13122364865
- sale1@shzysw.net
- Country
- China
- ProdList
- 9772
- Advantage
- 58
- Tel
- 021-38015121 15000105423
- wulan@absin.cn
- Country
- China
- ProdList
- 24731
- Advantage
- 58
- Tel
- 88888888888
- hongquchem@qq.com
- Country
- China
- ProdList
- 5132
- Advantage
- 58
- Tel
- 15869524721
- 3525679403@qq.com
- Country
- China
- ProdList
- 4322
- Advantage
- 58
- Tel
- 15342225168
- yutianchun2007@126.com
- Country
- China
- ProdList
- 10003
- Advantage
- 58
- Tel
- 021-69568360 18916172912
- order@med-bio.cn
- Country
- China
- ProdList
- 8140
- Advantage
- 58
- Tel
- 021-58432009 400-005-6266
- Fax
- 021-58436166
- marketing@energy-chemical.com
- Country
- China
- ProdList
- 44918
- Advantage
- 58
- Tel
- 021-51816796-820 13611835272
- Fax
- 021-5161 3951
- sales2@sunwaypharm.com
- Country
- China
- ProdList
- 44458
- Advantage
- 58
- Tel
- 0371-0371-55153829 18003835034
- Fax
- 18003835034(微信)
- 2853979819@qq.com
- Country
- China
- ProdList
- 9734
- Advantage
- 58
- Tel
- 18964309092 18964309092
- 2769493375@qq.com
- Country
- China
- ProdList
- 2634
- Advantage
- 58
- Tel
- 18051384581
- sales@chemhifuture.com
- Country
- China
- ProdList
- 3023
- Advantage
- 58
- Tel
- 010-60605840 15801484223;
- psaitong@jm-bio.com
- Country
- China
- ProdList
- 29774
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- 2625930290@qq.com
- Country
- China
- ProdList
- 6973
- Advantage
- 58
- Tel
- 400-1647117 13681763483
- product02@bidepharm.com
- Country
- China
- ProdList
- 62075
- Advantage
- 58
- Tel
- 13549236410
- sales@invivochem.cn
- Country
- China
- ProdList
- 6753
- Advantage
- 58
- Tel
- 17771424646
- shoubull@126.com
- Country
- China
- ProdList
- 973
- Advantage
- 58
- Tel
- 4008200310
- marketing@tsbiochem.com
- Country
- China
- ProdList
- 24644
- Advantage
- 58
- Tel
- 025-58851786 17714337195
- sales@tybiochem.com
- Country
- China
- ProdList
- 6829
- Advantage
- 58
- Tel
- 021-54306202 18917919676
- info@hanhongsci.com
- Country
- China
- ProdList
- 29979
- Advantage
- 58
- Tel
- 021-50795510 4000665055
- syeu@accelachem.com
- Country
- China
- ProdList
- 11710
- Advantage
- 58
- Tel
- 021-59167510 18117107507
- vip@med-life.cn
- Country
- China
- ProdList
- 4997
- Advantage
- 58
- Tel
- +86-18521732826
- market@aladdin-e.com
- Country
- China
- ProdList
- 48461
- Advantage
- 58
- Tel
- 18024082417
- market@ubiochem.com
- Country
- China
- ProdList
- 9266
- Advantage
- 58
- Tel
- +undefined-21-51877795
- Fax
- +86 21 5161 9052/ 5187 7796
- ivan@atkchemical.com
- Country
- China
- ProdList
- 32956
- Advantage
- 60
- Tel
- +8613817748580
- Fax
- 021-50175322
- cooperation@kean-chem.com
- Country
- China
- ProdList
- 40066
- Advantage
- 58
- Tel
- +86-371-86557731 +86-13613820652
- Fax
- 86-0371-86557731
- info@fdachem.com
- Country
- China
- ProdList
- 20274
- Advantage
- 58
- Tel
- +undefined18051384581
- sales@chemhifuture.com
- Country
- China
- ProdList
- 3135
- Advantage
- 58
- Tel
- --
- Fax
- --
- info@zzsrm.com
- Country
- CHINA
- ProdList
- 6650
- Advantage
- 58
- Tel
- --
- Fax
- --
- shizezjp@163.com
- Country
- CHINA
- ProdList
- 6174
- Advantage
- 58