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SML2971

Sigma-Aldrich

K03861

≥98% (HPLC)

Synonyme(s) :

1-[4-(2-Aminopyrimidin-4-yloxy)phenyl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-trifluoromethylphenyl]urea, AUZ 454, AUZ-454, AUZ454, CCG 269702, CCG-269702, CCG269702, K 03861, K-03861, N-[4-[(2-Amino-4-pyrimidinyl)oxy]phenyl]-N′-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]urea

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About This Item

Formule empirique (notation de Hill):
C24H26F3N7O2
Numéro CAS:
853299-07-7
Poids moléculaire :
501.50
Numéro MDL:
MFCD19443769
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

−20°C

InChI

1S/C24H26F3N7O2/c1-33-10-12-34(13-11-33)15-16-2-3-18(14-20(16)24(25,26)27)31-23(35)30-17-4-6-19(7-5-17)36-21-8-9-29-22(28)32-21/h2-9,14H,10-13,15H2,1H3,(H2,28,29,32)(H2,30,31,35)

Clé InChI

PWDLXPJQFNVTNL-UHFFFAOYSA-N

Actions biochimiques/physiologiques

K03861 is an ATP site-binding, cyclin-competitive, type II CDK2 inhibitor that selectively targets and locks the kinase in its inactive DFG-out conformation (CDK2 Kd = 50 nM, DFG-out stabilizing CDK2-C118L/A144C mutant Kd = 9.7 nM without vs. 134.1 nM with bound cycB; CDK2-C118L/A144C-cycA IC50 = 0.8 μM), rendering it incompatible for cyclin bining. K03861 selectively inhibits CDK2-C118L/A144C over CycA-bound wt CDK2 by in vitro kinase assay (IC50 = 0.8 vs. >10 μM) and inhibits the proliferation of immortalized multipotent otic progenitor (iMOP) murine cell line (by 81% and 92%, resepectively, at 0.1 and 1.0 μM).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Atsushi Okuma et al.
Nature communications, 8(1), 2050-2050 (2017-12-14)
p16Ink4a and p21Cip1/Waf1 act as tumour suppressors through induction of cellular senescence. However, senescence-independent roles of these CDK inhibitors are not well understood. Here, we report an unexpected function of p16Ink4 and p21Cip1/Waf1, namely, tumour promotion through chemotaxis. In monocytic
Carrow I Wells et al.
Nature communications, 11(1), 2743-2743 (2020-06-04)
Concerted multidisciplinary efforts have led to the development of Cyclin-Dependent Kinase inhibitors (CDKi's) as small molecule drugs and chemical probes of intracellular CDK function. However, conflicting data has been reported on the inhibitory potency of CDKi's and a systematic characterization
Zhichao Song et al.
Stem cell reports, 9(5), 1516-1529 (2017-10-17)
Loss of spiral ganglion neurons (SGNs) significantly contributes to hearing loss. Otic progenitor cell transplantation is a potential strategy to replace lost SGNs. Understanding how key transcription factors promote SGN differentiation in otic progenitors accelerates efforts for replacement therapies. A
Leila T Alexander et al.
ACS chemical biology, 10(9), 2116-2125 (2015-07-15)
Kinases can switch between active and inactive conformations of the ATP/Mg(2+) binding motif DFG, which has been explored for the development of type I or type II inhibitors. However, factors modulating DFG conformations remain poorly understood. We chose CDK2 as
Manman Wang et al.
Cell & bioscience, 10, 57-57 (2020-04-24)
Forced polyploidization is an effective strategy for acute megakaryoblastic leukemia (AMKL) therapy and factors controlling polyploidization are potential targets for drug development. Although bone morphology protein 2-inducible kinase (BMP2K) has been implied to be a potential target for fasudil, a
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