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K03861

SIGMA/SML2971 - ≥98% (HPLC)

Synonym: 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

CAS Number: 853299-07-7
Empirical Formula (Hill Notation): C24H26F3N7O2
Molecular Weight: 501.50
MDL Number: MFCD19443769
Linear Formula: C24H26F3N7O2
Product Type: Chemical

Catalog Number PKG Qty. Price Quantity
45-SML2971-5MG 5 mg
$107.00
1/EA
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45-SML2971-25MG 25 mg
$344.00
1/EA
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assay ≥98% (HPLC)
color white to beige
form powder
Quality Level 100 
solubility DMSO: 2 mg/mL, clear
storage temp. −20°C
Biochem/physiol Actions: 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).
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. −20°C
UNSPSC 12352200

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