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CDK2 inhibitor NU6301 Small Molecule (Tool Compound)

Info

Catalogue Number 152754
Antigen/Gene or Protein Targets Cyclin dependent kinase 2 (CDK2)
Type Inhibitor
Molecular Formula C18H21N6O4S1(CH3)- K+
lUPAC N-Acetyl-4-(6-cyclohexylmethoxy-9H-purin-2-ylamino)-benzenesulfonamide potassium salt
In vivo applications The prodrug NU6301 rapidly generated NU6102 in vitro in mouse plasma, and tumour NU6102 levels in vivo consistent with activity in vitro. Eight or 12 hourly dosing of 120 mg/kg NU6301 for 10 days was well tolerated in SKUT-1B tumour-bearing mice and inhibited Rb phosphorylation in tumour tissue. Two (8 hourly dosing) and 3 (12 hourly dosing) day tumour growth delay was observed (p=0.04 and p=0.007, respectively) following NU6301 administration.
In vitro applications NU6102 selectively inhibited the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GI₅₀ (concentration required to inhibit cell growth by 50%) 14 μM versus >30 μM), and was more growth-inhibitory in p53 mutant or null versus p53 WT cells (p=0.02), and in Rb (retinoblastoma protein) WT SKUT-1B versus SKUT 1 Rb deficient cells (p=0.01). In SKUT-1B cells NU6102 induced a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC₅₀ 2.6 μM for a 24h exposure).
Research Area Cancer, Cell Cycle
Relevance The CDK2 inhibitor NU6301 is a water soluble prodrug of NU6102, a potent CDK1/cyclin B and CDK2/cyclin A3 inhibitor (IC50 values are 9.5 and 5.4 nM for CDK1/cyclin B and CDK2/cyclin A3 respectively). CDK2 is a member of a family of serine/threonine protein kinases that participate in cell cycle regulation. CDK2 is the catalytic subunit of the cyclin-dependent protein kinase complex, which regulates progression through the cell cycle. Activity of this protein is especially critical during the G1 to S phase transition. CDK2 associates with and regulated by other subunits of the complex including cyclin A or E, CDK inhibitor p21Cip1 (CDKN1A), and p27Kip1 (CDKN1B).

References: 1 entry

Thomas et al. 2011. Eur J Cancer. 47(13):2052-9. PMID: 21570822.


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References: 1 entry

Thomas et al. 2011. Eur J Cancer. 47(13):2052-9. PMID: 21570822.


Add a reference

References: 1 entry

Thomas et al. 2011. Eur J Cancer. 47(13):2052-9. PMID: 21570822.


Add a reference


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