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NU6102

Catalog No. T28218 CAS 444722-95-6

Synonyms: NU-6102, NU 6102

NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1/cyclinB, CDK2/cyclinA3, CDK1/CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.

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NU6102, CAS 444722-95-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 107.00
10 mg	In stock	$ 156.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 385.00
100 mg	In stock	$ 572.00
1 mL * 10 mM (in DMSO)	In stock	$ 128.00

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Purity: 99.58%

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Description	NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1/cyclinB, CDK2/cyclinA3, CDK1/CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.
Targets&IC50	PDK1:0.8 μM, DYRK1A:0.9 μM, CDK4:1.6 μM, CDK2-CyclinA3:5.4 nM, CDK1-CyclinB:9.5 nM
In vitro	Treatment with NU6102 (0-30 μM; 1-24 hours) induces G2 arrest, inhibition of Rb phosphorylation, and cytotoxicity (LC50 2.6 μM for a 24-hour exposure) in SKUT-1B cells[3]. NU6102 inhibits cell growth and causes cell cycle phase arrest in human breast cancer cell lines, displaying G2/M arrest in asynchronously growing cell lines and G1/S arrest in cells released from serum starvation, and in Xenopus nuclei in a time-dependent manner[3]. Moreover, NU6102 selectively inhibits the growth of CDK2 WT (wild type) compared to KO MEFs (knockout mouse embryo fibroblasts) with a GI50 of 14 μM versus >30 μM[3].
In vivo	The pharmacokinetics of NU6102 are determined in Balb/C mice following i.v. and i.p. administration. Due to the limited solubility of NU6102, the maximum administrable dose is 1 mg/kg i.v. and 10 mg/kg i.p. NU6102 is liberated following either i.p. or i.v. administration of NU6301. After i.v. administration, peak plasma levels of 12 μM NU6102 are observed 5 minutes post-administration, while the peak concentration achieved with the maximum administrable dose of NU6102 i.v. is 0.92 μM. The plasma half-life of NU6102 liberated following NU6301 administration is 42 minutes after i.p. and 10 minutes after i.v. administration[3].

Synonyms	NU-6102, NU 6102
Molecular Weight	402.47
Formula	C18H22N6O3S
CAS No.	444722-95-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL(198.77 mM), Sonication is recommended.

References and Literature

1. Ian R Hardcastle,et al. N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. J Med Chem. 2004 Jul 15;47(15):3710-22. 2. David J Pratt, et al. Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J Med Chem. 2006 Sep 7;49(18):5470-7. 3. Huw D Thomas , et al. Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301. Eur J Cancer. 2011 Sep;47(13):2052-9. 4. Moore NL, Edwards DP, Weigel NL. Cyclin A2 and its associated kinase activity are required for optimal induction of progesterone receptor target genes in breast cancer cells. J Steroid Biochem Mol Biol. 2014 Oct;144 Pt B:471-82. doi: 10.1016/j.jsbmb.2014.09.009. PubMed PMID: 25220500; PubMed Central PMCID: PMC4201666.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library

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Keywords

NU6102 444722-95-6 Cell Cycle/Checkpoint CDK NU-6102 NU 6102 inhibitor inhibit

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