NU6102

NU6102 is a potent CDK1 and CDK2 inhibitor with IC50s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. NU6102 shows selectivity for CDK1/CDK2 over CDK4 (IC50 of 1.6 μM), DYRK1A (IC50 of 0.9 μM), PDK1 (IC50 of 0.8 μM) and ROCKII (IC50 of 0.6 μM).

Product information

CAS Number: 444722-95-6

Molecular Weight: 402.47

Formula: C18H22N6O3S

Chemical Name: 4-{[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino}benzene-1-sulfonamide

Smiles: NS(=O)(=O)C1C=CC(=CC=1)NC1N=C2N=CNC2=C(N=1)OCC1CCCCC1

InChiKey: OWXORKPNCHJYOF-UHFFFAOYSA-N

InChi: InChI=1S/C18H22N6O3S/c19-28(25,26)14-8-6-13(7-9-14)22-18-23-16-15(20-11-21-16)17(24-18)27-10-12-4-2-1-3-5-12/h6-9,11-12H,1-5,10H2,(H2,19,25,26)(H2,20,21,22,23,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

NU6102 (0-30 μM; 1-24 hours; SKUT 1B cells) treatment induces a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC50 2.6 μM for a 24 h exposure) in SKUT-1B cells. NU6102 inhibits cell growth and causes cell cycle phase arrest in human breast cancer cell lines, G2/M arrest in asynchronously growing cell lines and G1/S arrest in cells released from serum starvation, and in Xenopus nuclei in a timedependent manner. NU6102 selectively inhibits the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GI50 of 14 μM versus >30 μM).

In Vivo:

The pharmacokinetics of NU6102 is determined following i.v. and i.p. administration in Balb/C mice. The limited solubility of NU6102 meant 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, and following i.v. administration peak plasma levels of 12 μM NU6102 is observed 5 min post administration, whereas following administration of the maximum administrable dose of NU6102 i.v. the peak concentration achieved is 0.92 μM. The plasma half-life of NU6102 liberated following administration of NU6301 is 42 min following i.p. and 10 min following i.v. administration.

Products are for research use only. Not for human use.