NU-6102

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 CDK1 和 CDK2 抑制剂，对 CDK1/cyclinB 和 CDK2/cyclinA3 的 IC50 分别为 9.5 nM 和 5.4 nM。

A potent CDK1 and CDK2 inhibitor with IC50 of 9.5 nM and 5.4 nM against CDK1/cyclinB and CDK2/cyclinA3 respectively; exhibits synergistic growth inhibition, and enhanced cytotoxicity in HT29 cells in vitro and HT29 tumour growth inhibition in vivo combined with Pictilisib; induces G2 arrest, inhibition of Rb phosphorylation and cytotoxicity in SKUT-1B cells (LC50=2.6 uM, for a 24h exposure).

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).Cell Cycle Analysis Cell Line:SKUT 1B cells Concentration:0 μM, 3 μM, 10 μM, and 30 μM Incubation Time:1 hours, 3 hours, 6 hours, and 24 hours Result:Induced a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC50 2.6 μM for a 24 h exposure).

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.

NU6102 | NU 6102

Angiogenesis

CDK

CDK

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444722-95-6

402.5

C18H22N6O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (248.47 mM)

O=S(C1=CC=C(NC2=NC(OCC3CCCCC3)=C4N=CNC4=N2)C=C1)(N)=O

N-((3R,6S,9S,12R)-6-ethyl-9-(3-guanidinopropyl)-12-methyl-2,5,8,11-tetraoxo-3-phenyl-1,4,7,10-tetraazacyclohexadecan-12-yl)isobutyramide

(-20℃)

With Ice Pack

≥ 2 years