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  3. NU6102

NU6102 

Cat. No.: HY-15569 Purity: ≥95.0%
Handling Instructions

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).

For research use only. We do not sell to patients.

NU6102 Chemical Structure

NU6102 Chemical Structure

CAS No. : 444722-95-6

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Description

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)[1][2].

IC50 & Target[1][2]

Cdk1/cyclin B

9.5 nM (IC50)

CDK2/cyclin A3

5.4 nM (IC50)

CDK4

1.6 μM (IC50)

DYRK1A

0.9 μM (IC50)

PDK1

0.8 μM (IC50)

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[3].
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[3].
NU6102 selectively inhibits the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GI50 of 14 μM versus >30 μM)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[3]

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).
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

402.47

Formula

C₁₈H₂₂N₆O₃S

CAS No.

444722-95-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: ≥95.0%

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Keywords:

NU6102NU 6102NU-6102CDKCyclin dependent kinaseCDK1CDK2DYRK1APDK1ROCKIIanticancerG2arrestInhibitorinhibitorinhibit

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NU6102
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HY-15569
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