NU2058 | CAS#161058-83-9 | CDK inhibitor

MedKoo Cat#: 406329 | Name: NU2058

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NU2058 is a potent CDK inhibitor that has CDK2 IC(50)=17 microM and CDK1 IC(50)=26 microM.

Chemical Structure

NU2058

CAS#161058-83-9

Theoretical Analysis

MedKoo Cat#: 406329

Name: NU2058

CAS#: 161058-83-9

Chemical Formula: C12H17N5O

Exact Mass: 247.1433

Molecular Weight: 247.30

Elemental Analysis: C, 58.28; H, 6.93; N, 28.32; O, 6.47

Price and Availability

Size	Price	Availability
25mg	USD 200.00	2 Weeks
50mg	USD 300.00	2 Weeks
100mg	USD 550.00	2 Weeks
200mg	USD 850.00	2 Weeks
500mg	USD 1,450.00	2 Weeks
1g	USD 2,150.00

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Related CAS #

No Data

Synonym

NU2058; NU 2058; NU-2058.

IUPAC/Chemical Name

6-(cyclohexylmethoxy)-9H-purin-2-amine

InChi Key

MWGXGTJJAOZBNW-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H17N5O/c13-12-16-10-9(14-7-15-10)11(17-12)18-6-8-4-2-1-3-5-8/h7-8H,1-6H2,(H3,13,14,15,16,17)

SMILES Code

NC1=NC(OCC2CCCCC2)=C3N=CNC3=N1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly.

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1.

In vitro activity:

A panel of AIPC cells was found to be resistant to Casodex-induced growth inhibition, but with the exception of PC3 (GI(50)=38 microM) and CWR22Rv1 (GI(50)=46 microM) showed similar sensitivity to NU2058 (GI(50)=10-17 microM) compared to androgen-sensitive LNCaP cells (GI(50)=15 microM). In LNCaP cells and their Casodex-resistant derivative, LNCaP-cdxR, growth inhibition by NU2058 was accompanied by a concentration-dependent increase in p27 levels, reduced CDK2 activity and pRb phosphorylation, a decrease in early gene expression and G1 cell cycle phase arrest in both cell lines. Reference: Oncogene. 2007 Dec 6;26(55):7611-9. https://pubmed.ncbi.nlm.nih.gov/17599054/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMF	25.0	101.09
	DMSO	32.7	132.16
	DMSO:PBS (pH 7.2) (1:7)	0.1	0.49
	Ethanol	17.5	70.72

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 247.30 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Harrison LR, Ottley CJ, Pearson DG, Roche C, Wedge SR, Dolan ME, Newell DR, Tilby MJ. The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2. Biochem Pharmacol. 2009 May 15;77(10):1586-92. doi: 10.1016/j.bcp.2009.02.018. Epub 2009 Mar 5. PMID: 19426695. 2. Rigas AC, Robson CN, Curtin NJ. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer. Oncogene. 2007 Dec 6;26(55):7611-9. doi: 10.1038/sj.onc.1210586. Epub 2007 Jun 18. PMID: 17599054.

In vitro protocol:

In vivo protocol:

TBD

1: Harrison LR, Ottley CJ, Pearson DG, Roche C, Wedge SR, Dolan ME, Newell DR, Tilby MJ. The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2. Biochem Pharmacol. 2009 May 15;77(10):1586-92. doi: 10.1016/j.bcp.2009.02.018. Epub 2009 Mar 5. PubMed PMID: 19426695.