NU2058
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MedKoo CAT#: 406329

CAS#: 161058-83-9

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

Chemical Structure

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NU2058
CAS# 161058-83-9
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406329
Name: NU2058
CAS#: 161058-83-9
Chemical Formula: C12H17N5O
Exact Mass: 247.14
Molecular Weight: 247.302
Elemental Analysis: C, 58.28; H, 6.93; N, 28.32; O, 6.47

Price and Availability

Size Price Availability Quantity
25mg USD 200 2 Weeks
50mg USD 300 2 Weeks
100mg USD 550 2 Weeks
200mg USD 850 2 Weeks
500mg USD 1450 2 Weeks
1g USD 2150
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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

More Info:         

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. 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

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.

Recalculate based on batch purity %
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: 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 vivo protocol: TBD

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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.