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NU2058

Cat. No. M5332

NU2058 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

NU2058 is a competitive inhibitor of CDK2 with respect to ATP (Ki value CDK2, 12 3 μM) that binds in the ATP binding pocket in a different orientation from other purine-based inhibitors, including olomoucine and roscovotine. NU2058 is the lead compound in a structure-based drug discovery program to develop more potent and selective CDK inhibitors.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 247.3
Formula C12H17N5O
CAS Number 161058-83-9
Purity >99%
Solubility ≥ 32 mg/mL in DMSO
Storage at -20°C
References

The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2.
Harrison LR, et al. Biochem Pharmacol. 2009 May 15;77(10):1586-92. PMID: 19426695.

Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer.
Rigas AC, et al. Oncogene. 2007 Dec 6;26(55):7611-9. PMID: 17599054.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NU2058 supplier, CDK, inhibitors

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