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NU2058

Cat. No. M5332
NU2058 Structure
Synonym:

NU-2058; O6-(Cyclohexylmethyl)guanine

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 95  USD95 In stock
50mg USD 245  USD245 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 247.3
Formula C12H17N5O
CAS Number 161058-83-9
Solubility (25°C) ≥ 32 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Harrison LR, et al. Biochem Pharmacol. The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2.

[2] Rigas AC, et al. Oncogene. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer.

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  Catalog
Abmole Inhibitor Catalog




Keywords: NU2058, NU-2058; O6-(Cyclohexylmethyl)guanine supplier, CDK, inhibitors, activators


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