Cas No.: | 161058-83-9 |
Synonyms: | NU 2058,NU-2058,NU2058 |
SMILES: | C1(COC2N=C(N)N=C3C=2N=CN3)CCCCC1 |
Formula: | C12H17N5O |
M.Wt: | 247.3 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1. |
Target: | CDK2:17 μM (IC50) CDK1:26 μM (IC50) |
In Vitro: | 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. |
References: | [1]. Rigas AC, et al. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer. Oncogene. 2007 Dec 6;26(55):7611-7619. |