RGB-286638, free base

• CAT Number: I004883
• CAS Number: 784210-88-4
• Molecular Formula: C₂₉H₃₅N₇O₄
• Molecular Weight: 545.63
• Purity: ≥95%
• Target: Cyclin-Dependent Kinases
• Solubility: DMSO: ≥ 36 mg/mL
• Storage: Store at -20°C
• IC50: 1 nM/2 nM/3 nM/4 nM/5 nM(cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5) [1]
• IUPAC Name: 1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-ylurea
• InChI: InChI=1S/C29H35N7O4/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38)
• InChIKey: XLSYZSRXVVCHLS-UHFFFAOYSA-N
• SMILES: COCCN1CCN(CC1)CC2=CC=C(C=C2)C3=NNC4=C3C(=O)C5=C4C=CC=C5NC(=O)NN6CCOCC6

RGB-286638 free base（Cat No.:I004883） is a novel cyclin-dependent kinase (CDK) inhibitor that demonstrates potent activity against multiple CDKs. It exhibits IC50 values of 1 nM for cyclin T1-CDK9, 2 nM for cyclin B1-CDK1, 3 nM for cyclin E-CDK2, 4 nM for cyclin D1-CDK4, and 5 nM for cyclin E-CDK3/p35-CDK5. However, it is less potent against cyclin H-CDK7 and cyclin D3-CDK6. The selective inhibition of these CDKs makes RGB-286638 free base a promising candidate for the development of targeted therapies for various diseases, including cancer.

Reference

[1]. Cirstea D, et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.