Description
RGB-286638 is a potent and selective cyclin-dependent kinase (CDK) inhibitor with IC₅₀ values of 1, 2, 3 and 44 nM for CDK9, CDK1, CDK2, and CDK4, respectively. Less potent against cyclin H-CDK7 and cyclin D3-CDK6. It inhibits cell cycle progression in cancer cells by targeting CDKs, and is also found to induce apoptosis. In a range of pre-clinical models of solid and hematological tumors, RGB-286638 treatment results in tumor regression and increased survival.
RGB-286638 is a potent and selective cyclin-dependent kinase (CDK) inhibitor with IC₅₀ values of 1, 2, 3 and 44 nM for CDK9, CDK1, CDK2, and CDK4, respectively. Less potent against cyclin H-CDK7 and cyclin D3-CDK6. It inhibits cell cycle progression in cancer cells by targeting CDKs, and is also found to induce apoptosis. In a range of pre-clinical models of solid and hematological tumors, RGB-286638 treatment results in tumor regression and increased survival.
2886 | RGB-286638, free base DataSheet
Alternate Name/Synonyms: 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
Appearance: Crystalline solid
Formulation: N/A
CAS Number: 784210-88-4
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₉H₃₅N₇O₄
Molecular Weight: 545.63
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO
Handling: Protect from air and light
Country of Origin: USA
Tag Line: A potent and selective cyclin-dependent kinase (CDK) inhibitor
MDL Number: N/A
PubChem CID: 11285002
SMILES: COCCN1CCN(CC1)CC2=CC=C(C=C2)C3=NNC4=C3C(=O)C5=C4C=CC=C5NC(=O)NN6CCOCC6
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)
InChi Key: XLSYZSRXVVCHLS-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |