RGB-286638, free base | 2886

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