402857-39-0
Chemical Structure
CEP-5214
- CAS No.: 402857-39-0
- Formula:C28H28N2O3
- Molecular Weight:440.53
IUPAC Name: 12-(3-hydroxypropyl)-9-(isopropoxymethyl)-6,7,12,13-tetrahydro-5H-indeno[2,1-a]pyrrolo[3,4-c]carbazol-5-one
InChIKey: MLIFNJABMANKEU-UHFFFAOYSA-N
SMILES: O=C1NCC2=C1C3=C(CC4=C3C=CC=C4)C(N5CCCO)=C2C6=C5C=CC(COC(C)C)=C6
Biological Activity: CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability[1].
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CEP-5214 | CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability. | |||||||||||||||||||||
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