| Identification | Back Directory | [Name]
CEP-5214 | [CAS]
402857-39-0 | [Synonyms]
CEP-5214
MLIFNJABMANKEU-UHFFFAOYSA-N
5H-Indeno[2,1-a]pyrrolo[3,4-c]carbazol-5-one, 6,7,12,13-tetrahydro-12-(3-hydroxypropyl)-9-[(1-methylethoxy)methyl]- | [Molecular Formula]
C28H28N2O3 | [MOL File]
402857-39-0.mol | [Molecular Weight]
440.53 |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[1] A New Class of Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Structure-Activity Relationships for a Series of 9-Alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the Identification of CEP-5214 and Its Dimethylglycine Ester Prodrug Clinical Candidate CEP-7055 |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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