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CEP-5214

CAT: 0804-HY-15334Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-15334Size:1 Each
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Description
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].
CAS Number
402857-39-0
UNSPSC
12352005
Target
VEGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/cep-5214.html
Smiles
O=C1NCC2=C1C3=C(CC4=C3C=CC=C4)C(N5CCCO)=C2C6=C5C=CC(COC(C)C)=C6
Molecular Formula
C28H28N2O3
Molecular Weight
440.53
References & Citations
[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
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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Alternative Products

CatalogName
T68039-01Cep-5214
531311SU 5214
B1307-5SU-5214
A17152-50SU 5214 50mg
A17152-100SU 5214 100mg
A17152-25SU 5214 25mg
A17152-200SU 5214 200mg
A17152-10SU 5214 10mg
A17152-5SU 5214 5mg
8108/5CEP

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