CEP-5214

Details

Stereochemistry	ACHIRAL
Molecular Formula	C28H28N2O3
Molecular Weight	440.5335
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(C)OCC1=CC2=C(C=C1)N(CCCO)C3=C2C4=C(C(=O)NC4)C5=C3CC6=C5C=CC=C6

InChI

InChIKey=MLIFNJABMANKEU-UHFFFAOYSA-N

InChI=1S/C28H28N2O3/c1-16(2)33-15-17-8-9-23-20(12-17)25-22-14-29-28(32)26(22)24-19-7-4-3-6-18(19)13-21(24)27(25)30(23)10-5-11-31/h3-4,6-9,12,16,31H,5,10-11,13-15H2,1-2H3,(H,29,32)

HIDE SMILES / InChI

Molecular Formula	C28H28N2O3
Molecular Weight	440.5335
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

PubMed

Title	Date	PubMed
No data available in table

Patents

Substance Class	Chemical
Record UNII	A3X38AF5BQ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CEP5214

Preferred Name

English

CEP-5214

Code

English

3-(5,6,7,13-TETRAHYDRO-9-((1-METHYLETHOXY)METHYL)-5-OXO-12H-INDENO(2,1-A)PYRROLO(3,4-C)CARBAZOL-12-YL)PROPANOL

Systematic Name

English

5H-INDENO(2,1-A)PYRROLO(3,4-C)CARBAZOL-5-ONE, 6,7,12,13-TETRAHYDRO-12-(3-HYDROXYPROPYL)-9-((1-METHYLETHOXY)METHYL)-

Systematic Name

English

3-(3-HYDROXYPROPYL)-7-((PROPAN-2-YLOXY)METHYL)-3,13-DIAZAHEXACYCLO(14.7.0.0(2,10).0(4,9).0(11,15).0(17,22))TRICOSA-1(16),2(10),4,6,8,11(15),17(22),18,20-NONAEN-14-ONE

Systematic Name

English

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Code System

Code

Type

Description

PUBCHEM

10275001

PRIMARY

MANUFACTURER PRODUCT INFORMATION

CEP-5214

PRIMARY

CEP-5214 is a potent, low-nanomolar pan inhibitor of human VEGF-R tyrosine kinases, displaying IC(50) values of 16, 8, and 4 nM for VEGF-R1/FLT-1, VEGF-R2/KDR, and VEGF-R3/FLT-4, respectively, with cellular activity equivalent to the isolated enzyme activity. Compound 21 exhibited good selectivity against numerous tyrosine and serine/threonine kinases including PKC, Tie2, TrkA, CDK1, p38, JNK, and IRK.

FDA UNII

A3X38AF5BQ

PRIMARY

CAS

402857-39-0

PRIMARY

ChEMBL

CHEMBL150894

PRIMARY

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Related Record

Type

Details


					A3X38AF5BQ

CEP-5214

ACTIVE MOIETY

Comments:

CEP-5214 demonstrates IC(50) values of 18 nM, 12 nM, and 17 nM against human VEGF-R2/KDR kinase, VEGF-R1/FLT-1 kinase, and VEGF-R3/FLT-4 kinase, respectively, in biochemical kinase assays. CEP-5214 inhibited VEGF-stimulated VEGF-R2/KDR autophosphorylation in human umbilical vein endothelial cells (HUVECs) with an IC (50) of approximately 10 nM and demonstrated an equivalent inhibition of murine FLK-1 autophosphorylation in transformed SVR endothelial cells.

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