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PDK1 inhibitor

Catalog Number: EVT-253006

CAS Number: 1001409-50-2

Molecular Formula: C28H22F2N4O4

Molecular Weight: 516.5

The product is for non-human research only. Not for therapeutic or veterinary use.

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Product Introduction

Description

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent with IC50 of 1 nM, displays >3,000-fold selectivity against a panel of 256 kinases; specifically inhibits cellular PDK1 T-loop phosphorylation (Ser-241), inhibits p-RSK S221 in PC-3 cells with EC50 of 300 nM, inhibits colony formation in a subset of cancer cell lines (4 of 10) and primary xenograft tumor lines (9 of 57).

Properties

CAS Number

1001409-50-2

Product Name

PDK1 inhibitor

IUPAC Name

1-[(3,4-difluorophenyl)methyl]-2-oxo-N-[(1R)-2-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)oxy]-1-phenylethyl]pyridine-3-carboxamide

Molecular Formula

C28H22F2N4O4

Molecular Weight

516.5

InChI

InChI=1S/C28H22F2N4O4/c29-21-10-8-17(13-22(21)30)15-34-12-4-7-20(27(34)36)26(35)31-25(18-5-2-1-3-6-18)16-38-19-9-11-23-24(14-19)33-28(37)32-23/h1-14,25H,15-16H2,(H,31,35)(H2,32,33,37)/t25-/m0/s1

InChI Key

GCWCGSPBENFEPE-VWLOTQADSA-N

SMILES

C1=CC=C(C=C1)C(COC2=CC3=C(C=C2)NC(=O)N3)NC(=O)C4=CC=CN(C4=O)CC5=CC(=C(C=C5)F)F

Synonyms

1-[(3,4-difluorophenyl)methyl]-2-oxo-N-[(1R)-2-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)oxy]-1-phenylethyl]pyridine-3-carboxamide

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