eIF4A3-IN-1q( —— )

Catalog No. M13396 CAS No. 2132392-89-1

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Product Name

eIF4A3-IN-1q
Note

Research use only, not for human use.
Brief Description

A potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM.
Description

A potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM; displays no activity against eIF4A1, eIF4A2, BRR2 and DHX29 (IC50>100 uM); upregulates SC35 1.6 kb mRNA expression by 8-fold at 3 uM and 20-fold at 10 uM, potently inhibit cell growth in HCT-116 cells (GI50=1.18 uM) ; shows antitumor efficacy and promising PK profiles in vivo, without severe body weight loss.
In Vitro

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In Vivo

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Synonyms

——
Pathway

Nuclear Receptor/Transcription Factor
Target

eIF
Recptor

eIF
Research Area

——
Indication

——

CAS Number

2132392-89-1
Formula Weight

645.861
Molecular Formula

C29H21BrClF3N4O3
Purity

>98% (HPLC)
Solubility

——
SMILES

C1CN(C(CN1C(=O)C2=CN(C(=O)C(=C2)C(F)(F)F)C3=CC=CC=C3)C4=CC=C(C=C4)Cl)C(=O)C5=NC=C(C=C5)Br
Chemical Name

(S)-5-(4-(5-bromopicolinoyl)-3-(4-chlorophenyl)piperazine-1-carbonyl)-1-phenyl-3-(trifluoromethyl)pyridin-2(1H)-one

1. Mizojiri R, et al. ACS Med Chem Lett. 2017 Sep 8;8(10):1077-1082.

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