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eIF4A3-IN-1q

Chemical Structure : eIF4A3-IN-1q

CAS No.: 2132392-89-1

eIF4A3-IN-1q

Catalog No.: PC-60161Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 645.861
Formula C29H21BrClF3N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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