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CHR-3996

Chemical Structure : CHR-3996

CAS No.: 1256448-47-1

CHR-3996 (Nanatinostat;CHR3996;VRx-3996;Tractinostat)

Catalog No.: PC-36094Not For Human Use, Lab Use Only.

CHR-3996 (Nanatinostat, VRx-3996, CHR3996, Tractinostat) is a potent, class I-selective, orally active HDAC inhibitor with IC50 of 3-7 nM for HDAC1/2/3.

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Biological Activity

CHR-3996 (Nanatinostat, VRx-3996, CHR3996, Tractinostat) is a potent, class I-selective, orally active HDAC inhibitor with IC50 of 3-7 nM for HDAC1/2/3.
CHR-3996 displays little to no activity against HDAC5 and HDAC6 (IC50=200-2000 nM).
CHR-3996 demonstrates growth inhibition of HCT116 cells with GI50 of 72 nM, shows efficacy in human tumor xenograft and exhibits good activity in combination with other anticancer agents.

Physicochemical Properties

M.Wt 394.41
Formula C20H19FN6O2
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

2-[(1R,5S,6s)-6-{[(6-fluoroquinolin-2-yl)methyl]amino}-3-azabicyclo[3.1.0]hexan-3-yl]-N-hydroxypyrimidine-5-carboxamide

References

1. Moffat D, et al. J Med Chem. 2010 Dec 23;53(24):8663-78.

2. Banerji U, et al. Clin Cancer Res. 2012 May 1;18(9):2687-94.

3. Smith EM, et al. Oncotarget. 2015 Jul 10;6(19):17314-27.

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