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Nanatinostat (TFA)

CAT: 0804-HY-13432ASize: 1 EachDry Ice: NoHazardous: No
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Description
Nanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM) . Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer[1][2][3].
CAS Number
1256448-48-2
Product Name Alternative
CHR-3996 (TFA)
UNSPSC
12352005
Target
Apoptosis; HDAC
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/nanatinostat-tfa.html
Smiles
OC(C(F)(F)F)=O.FC(C=C1)=CC(C=C2)=C1N=C2CN[C@H]3[C@@]4([H])[C@]3([H])CN(C5=NC=C(C(NO)=O)C=N5)C4
Molecular Formula
C22H20F4N6O4
Molecular Weight
508.43
References & Citations
[1]Moffat D, et al. Discovery of 2- (6-{[ (6-fluoroquinolin-2-yl) methyl]amino}bicyclo[3.1.0]hex-3-yl) -N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J Med Chem. 2010 Dec 23;53 (24) :8663-78.|[2]Smith EM, et al. The combination of HDAC and aminopeptidase inhibitors is highly synergistic in myeloma and leads to disruption of the NFκB signalling pathway. Oncotarget. 2015 Jul 10;6 (19) :17314-27.|[3]Banerji U, et al. A phase I pharmacokinetic and pharmacodynamic study of CHR-3996, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. Clin Cancer Res. 2012 May 1;18 (9) :2687-94.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
HDAC; HDAC1; HDAC2; HDAC3; HDAC5; HDAC6

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