Nanatinostat

Nanatinostat (CHR-3996) 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 has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM) . Nanatinostat induces apoptosis in myeloma cells. Nanatinostat has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer[1][2][3].

Product Specifications

CAS Number

[1256448-47-1]

Product Name Alternative

CHR-3996

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.html

Purity

99.67

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

C20H19FN6O2

Molecular Weight

394.40

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.