KPT-276

PKT-276, an analogue of PKT-185, is an oral bioavailable and selective inhibitor of nuclear output (SINE) . PKT-276 is also a CRM1 antagonist that irreversibly binds to and blocks the function of CRM1[1].

Product Specifications

CAS Number

[1421919-75-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

CRM1

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/kpt-276.html

Concentration

10mM

Purity

99.94

Solubility

DMSO : 20 mg/mL (ultrasonic)

Smiles

O=C(N1CC(F)(F)C1)/C=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2

Molecular Formula

C16H10F8N4O

Molecular Weight

426.26

Precautions

H302, H315, H319, H335

References & Citations

[1]Ranganathan P, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood. 2012 Aug 30;120 (9) :1765-73.|[2]Zhang K, et al. Novel selective inhibitors of nuclear export CRM1 antagonists for therapy in mantle cell lymphoma. Exp Hematol. 2013 Jan;41 (1) :67-78.e4.|[3]Schmidt J, et al. Genome-wide studies in multiple myeloma identify XPO1/CRM1 as a critical target validated using the selective nuclear export inhibitor KPT-276. Leukemia. 2013 Dec;27 (12) :2357-65.