KPT-185

KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts[1].

Product Specifications

CAS Number

[1333151-73-7]

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-185.html

Purity

99.04

Solubility

DMSO : 50 mg/mL (ultrasonic) |Ethanol : 50 mg/mL (ultrasonic)

Smiles

O=C(OC(C)C)/C=C\N1N=C(C2=CC(C(F)(F)F)=CC(OC)=C2)N=C1

Molecular Formula

C16H16F3N3O3

Molecular Weight

355.31

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]Salas Fragomeni RA, et al. CRM1 and BRAF inhibition synergize and induce tumor regression in BRAF-mutant melanoma. Mol Cancer Ther. 2013 Jul;12 (7) :1171-9.|[4]Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1) -mediated nuclear export has selective anti-leukaemic activityin preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161 (1) :117-27.