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KPT-185

CAT: 0804-HY-15611-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15611-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported