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KPT-185

Chemical Structure : KPT-185

CAS No.: 1333151-73-7

KPT-185 (KPT185)

Catalog No.: PC-49221Not For Human Use, Lab Use Only.

KPT-185 (KPT185) is a potent, selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein, shows antileukemic activity in vitro and in vivo in acute myeloid leukemia (AML).

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Biological Activity

KPT-185 (KPT185) is a potent, selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein, shows antileukemic activity in vitro and in vivo in acute myeloid leukemia (AML).
KPT-185 inhibits a panel of AML cell lines proliferation (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1) with IC50 of 100-500 nM.
KPT-185 decreases CRM1 protein level and accumulates CRM1 cargo proteins in the nucleus.
KPT-185 induces differentiation of AML cell lines.

Physicochemical Properties

M.Wt 355.317
Formula C16H16F3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2Z-propenoic acid, 1-methylethyl ester

References

1. Ranganathan P, et al. Blood. 2012 Aug 30;120(9):1765-73.

2. Zhang K, et al. Exp Hematol. 2013 Jan;41(1):67-78.e4.

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