KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM. A study demonstrated striking in vivo activity of KPT-330 against T-ALL and AML cells, with little toxicity to normal murine haematopoietic cells.
|Cell lines||MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines|
|Preparation method||Culturing cell lines in RPMI 1640 medium, supplemented with 10% fetal bovine serum and penicillin/streptomycin.Using cell Titer Glo assay to assess cell viability upon treatment with either dimethyl sulfoxide (DMSO) or KPT-330. Plating cells at a density of 10 000 cells per well in a 96-well plate and incubating them with DMSO or increasing concentrations of KPT-330. After 72 h exposure to KPT-330 ,mearsuring the cell viability and reporting as a percentage of DMSO control cells. Jurkat cells that overexpress BCL2 are generated using MSCV-IRES-GFP retroviral expression system. Jurkat cells infected with BCL2 or control vector viruses are sorted by flow cytometry and the expression of BCL2 confirmed by Western blot analysis using BCL2 antibody|
|Incubation time||72 hours|
|Animal models||T-ALL and AML orthograft mouse model|
|Dosages||20 -25 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 89 mg/mL (200 mM)
Ethanol 40 mg/mL (90 mM)
|Source||Cell Death Discov (2018). Figure 2. KPT-330|
|Cell Lines||K562 and K562G cells|
|Incubation Time||24, 48 and 72 h|
|Results||KPT-330 inhibited proliferation of K562 and K562G cells in a time and dosedependent manner, as shown in the morphology analysis (data not shown) and MTS assay|
KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.
Etchin J, et al. Br J Haematol. 2013 Apr;161(1):117-27. PMID: 23373539.
|Related CRM1 Products|
KPT 330 is a chromosome maintenance protein 1 (CRM1) inhibitor. KPT 330 suppresses downstream effectors of B-cell activation, proliferation and migration in chronic lymphocytic leukemia cells.
Verdinexor (KPT-335) is an orally bioavailable, selective XPO1/CRM1 inhibitor.
KPT-276 is an orally bioavailable selective CRM1 inhibitor.
KPT-185 is a selective CRM1 inhibitor.
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