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KPT-330

Cat. No. M3152

KPT-330 Structure

Synonym: Selinexor

Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 150 In stock
50mg USD 400 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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
Concentrations ~1 μM
Incubation time 72 hours
Animal Experiment
Animal models T-ALL and AML orthograft mouse model
Formulation Pluronic F-68/PVP-K29/32
Dosages 20 -25 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 443.31
Formula C17H11F6N7O
CAS Number 1421923-86-5
Purity >99%
Solubility DMSO 89 mg/mL (200 mM)
Ethanol 40 mg/mL (90 mM)
Storage at -20°C
References

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.

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Keywords: KPT-330, Selinexor supplier, CRM1, inhibitors

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