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Selinexor

SKU: orb1301068

Description

Selinexor (KPT-330) is an orally bioavailable, selective inhibitor of Exportin 1 (XPO1/CRM1). It induces cell cycle arrest and apoptosis, demonstrating antitumor activity in preclinical models of multiple myeloma, including both in vitro cell studies and in vivo xenograft experiments.

Research Area

Neuroscience

Images & Validation

Key Properties

CAS Number1393477-72-9
MW443.3
Purity>98%
FormulaC17H11F6N7O
SMILESFC(F)(F)c1cc(cc(c1)C(F)(F)F)-c1ncn(\C=C/C(=O)NNc2cnccn2)n1
TargetCRM1
SolubilitySoluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)

Bioactivity

Target IC50
Jurkat cells:34 - 203 nM|HBP-ALL cells:34-203 nM|ATC cell:150–500 nM|SKW-3 cells:34-203 nM|DND-41 cells:34-203 nM|MOLT-4 cells:34-203 nM|KOPTK-1 cells:34-203 nM|T-ALL cells:34-203 nM
In Vivo
METHODS: To assay antitumor activity in vivo, Selinexor (20-25 mg/kg) was administered by gavage to NSG mice harboring the human T-ALL tumor MOLT-4 three times per week for thirty-six days. RESULTS: Selinexor-treated mice exhibited significant inhibition of leukemia cell growth with significant survival benefit. METHODS: To assay anti-tumor activity in vivo, Selinexor (20 mg/kg) was administered by gavage three times per week for four weeks to an NSG mouse model of primary AML in patients. RESULTS: Selinexor was cytotoxic to primary AML cells transplanted into mice.
In Vitro
METHODS: Six T-ALL cells, MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3 and DND-41, were treated with Selinexor (0-1000 µM) for 72 h. Cell growth inhibition was detected using Cell Titer Glo assay. RESULTS: Selinexor treatment inhibited T-ALL cell growth with IC50 values of 34-203 nM. METHODS: Multiple myeloma cells MM1S were treated with Selinexor (100 nM) for 8 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Selinexor treatment resulted in the accumulation of p53, IκB, p21 and p27 in the nucleus of MM1S cells.

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

KPT-330

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Key Properties

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Selinexor (orb1301068)

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5 mg
¥ 2,600.00
25 mg
¥ 4,680.00
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