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Selinexor | Inhibitor of the nuclear export receptor CRM1/XPO1

Selinexor (1393477-72-9) is a potent inhibitor of the nuclear export receptor, chromosome region maintenance 1 (CRM1; Exportin-1 (XPO1)). It exhibited potent growth suppression in various T-cell acute lymphoblastic leukemia (T-ALL) cells (IC50’s = 34-203 nM)1 and pancreatic cancer cells (IC50 ~ 150 nM)2. Selinexor is being investigated as a possible chemotherapeutic in treating multiple types of cancer.3-8 Currently in clinical trials.

 

References/Citations
1) Etchin et al. (2013), KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-ALL and AML; Br. J. Haematol. 161 117
2) Azmi et al. (2013), Selective Inhibitors of Nuclear Export Block Pancreatic Cancer Cell Proliferation and Reduce Tumor Growth in Mice; Gastroenterology 144 447
3) Desisto et al. (2019), Exportin 1 inhibition induces nerve growth factor receptor expression to inhibit the NF-kB pathway in preclinical models of pediatric high-grade glioma; Mol. Cancer Ther. Epub ahead of print
4) Aboukameel et al. (2018), Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression; Oncotarget 9 35327
5) Baek et al. (2018), XPO1 inhibition by selinexor induces potent cytotoxicity against high grade bladder malignancies; Oncotarget 9 34567
6) Wahba et al. (2018), The XPO1 Inhibitor Selinexor Inhibits Translation and Enhances the Radiosensitivity of Glioblastoma Cells Grown In Vitro and In Vivo; Mol. Cancer Ther. 17 1717
7) Arango et al. (2017), Selinexor (KPT-330) demonstrates anti-tumor efficacy in preclinical models of triple-negative breast cancer; Breast Cancer Res. 19 93
8) Conforti et al. (2017), Therapeutic Effects of XPO1 Inhibition in Thymic Epithelial Tumors; Cancer Res. 77 5614

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Catalog#  10-4011-0005

$60.00
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CAS:
1393477-72-9
Catalog Number:
10-4011
Activity:
Inhibitor of the nuclear export receptor CRM1/XPO1
Chemical Name:
(Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N’-pyrazin-2-ylprop-2-enehydrazide
Alternate Name:
KPT-330
Molecular Weight:
443.31
Molecular Formula:
C17H11F6N7O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml). or in Ethanol (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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