KPT-330

Description

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.

Uses

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.

storage

Store at -20°C

References

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.?19 540 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