ChemicalBook Product Catalog Biochemical Engineering Inhibitors Transmembrane Transporters CRM1 inhibitors Selinexor

Selinexor

Product NameSelinexor
CAS1393477-72-9
MFC17H11F6N7O
MW443.31
EINECS
MOL File1393477-72-9.mol

Chemical Properties

Density	1.55±0.1 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO (up to at least 25 mg/ml). or in Ethanol (up to at least 25 mg/ml)
pka	9.74±0.43(Predicted)
form	solid
color	Off-white
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
InChI	InChI=1S/C17H11F6N7O/c18-16(19,20)11-5-10(6-12(7-11)17(21,22)23)15-26-9-30(29-15)4-1-14(31)28-27-13-8-24-2-3-25-13/h1-9H,(H,25,27)(H,28,31)/b4-1-
InChIKey	DEVSOMFAQLZNKR-RJRFIUFISA-N
SMILES	C(NNC1=NC=CN=C1)(=O)/C=C\N1C=NC(C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=N1

Usage And Synthesis

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)1and pancreatic cancer cells (IC50~ 150 nM)2. Selinexor is being investigated as a possible chemotherapeutic in treating multiple types of cancer.3-8Currently 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.

Synthesis

Synthesis route of Selinexor
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in vivo

Selinexor (KPT-330) dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV4–11) in vivo, with little toxicity to normal haematopoietic cells^[1]. In SCID mice with diffuse human MM bone lesions, KPT-330 inhibits MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs^[2].

storage

Store at -20°C

References

[1] JULIA ETCHIN. 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[J]. British Journal of Haematology, 2013, 161 1: 117-127. DOI:10.1111/bjh.12231
[2] ASFAR S. AZMI . Selective Inhibitors of Nuclear Export Block Pancreatic Cancer Cell Proliferation and Reduce Tumor Growth in Mice[J]. Gastroenterology, 2013, 144 2: Pages 447-456. DOI:10.1053/j.gastro.2012.10.036
[3] JOHN A DESISTO. Exportin 1 Inhibition Induces Nerve Growth Factor Receptor Expression to Inhibit the NF-κB Pathway in Preclinical Models of Pediatric High-Grade Glioma.[J]. Molecular Cancer Therapeutics, 2020, 19 1: 540-551. DOI:10.1158/1535-7163.mct-18-1319
[4] AMRO ABOUKAMEEL. Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression.[J]. Oncotarget, 2018, 9 82: 35327-35342. DOI:10.18632/oncotarget.26239
[5] HAN BIT BAEK. XPO1 inhibition by selinexor induces potent cytotoxicity against high grade bladder malignancies.[J]. Oncotarget, 2018: 34567-34581. DOI:10.18632/oncotarget.26179
[6] AMY WAHBA. The XPO1 Inhibitor Selinexor Inhibits Translation and Enhances the Radiosensitivity of Glioblastoma Cells Grown In Vitro and In Vivo.[J]. Molecular Cancer Therapeutics, 2018, 17 8: 1717-1726. DOI:10.1158/1535-7163.mct-17-1303
[7] NATALIA PAEZ ARANGO. Selinexor (KPT-330) demonstrates anti-tumor efficacy in preclinical models of triple-negative breast cancer.[J]. Breast Cancer Research : BCR, 2017: 93. DOI:10.1186/s13058-017-0878-6
[8] FABIO CONFORTI. Therapeutic Effects of XPO1 Inhibition in Thymic Epithelial Tumors.[J]. ACS Chemical Health & Safety, 2017: 5614-5627. DOI:10.1158/0008-5472.can-17-1323

Selinexor

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