| Identification | Back Directory | [Name]
KPT-330 | [CAS]
1393477-72-9 | [Synonyms]
KPT-330
CS-1056
Aloradine
Selinexor
KPT330; KPT 330
KPT330,Selinexor
KPT-330 USP/EP/BP
Selinexor free base
Selinexor (KPT-330)
KPT-330,Selinexor, >98%
SELINEXOR;KPT330;KPT 330
(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyrazin-2-ylprop-2-enehydrazide
(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
(KPT330)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
(2Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 2-(2-pyrazinyl)hydrazide
2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyrazinyl)hydrazide, (2Z)-
(2Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 2-(2-pyrazinyl)hydrazide(Selinexor) | [Molecular Formula]
C17H11F6N7O | [MDL Number]
MFCD27987944 | [MOL File]
1393477-72-9.mol | [Molecular Weight]
443.31 |
| Chemical Properties | Back Directory | [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) | [form ]
solid | [pka]
9.74±0.43(Predicted) | [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. |
| Hazard Information | Back Directory | [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. | [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) 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 |
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