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| | KPT-330 Basic information |
| Product Name: | KPT-330 | | Synonyms: | KPT-330;(2Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 2-(2-pyrazinyl)hydrazide;Selinexor (KPT-330);(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide;2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyrazinyl)hydrazide, (2Z)-;Aloradine;KPT330,Selinexor;(KPT330)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide | | CAS: | 1393477-72-9 | | MF: | C17H11F6N7O | | MW: | 443.31 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 1393477-72-9.mol |  |
| | KPT-330 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. |
| | KPT-330 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)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 |
| | KPT-330 Preparation Products And Raw materials |
| Raw materials | 3,5-Bis(trifluoromethyl)benzonitrile-->2-Hydrazinopyrazine-->3,5-DI(TRIFLUOROMETHYL)BENZENE-1-CARBOTHIOAMIDE-->(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid-->3,5-Di(trifluoromethyl)benzamide-->(Z)-isopropyl 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate | | Preparation Products | 3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazole |
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