1393477-72-9

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;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
• CAS NO: 1393477-72-9
• Molecular Formula: C₁₇H₁₁F₆N₇O
• Molecular Weight: 443.3059592
• Product Categories: API;Inhibitors
• Mol File: 1393477-72-9.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• 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)
• 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.
• CAS DataBase Reference: KPT-330(CAS DataBase Reference)
• NIST Chemistry Reference: KPT-330(1393477-72-9)
• EPA Substance Registry System: KPT-330(1393477-72-9)

Safety Data

• Hazardous Substances Data: 1393477-72-9(Hazardous Substances Data)

Usage

Description

KPT-330, also known as Selinexor, is a potent inhibitor of the nuclear export receptor, chromosome region maintenance 1 (CRM1; Exportin-1 (XPO1)). It has demonstrated significant growth suppression in various cancer cells, including T-cell acute lymphoblastic leukemia (T-ALL) and pancreatic cancer cells. KPT-330 is currently being investigated as a potential chemotherapeutic agent for the treatment of multiple types of cancer and is in the clinical trial phase.

Uses

Used in Oncology:
KPT-330 is used as a CRM1 inhibitor for suppressing downstream effectors of B-cell activation, proliferation, and migration in chronic lymphocytic leukemia cells. Its potent growth suppression in various cancer cells makes it a promising candidate for the treatment of multiple types of cancer.
Used in Drug Development:
KPT-330 is being investigated for its potential as a chemotherapeutic agent in treating various types of cancer. Its ability to inhibit the nuclear export receptor CRM1 makes it a valuable compound in the development of new cancer treatments.
Used in Clinical Trials:
KPT-330 is currently in clinical trials, where its efficacy and safety are being evaluated for the treatment of multiple types of cancer. The results of these trials will help determine the future of KPT-330 as a potential chemotherapeutic agent.

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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Relevant articles and documents

NOVEL CRYSTALLINE FORMS OF SELINEXOR AND PROCESS FOR THEIR PREPARATION

The present disclosure relates to solid state forms of Selinexor, processes for preparation thereof and pharmaceutical compositions thereof.

POLYMORPHS OF SELINEXOR

The present invention relates to crystalline forms of the compound represented by Structural Formula I, and compositions comprising crystalline forms of the compound represented by Structural Formula I described herein. The crystalline forms of the compound of Structural Formula I and compositions comprising the crystalline forms of the compound of Structural Formula I provided herein, in particular, single crystalline Form A, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders associated with CRM1 activity, including cancer. Also described herein are methods for preparing the compound of Structural Formula I and its single crystalline forms.