KPT-330, (E)-RN
- Product Name
- KPT-330, (E)-RN
- CAS No.
- 1421923-86-5
- Chemical Name
- KPT-330, (E)-RN
- Synonyms
- (E)-KPT330;Kpt-330, (E)-;KPT-330, (E)-RN;Selinexor E-isomer;Selinexor trans-isomer;KPT-330,(E)-,KPT330,(E);SELINEXOR;KPT-330; (E)-RN;KPT330,(E)-, 10 mM in DMSO;Cariprazine Impurity 30 Hydrochloride;(E)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyrazin-2-ylprop-2-enehydrazide
- CBNumber
- CB92716546
- Molecular Formula
- C17H11F6N7O
- Formula Weight
- 443.31
- MOL File
- 1421923-86-5.mol
KPT-330, (E)-RN Property
- Density
- 1.55±0.1 g/cm3(Predicted)
- solubility
- DMSO: Soluble
- pka
- 9.74±0.43(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- P000111055
- Product name
- (E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
- Purity
- 95+%
- Packaging
- 100mg
- Price
- $258
- Updated
- 2021/12/16
- Product number
- P000111055
- Product name
- (E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
- Purity
- 95+%
- Packaging
- 250mg
- Price
- $386
- Updated
- 2021/12/16
- Product number
- CD11260232
- Product name
- (E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
- Purity
- 95+%
- Packaging
- 100mg
- Price
- $282
- Updated
- 2021/12/16
- Product number
- CD11260232
- Product name
- (E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
- Purity
- 95+%
- Packaging
- 250mg
- Price
- $452
- Updated
- 2021/12/16
- Product number
- 1421923865
- Product name
- (E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
- Packaging
- 250mg
- Price
- $506.16
- Updated
- 2021/12/16
KPT-330, (E)-RN Chemical Properties,Usage,Production
Uses
KPT-330 is an orally bioavailable selective?Chromosome Region Maintenance (CRM1)?inhibitor, that has been shown to block pancreatic cancer cell proliferation and reduce tumor growth in mice.
Synthesis
1421923-96-7
54608-52-5
1421923-86-5
General procedure for the synthesis of (E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylhydrazide from the compound (CAS: 1421923-96-7) and pyrazin-2-hydrazine: 1. a solution was prepared by dissolving (E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid (0.75 g) in EtOAc (25 mL) and THF (12.5 mL). 2. To the above solution, a solution of 2-hydrazinopyrazine (0.23 g) in THF (12 mL) was added dropwise at room temperature. 3. Subsequently, T3P (50% ethyl acetate solution, 1.52 mL) and DIPEA (1.46 mL) were added dropwise and the reaction mixture was stirred at room temperature for 30 minutes. 4. After completion of the reaction, the reaction was quenched with ice-cold water and extracted with EtOAc (3 x 25 mL). 5. The organic layers were combined, washed with brine and dried over anhydrous Na2SO4. 6. concentrated under reduced pressure (35 °C, 20 mmHg) to give 0.698 g of crude product. 7. The crude product was first ground with petroleum ether and then with Et2O to give 275 mg (yield: 29%) of the target compound. Product characterization: 1H NMR (400 MHz, DMSO-d6) δ: 10.3 (s, 1H), 9.15 (s, 2H), 8.59 (s, 2H), 8.30-8.26 (d, J = 14.8 Hz, 1H), 8.13 (s, 1H), 8.06-8.07 (m, 1H), 6.98-6.95 (d, J = 13.4 Hz. 1H); LCMS for C17H12F6N7O [M + H]+: 443.31; found: 444.19 (retention time: 2.625 min, purity: 99.06%).
References
[1] Patent: WO2013/19548, 2013, A1. Location in patent: Page/Page column 71-72
[2] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
KPT-330, (E)-RN Preparation Products And Raw materials
Raw materials
Preparation Products
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