| Identification | Back Directory | [Name]
KPT-8602 | [CAS]
1642300-52-4 | [Synonyms]
CS-2388
KPT-8602
Eltanexor
KPT-8602 (KPT 8602
Eltanexor
(KPT-8602
(E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)acrylamide
5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αE)- | [Molecular Formula]
C17H10F6N6O | [MDL Number]
MFCD30489739 | [MOL File]
1642300-52-4.mol | [Molecular Weight]
428.29 |
| Chemical Properties | Back Directory | [Boiling point ]
574.4±60.0 °C(Predicted) | [density ]
1.57±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
13.06±0.50(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
(αE)?-α-?[[3-?[3,?5-?bis(Trifluoromethyl)?phenyl]?-?1H-?1,?2,?4-?triazol-?1-?yl]?methylene]?-?5-pyrimidineacetamide is an exportin-1 inhibitor with anti-leukemic activity. Exportin-1 mediates nuclear trafficking of proteins. (αE)?-α-?[[3-?[3,?5-?bis(Trifluoromethyl)?phenyl]?-?1H-?1,?2,?4-?triazol-?1-?yl]?methylene]?-?5-pyrimidineacetamide can be used to develop treatments for acute lymphoblastic leukemia. | [in vivo]
KPT-8602 (15 mg/kg; oral gavage; daily for 12 days) shows potent anti-lymphoblastic leukemia activity[1]. | Animal Model: | Female BALB/c mice (model with the JAK3 (M511I) mutation)[1] | | Dosage: | 15 mg/kg | | Administration: | Oral gavage; daily for 12 days | | Result: | Showed a marked reduction in total white blood cell (WBC) counts after 2 days of treatment compared to placebo-treated animals and the WBC counts continued to drop until they reached normal levels (<10,000 cells/μL) by day 12. |
| [storage]
Store at -20°C |
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