KPT-8602 (KPT 8602

Name	KPT-8602
Synonyms	CS-2388 ATG-016 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)-
CAS	1642300-52-4

Molecular Formula	C17H10F6N6O
Molar Mass	428.3
Density	1.57±0.1 g/cm3(Predicted)
Boling Point	574.4±60.0 °C(Predicted)
Solubility	DMSO: 4.72 mg/mL
pKa	13.06±0.50(Predicted)
Storage Condition	-20℃
In vitro study	In cell viability assays, KPT-8602 were potent inhibitors of AML cells. It inhibits XPO1/cargo interaction and nuclear export, induces apoptosis in primary CLL cells and significantly inhibits proliferation of diffuse large B- cell lymphoma cell lines.
In vivo study	KPT-8602 has Oral activity, and selinexor has similar pharmacokinetic activity, but the blood brain barrier penetration is significantly reduced. Toxicity tests in rats and monkeys showed that KPT-8602 was safe and well tolerated, possibly due to its inability to penetrate the blood-brain barrier into the central nervous system, anorexia, restlessness, there was a decrease in the symptoms of weight loss. KPT-8602 had better anti-leukemic activity and better tolerability in the AML PDX model. In the AML-CN model, almost complete elimination was achieved for human AML cells. KPT-8602 has little toxicity to normal hematopoietic stem cells and progenitor cells. After repeated dosing, KPT-8602 did not accumulate in plasma and prolonged the survival of the human leukemia xenograft model.

Last Update：2024-01-02 23:10:35

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Product Name: KPT-8602 Visit Supplier Webpage Request for quotation
CAS: 1642300-52-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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KPT-8602 (KPT 8602

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