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Eltanexor(KPT-8602)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1642300-52-4
规格:98%
分子量:428.29
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
500mg电议
1g电议

产品介绍

Eltanexor (KPT-8602)

A second-generation exportin-1 inhibitor
CAS:1642300-52-4
分子式:C17H10F6N6O
分子量:428.29
纯度:98%
存储:Store at -20°C

Background:

Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor. KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. KPT-8602 is well tolerated and highly active against AML blasts and leukemia-initiating cells. Eltanexor shows improved efficacy and in vivo tolerability in hematological malignancies.


KPT-8602 is a potent inhibitor of AML cells in cell-based viability assays[1]. KPT-8602 inhibits XPO1/cargo interactions and nuclear export, induces apoptosis of primary CLL cells and significantly inhibits proliferation of diffuse large B-cell lymphoma cell lines[2]
KPT-8602 is orally bioavailable and has similar pharmacokinetic properties to selinexor, but has markedly reduced (approximately 30-fold less) penetration across the blood?brain barrier. Toxicology studies in rats and monkeys indicate that KPT-8602 has a substantially better tolerability profile, probably due to its inability to penetrate into the CNS, with reduced anorexia, malaise and weight loss compared to selinexor.


KPT-8602 exhibits superior anti-leukemic activity and better tolerability in the AML PDX models tested, with nearly complete elimination of human AML cells in the AML-CN model. KPT-8602 is minimally toxic to normal hematopoietic stem and progenitor cells[1]. KPT-8602 does not accumulate in plasma after repetitive dosing and prolongs survival in a human leukemia xenograft model of AML[2].


Reference:
[1] Etchin J, et al. Leukemia. 2017, 31(1):143-150.
[2] Hing ZA, et al. Leukemia. 2016, 30(12):2364-2372.