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Eltanexor (KPT-8602) 目录号 GC19466

A second-generation exportin-1 inhibitor

规格 价格 库存 购买数量
1mg
¥529.00
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5mg
¥1,588.00
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10mg
¥2,315.00
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50mg
¥6,284.00
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500mg
¥43,995.00
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1g
¥70,392.00
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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1642300-52-4 SDF Download SDF
别名 N/A
化学名 (E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)acrylamide
Canonical SMILES FC(F)(F)C1=CC(C2=NN(/C=C(C3=CN=CN=C3)/C(N)=O)C=N2)=CC(C(F)(F)F)=C1
分子式 C17H10F6N6O 分子量 428.29
溶解度 Soluble in DMSO 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

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.