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Eltanexor, also known as KPT-8602, is a second-generation exportin-1 (CRM1) inhibitor with IC50 values of 20−211 nM in 10 AML lines. Eltanexor (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 (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.
J Cell Mol Med. 2022 May;26(9):2646-2657.
Venetoclax enhances DNA damage induced by XPO1 inhibitors: A novel mechanism underlying the synergistic antileukaemic effect in acute myeloid leukaemia
Eltanexor purchased from AbMole
| Molecular Weight | 428.29 |
| Formula | C17H10F6N6O |
| CAS Number | 1642300-52-4 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CRM1 Products |
|---|
| CRM1-IN-2
CRM1-IN-2 is a noncovalent CRM1 inhibitor. |
| CRM1-IN-1
CRM1-IN-1 is a noncovalent CRM1 inhibitor. |
| KPT-251
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity. |
| Felezonexor (CBS9106)
Felezonexor (CBS9106; SL-801) is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity without affecting CRM1 mRNA levels. Felezonexor is also a reversible inhibitor of XPO1, inhibits nuclear export by covalently binding to Cys528 as well as by inducing the degradation of XPO1. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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