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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.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 428.29 |
| Formula | C17H10F6N6O |
| CAS Number | 1642300-52-4 |
| Purity | >99% |
| Solubility | DMSO 50 mg/mL (warmed) |
| Storage | at -20°C |
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