[CAS NO. 1642300-52-4] Eltanexor (KPT-8602)
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PRODUCTS SPECIFICATIONS [1642300-52-4]
Catalog
SLK-S8397
Brand
Selleck
CAS
1642300-52-4
DESCRIPTION [1642300-52-4]
Overview
| MDL | MFCD30489739 |
|---|---|
| Molecular Weight | 428.29 |
| Molecular Formula | C17H10F6N6O |
| SMILES | O=C(N)/C(C1=CN=CN=C1)=C/N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3349 mL | 11.6743 mL | 23.3487 mL |
| 5 mM | 0.4670 mL | 2.3349 mL | 4.6697 mL |
| 10 mM | 0.2335 mL | 1.1674 mL | 2.3349 mL |
| 50 mM | 0.0467 mL | 0.2335 mL | 0.4670 mL |
Description
Eltanexor (KPT-8602, ONO-7706，ATG-016) is a second-generation, orally bioavailable inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure.
Targets
| XPO1 [1] |
In vitro
KPT-8602 is a potent inhibitor of AML cells in cell-based viability assays. 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
In vivo
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. KPT-8602 does not accumulate in plasma after repetitive dosing and prolongs survival in a human leukemia xenograft model of AML.
References
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