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Eltanexor

Cat. No. M9909
Eltanexor Structure
Synonym:

KPT-8602

Size Price Availability Quantity
2mg USD 145  USD145 In stock
5mg USD 290  USD290 In stock
10mg USD 495  USD495 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 428.29
Formula C17H10F6N6O
CAS Number 1642300-52-4
Purity >99%
Solubility DMSO 50 mg/mL (warmed)
Storage at -20°C
References

[1] Thomas Vercruysse, et al. Clin Cancer Res. The Second-Generation Exportin-1 Inhibitor KPT-8602 Demonstrates Potent Activity against Acute Lymphoblastic Leukemia

[2] Z A Hing, et al. Leukemia. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies

[3] J Etchin, et al. Leukemia. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells

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Keywords: Eltanexor, KPT-8602 supplier, CRM1, inhibitors

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