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Eltrombopag

Cat. No. M3488
Eltrombopag Structure
Synonym:

SB-497115-GR, SB497115

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 70  USD70 In stock
5mg USD 40  USD40 In stock
10mg USD 70  USD70 In stock
50mg USD 180  USD180 In stock
100mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Eltrombopag (SB-497115) is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia. In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes. Animal studies confirmed that administration could increase platelet counts. In addition, eltrombopag (SB-497115) decreased proliferation of all cancer cell lines.

Chemical Information
Molecular Weight 442.47
Formula C25H22N4O4
CAS Number 496775-61-2
Solubility (25°C) DMSO 27 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Bruno Fattizzo, et al. Eltrombopag in Immune Thrombocytopenia, Aplastic Anemia, and Myelodysplastic Syndrome: From Megakaryopoiesis to Immunomodulation

[2] Phillip Scheinberg. Activity of eltrombopag in severe aplastic anemia

[3] Taylor Olmsted Kim, et al. Eltrombopag for use in children with immune thrombocytopenia

[4] Raymond S M Wong, et al. Safety and efficacy of long-term treatment of chronic/persistent ITP with eltrombopag: final results of the EXTEND study

[5] Danielle M Townsley, et al. Eltrombopag Added to Standard Immunosuppression for Aplastic Anemia

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Keywords: Eltrombopag, SB-497115-GR, SB497115 supplier, Thrombopoietin/Thrombin, inhibitors, activators


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