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Eltrombopag

Catalog No. T2562 CAS 496775-61-2

Synonyms: SB-497115, SB-497115-GR

Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).

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Eltrombopag, CAS 496775-61-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 67.00
25 mg	In stock	$ 119.00
50 mg	In stock	$ 155.00
100 mg	In stock	$ 196.00
200 mg	In stock	$ 297.00
500 mg	In stock	$ 490.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Description	Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).
In vitro	Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. [1] Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.[2] Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells. Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells. [3]
In vivo	Eltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees. [1] Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. [3]

Synonyms	SB-497115, SB-497115-GR
Molecular Weight	442.47
Formula	C25H22N4O4
CAS No.	496775-61-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 25 mg/mL (56.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Erickson-Miller CL, et al. Stem Cells, 2009, 27(2), 424-430. 2. Erickson-Miller CL, et al. Leuk Res, 2010, 34(9), 1224-1231. 3. Roth M, et al. Blood, 2012, 120(2), 386-394.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Hematonosis Compound Library Endocrinology-Hormone Compound Library Approved Drug Library Coagulation and Anticoagulation Compound Library

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Keywords

Eltrombopag 496775-61-2 Proteases/Proteasome Thrombin hepatocellular carcinomab Apoptosis SB-497115 Inhibitor hematopoiesis chimpanzee inhibit SB497115 immune thrombocytopenia CD34 blood platelet BAF3 Thrombopoietin Receptor SB-497115-GR Bacterial N2C-Tpo megakaryocyte SB 497115 inhibitor

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