Eltrombopag (SB497115) Olamine

Catalog No.S2229 Synonyms: SB-497115-GR

For research use only.

Eltrombopag Olamine (SB-497115-GR, SB497115) is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR).

Eltrombopag (SB497115) Olamine Chemical Structure

CAS No. 496775-62-3

Selleck's Eltrombopag (SB497115) Olamine has been cited by 11 Publications

Purity & Quality Control

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Biological Activity

Description Eltrombopag Olamine (SB-497115-GR, SB497115) is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR).
Targets
thrombopoietin receptor [1]
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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 564.63
Formula

C29H36N6O6

CAS No. 496775-62-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)N=NC3=CC=CC(=C3O)C4=CC(=CC=C4)C(=O)O)C.C(CO)N.C(CO)N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01550185 Terminated Drug: eltrombopag olamine|Procedure: standard follow-up care Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia Roswell Park Cancer Institute|GlaxoSmithKline May 2012 Phase 1
NCT01428635 Completed Drug: Eltrombopag Olamine Accelerated Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Blast Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Primary Myelofibrosis|Thrombocytopenia M.D. Anderson Cancer Center|National Cancer Institute (NCI) January 13 2012 Phase 2|Phase 3
NCT00102726 Completed Drug: SB497115|Other: Placebo Thrombocytopaenia GlaxoSmithKline February 2005 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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