research use only
Cat.No.S2229
| Related Targets | PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX |
|---|---|
| Other TpoR Inhibitors | Butyzamide |
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In vitro |
DMSO
: 89 mg/mL
(157.62 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 564.63 | Formula | C29H36N6O6 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 496775-62-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | SB497115,SB-497115-GR | 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 | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
thrombopoietin receptor
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|---|---|
| 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. Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL. 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. |
| 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. Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. |
References |
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(data from https://clinicaltrials.gov, updated on 2025-09-24)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07189910 | NOT_YET_RECRUITING | Primary Immune Thrombocytopenia (ITP) |
Union Hospital, Tongji Medical College, Huazhong University of Science and Technology |
2025-12-01 | PHASE4 |
| NCT05961410 | RECRUITING | Lymphoma; Peripheral Blood Stem Cell Transplantation |
National Taiwan University Hospital |
2023-08-15 | PHASE2 |
| NCT01927731 | COMPLETED | Bone Marrow Transplantation Recipient; Cord Blood Transplant Recipient; Hematopoietic Cell Transplantation Recipient |
M.D. Anderson Cancer Center |
2013-10-14 | PHASE2 |
| NCT06768619 | COMPLETED | Thrombocytopenia |
Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
2023-03-20 | |
| NCT01428635 | COMPLETED | 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 |
2012-01-13 | PHASE2; PHASE3 |
| NCT01772420 | COMPLETED | Adult Myelodysplastic Syndrome; Anemia; Chronic Myelomonocytic Leukemia |
Albert Einstein College of Medicine |
2012-10 | PHASE2 |
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