WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H100941
CAS#: 496775-62-3 (olamine)
Description: Eltrombopag, also known as SB-497115-GR, is an agonist of the c-mpl (TpoR) receptor, which is the physiological target of the hormone thrombopoietin. Eltrombopag was initially approved by in 2008, for the treatment of thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenic purpura who have had an insufficient response to corticosteroids, immunoglobulin therapy, or splenectomy. In preclinical studies, Eltrombopag was shown to interact selectively with the thrombopoietin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes.
Hodoodo Cat#: H100941
Name: Eltrombopag olamine
CAS#: 496775-62-3 (olamine)
Chemical Formula: C29H36N6O6
Exact Mass: 0.00
Molecular Weight: 564.643
Elemental Analysis: C, 61.69; H, 6.43; N, 14.88; O, 17.00
Related CAS #: 496775-61-2 (free base) 496775-62-3 (olamine)
Synonym: SB 497115GR; SB-497115-GR; SB-497115; SB 497115; SB497115; Eltrombopag olamine; Promacta; Revolade.
IUPAC/Chemical Name: (Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxyiic acid;2-aminoethan-1-ol (1:2)
InChi Key: PLILLUUXAVKBPY-SBIAVEDLSA-N
InChi Code: InChI=1S/C25H22N4O4.2C2H7NO/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33;2*3-1-2-4/h4-13,26,30H,1-3H3,(H,32,33);2*4H,1-3H2/b27-22-;;
SMILES Code: O=C(C1=CC(C2=CC=CC(N/N=C3C(C)=NN(C4=CC=C(C)C(C)=C4)C/3=O)=C2O)=CC=C1)O.NCCO.NCCO
Appearance: Red solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Related CAS# 496775-61-2 (Eltrombopag free base); 496775-62-3 (Eltrombopag olamine).
| Biological target: | Eltrombopag Olamine (Eltrombopag diethanolamine salt) is a thrombopoietin-receptor agonist. |
| In vitro activity: | Eltrombopag's cell toxicity to five cancer cell lines and one macrophage cell line (4T1, A549, H1299, LLC, SMMC7721 and RAW264.7) was evaluated. As shown in Fig. 3A, eltrombopag could inhibit the in vitro cell viability of all the detected cell lines. Reference: Acta Pharm Sin B. 2020 Aug;10(8):1414-1425. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7488360/ |
| In vivo activity: | To detect the in vivo anti-tumor effect of eltrombopag, mice bearing allografts with 4T1 cell lines were used. Over the course of the experiment, eltrombopag was well tolerated, and no signs of acute toxicity were observed (Fig. 3B and Supporting Information Fig. S2). Obvious anti-tumor effects of eltrombopag were observed for the 75 mg/kg dose (P < 0.01) and 150 mg/kg dose (P < 0.01) (Fig. 3C and D). Reference: Acta Pharm Sin B. 2020 Aug;10(8):1414-1425. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7488360/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.3 | 99.76 | |
| DMF | 1.0 | 1.77 | |
| DMF:PBS (pH 7.2) (1:3) | 0.3 | 0.44 | |
| Ethanol | 0.1 | 0.18 |
The following data is based on the product molecular weight 564.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Zhu Y, Yang L, Xu J, Yang X, Luan P, Cui Q, Zhang P, Wang F, Li R, Ding X, Jiang L, Lin G, Zhang J. Discovery of the anti-angiogenesis effect of eltrombopag in breast cancer through targeting of HuR protein. Acta Pharm Sin B. 2020 Aug;10(8):1414-1425. doi: 10.1016/j.apsb.2020.02.007. Epub 2020 Feb 24. PMID: 32963940; PMCID: PMC7488360. 2. Di Paola A, Palumbo G, Merli P, Argenziano M, Tortora C, Strocchio L, Roberti D, Santoro C, Perrotta S, Rossi F. Effects of Eltrombopag on In Vitro Macrophage Polarization in Pediatric Immune Thrombocytopenia. Int J Mol Sci. 2020 Dec 24;22(1):97. doi: 10.3390/ijms22010097. PMID: 33374151; PMCID: PMC7796119. 3. Nevil G, Roth M, Gill J, Zhang W, Teicher B, Erickson SW, Gatto G, Smith M, Kolb EA, Gorlick R. Initial in vivo testing of TPO-receptor agonist eltrombopag in osteosarcoma patient-derived xenograft models by the pediatric preclinical testing consortium. Pediatr Hematol Oncol. 2021 Feb;38(1):8-13. doi: 10.1080/08880018.2020.1802539. Epub 2020 Aug 17. PMID: 32804009. |
| In vitro protocol: | 1. Zhu Y, Yang L, Xu J, Yang X, Luan P, Cui Q, Zhang P, Wang F, Li R, Ding X, Jiang L, Lin G, Zhang J. Discovery of the anti-angiogenesis effect of eltrombopag in breast cancer through targeting of HuR protein. Acta Pharm Sin B. 2020 Aug;10(8):1414-1425. doi: 10.1016/j.apsb.2020.02.007. Epub 2020 Feb 24. PMID: 32963940; PMCID: PMC7488360. 2. Di Paola A, Palumbo G, Merli P, Argenziano M, Tortora C, Strocchio L, Roberti D, Santoro C, Perrotta S, Rossi F. Effects of Eltrombopag on In Vitro Macrophage Polarization in Pediatric Immune Thrombocytopenia. Int J Mol Sci. 2020 Dec 24;22(1):97. doi: 10.3390/ijms22010097. PMID: 33374151; PMCID: PMC7796119. |
| In vivo protocol: | 1. Zhu Y, Yang L, Xu J, Yang X, Luan P, Cui Q, Zhang P, Wang F, Li R, Ding X, Jiang L, Lin G, Zhang J. Discovery of the anti-angiogenesis effect of eltrombopag in breast cancer through targeting of HuR protein. Acta Pharm Sin B. 2020 Aug;10(8):1414-1425. doi: 10.1016/j.apsb.2020.02.007. Epub 2020 Feb 24. PMID: 32963940; PMCID: PMC7488360. 2. Nevil G, Roth M, Gill J, Zhang W, Teicher B, Erickson SW, Gatto G, Smith M, Kolb EA, Gorlick R. Initial in vivo testing of TPO-receptor agonist eltrombopag in osteosarcoma patient-derived xenograft models by the pediatric preclinical testing consortium. Pediatr Hematol Oncol. 2021 Feb;38(1):8-13. doi: 10.1080/08880018.2020.1802539. Epub 2020 Aug 17. PMID: 32804009. |
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