Eltrombopag

For research use only.

Catalog No.S4502 Synonyms: SB-497115

6 publications

Eltrombopag  Chemical Structure

CAS No. 496775-61-2

Eltrombopag (SB-497115), a member of the biarylhydrazone class, is a nonpeptide agonist of the thrombopoietin receptor (TpoR), used to treat chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP).

Selleck's Eltrombopag has been cited by 6 publications

2 Customer Reviews

  • 32D‐MPL cells were treated with hetrombopag (10 nmol/L), eltrombopag (100 nmol/L) or rhTPO (10 ng/mL) for the indicated time. Whole‐cell lysates were analysed by Western blotting using the indicated antibodies.

    J Cell Mol Med, 2018, 22(11):5367-5377. Eltrombopag purchased from Selleck.

    Effect of eltrombopag on cell cycle progression in Huh7 cells. (A) Cells were treated with EP (0 and 10 μg/ml) for 72 h. DNA was stained with propidium iodide, and flow cytometric analysis of cell phase distribution was performed using a Muse™ cell analyzer. (B) Cells were treated with EP (0, 1 and 10 μg/ml) for 72 h. Protein expression was determined by western blot analysis using anti-cyclin D1, anti-p21 and anti-GAPDH antibodies. SDS-PAGE was performed on acrylamide gels.

    Int J Oncol, 2015, 47(5):1696-702.. Eltrombopag purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Eltrombopag (SB-497115), a member of the biarylhydrazone class, is a nonpeptide agonist of the thrombopoietin receptor (TpoR), used to treat chronic hepatitis C-associated thrombocytopenia and chronic immune (idiopathic) thrombocytopenia (ITP).
Targets
thrombopoietin receptor (TpoR) [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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Ba/F3 M3HvbWZ2dmO2aX;uJIF{e2G7 NHHDc|FC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJJRpem:vYn;wc4lmfGmwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBud3W|ZTDCZU9HOyClZXzsd{BjgSCtaX7hd4Uh[WO2aY\heIlwdiCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvODN6zszN M1;sTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{izPVQ6Lz5zOEe4N|k1QTxxYU6=
Ba/F3 NWPVWYY4TnWwY4Tpc44h[XO|YYm= MYTB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIITodo9u[m:yb3nleIlvKHKnY3XweI9zKGmwIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGGldHn2ZZRqd25ib3[gV5RifDVicnXzdI9ve2ViZXzlcYVvfC2mcnn2[Y4hemWyb4L0[ZIh\2WwZTDlfJBz\XO|aX;uMEBGSzVyPUCuNFM5|ryP NGjhPIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEe3PFk{Pid-MUi3O|g6OzZ:L3G+
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HEK293/PDZK1 M2LyfGZ2dmO2aX;uJIF{e2G7 NYi0[5BFUW6qaXLpeIlwdiCxZjDPRXRROUJzLX3l[IlifGWmIGuzTH1me3S{b37lMVMue3WuZnH0[UB2eHSja3WgbY4hcHWvYX6gU2FVWDGEMTDlfJBz\XO|aX7nJGhGUzJ7Mz;QSHpMOSClZXzsd{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBMcT1zND65{txO Mlj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2MkKxPVEoRjJzNEKyNVkyRC:jPh?=
HEK293/PDZK1 MULGeY5kfGmxbjDhd5NigQ>? MmPGTY5pcWKrdHnvckBw\iCRQWTQNWI{NW2nZHnheIVlKFt|SG3ld5Rz[WSrb3ygNVdj\XSjLXfseYN2em:waXTlJJVxfGGtZTDpckBpfW2jbjDPRXRROUJ|IHX4dJJme3OrbnegTGVMOjl|L2DEXmsyKGOnbHzzJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGtqRTJ3LkdOwG0> M4\NdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEKyNVkyLz5{MUSyNlE6OTxxYU6=
HEK293/PDZK1 MX3GeY5kfGmxbjDhd5NigQ>? M1jnSmlvcGmkaYTpc44hd2ZiT1HUVFFDOy2vZXTpZZRm\CCdM1jd[ZN1emGmaX;sJFE4[mW2YT3ncJVkfXKxbnnk[UB2eHSja3WgbY4hcHWvYX6gU2FVWDGEMzDlfJBz\XO|aX7nJGhGUzJ7Mz;QSHpMOSClZXzsd{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7n M3vMcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEKyNVkyLz5{MUSyNlE6OTxxYU6=
HEK293/PDZK1 MX;GeY5kfGmxbjDhd5NigQ>? NH;Cd4dKdmirYnn0bY9vKG:oIF;DWFEudWWmaXH0[YQhYzF2Q230[ZRz[WW2aInsZY1ud26rdX2geZB1[WunIHnuJIh2dWGwIF;DWFEh\XiycnXzd4lv\yCKRVuyPVMwWEScS{GgZ4VtdHNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\w>? Mnr3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2MkKxPVEoRjJzNEKyNVkyRC:jPh?=
HEK293/PDZK1 MoC5SpVv[3Srb36gZZN{[Xl? MoDaN|AhdWmwcx?= MkfaSJJ2\yC3cIThb4UhcW5iaIXtZY4hV0GWUEHCNUBmgHC{ZYPzbY5oKEiHS{K5N{9RTFqNMTDj[YxteyCjdDCzO{Bl\WeFIH\vdkA{OCCvaX7z NULaT2N1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0NlIyQTFpPkKxOFIzOTlzPD;hQi=>
HEK293/PDZK1 NEPhNmFHfW6ldHnvckBie3OjeR?= NVvqTWM2OzBibXnudy=> MWfEdpVoKHWydHHr[UBqdiCqdX3hckBQSVSSMlKxJIV5eHKnc4PpcochUEWNMkmzM3BFYktzIHPlcIx{KGG2IEO3JIRm\0NiZn;yJFMxKG2rboO= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR{MkG5NUc,OjF2MkKxPVE9N2F-
HEK293/PDZK1 NXra[nF4TnWwY4Tpc44h[XO|YYm= NXrxR242OzBibXnudy=> NH;GXohFenWpIIXweIFs\SCrbjDoeY1idiCRQ2SxJIV5eHKnc4PpcochUEWNMkmzM3BFYktzIHPlcIx{KGG2IEO3JIRm\0NiZn;yJFMxKG2rboO= NEnHUHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUSyNlE6OSd-MkG0NlIyQTF:L3G+
HEK293/PDZK1 MmTDSpVv[3Srb36gZZN{[Xl? MljLTY5pcWKrdHnvckBw\iCRQWTQNWIyNW2nZHnheIVlKFt|SG3ld5Rzd26nLUOtd5Vt\mG2ZTD1dJRic2ViaX6gbJVu[W5iT1HUVFFDOSCneIDy[ZN{cW6pIFjFT|I6Oy:SRGrLNUBk\WyuczDifUB{[2mwdHnscIF1cW:wIHPveY51cW6p M2L6RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEKyNVkyLz5{MUSyNlE6OTxxYU6=
HEK293/PDZK1 MWrGeY5kfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKE:DVGCyRlEudWWmaXH0[YQhYzOKXXXzeJJwdmVvMz3zeYxn[XSnIIXweIFs\SCrbjDoeY1idiCRQWTQNmIyKGW6cILld5NqdmdiSFXLNlk{N1CGWluxJINmdGy|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmd? NHK3OpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUSyNlE6OSd-MkG0NlIyQTF:L3G+
DAOY MkTQdWhVWyCjc4PhfS=> NV3Dd5I4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= NYq5O4k2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 MXTxTHRUKGG|c3H5 NH\ESnJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MlvhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MkT5dWhVWyCjc4PhfS=> M4[4RZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NVXZZZk3eUiWUzDhd5NigQ>? NITIblZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 NX7tc4l1eUiWUzDhd5NigQ>? MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MkTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MYPxTHRUKGG|c3H5 MY\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NXXaVHBIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NVHtSGc{eUiWUzDhd5NigQ>? MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NVTRbpJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) M3PQbJFJXFNiYYPzZZk> MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NFOxfYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M4H1dJFJXFNiYYPzZZk> NFrSOHdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= MoryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
VERO-E6 MoTBSpVv[3Srb36gZZN{[Xl? MUW0PEBpenN? NH3tbWhVd3irY3n0fUBESzVyIHHnZYlve3RiVlXSU{1GPiClZXzsd{Bl\XSncn3pcoVlKGG2IES4JIhwfXK|IHL5JIhq\2hiY3;ueIVvfCCrbXHnbY5oKCi|YX3lJINwdmSrdHnvcpMh[XNiMm;MSXkhf2m2aH;1eEBmgHCxc4Xy[UB1dyByLkCxJG1QUSCVQWLTJGNwXi1{II\pdpV{MSxiQ1O1NF0{NjJ4zszN NUK5eopRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDZzMUCxM{c,S2iHTVLMQE9iRg>?
Vero MnPGRY51cX[rcnHsJIF{e2G7 MlrkNlQhcHK| MUjBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDTRXJUNUOxVj2yJEh3cXKjbDD0bZRmeilibXXhd5Vz\WRiYomgdIxieXWnIHHzd4F6KGmwIG\ldo8h[2WubIOgZZQhVU:LIECuNFEzPSCjZoTldkAzPCCqcjygTWM2OD16LkK3{txO NHfCfmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PjFzMEGvK|5EcEWPQly8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT5 / STAT5 / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 30156363     


32D‐MPL cells were treated with hetrombopag (10 nmol/L), eltrombopag (100 nmol/L) or rhTPO (10 ng/mL) for the indicated time. Whole‐cell lysates were analysed by Western blotting using the indicated antibodies

p-RB / RB / CDK4 / CDK6 / Cyclin D1 ; 

PubMed: 30156363     


After treatment of 32D‐MPLcells with hetrombopag, eltrombopag or 10 ng/mL rhTPO for 24 hours, whole‐cell lysates were immunoblotted with the indicated antibodies. 

30156363
Growth inhibition assay
Cell viability; 

PubMed: 31564981     


Viability of K562 cells incubated with EP (2.5, 5, 10 and 30 μg/mL) alone for 24, 48, 72 and 96 hrs. 

31564981
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

Solubility (25°C)

In vitro DMSO 26 mg/mL warmed (58.76 mM)
Water Insoluble
Ethanol Insoluble

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Chemical Information

Molecular Weight 442.47
Formula

C25H22N4O4

CAS No. 496775-61-2
Storage powder
in solvent
Synonyms SB-497115
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04797000 Recruiting Drug: Eltrombopag|Drug: Placebo Myelodysplastic Syndromes Novartis Pharmaceuticals|Novartis May 25 2021 Phase 2
NCT04600960 Recruiting Drug: Eltrombopag Chemotherapy-induced Thrombocytopenia|Eltrombopag Institute of Hematology & Blood Diseases Hospital December 31 2020 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID