ABT-737

Catalog No.S1002

ABT-737 Chemical Structure

Molecular Weight(MW): 813.43

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

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Cited by 212 Publications

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Biological Activity

Description ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
Features First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
Targets
Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
Bcl-B [1]
(Cell-free assay)
30.3 nM(EC50) 78.7 nM(EC50) 197.8 nM(EC50) 1.82 μM(EC50)
In vitro

ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. [1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. [2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. [3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. [4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OCI-Ly1  NXfJOJgxS2WubDDWbYFjcWyrdImgRZN{[Xl? MkXWNlUxKG6PwrC= NIj0eok4OiCq NGP3TYlFVVOR NH6wV3pk[XW|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>? NVK3bJlOOjZ4NUeyPFg>
KG1a NIWxXYlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFXJbpExNTFyIN88US=> MkPTNlQhcA>? MnzvSG1UVw>? NFTBb5lKSzVyPUeuOlgh|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2PNclI3PTV{N{Gy
Kasumi-1 NYPBfZJTS2WubDDWbYFjcWyrdImgRZN{[Xl? M2XRRlAuOTBizszN NYezZW5pOjRiaB?= NVfreY9ETE2VTx?= MVvJR|UxRTRwOEeg{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mn\1NlY2PTJ5MUK=
KG1a M3PVeWFxd3C2b4Ppd{BCe3OjeR?= NHHGZYQxNTFyIN88US=> M1W5bFI1KGh? NGfoV5ZFVVOR NFTnTVJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NHvYcnozPjV3MkexNi=>
Kasumi-1 M3zadGFxd3C2b4Ppd{BCe3OjeR?= NHH3SYUxNTFyIN88US=> NHfZdYUzPCCq NYnjNI1STE2VTx?= M1nPZYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGrHV3EzPjV3MkexNi=>
MC-3  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnWc4I1PS9zMD:yNEDPxE1? M3;ZVVI1KGh? M{nnN2ROW09? M2S4d4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWLlfnFFOjZ2NEe2NVU>
HN22  NWq1dnVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHGwXJAzNjVxNz61M|IzNjVizszN MkLBNlQhcA>? NXL4fFdsTE2VTx?= MoLtbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUOyOlQ1PzZzNR?=
MC-3  MYHBdI9xfG:|aYOgRZN{[Xl? MXK1M|ExNzJyIN88US=> M3HPVlI1KGh? NGXKbnRFVVOR MXzpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| MkL3NlY1PDd4MUW=
HN22  NVnFdFN5SXCxcITvd4l{KEG|c3H5 MmPTNk42NzdwNT:yNk42KM7:TR?= NYjmenplOjRiaB?= MYjEUXNQ NFjjVHBqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz MXOyOlQ1PzZzNR?=
MOLT-4 NI\3TGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2xNE02ODByIH7N MV:3NkBp MUTEUXNQ NFnNNFZKSzVyPUCuNVk5KM7:TR?= NITZO4gzPjN7MkOzNi=>
RS4;11 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHW1dIcyOC13MECwJI5O M4i5WFczKGh? MmrjSG1UVw>? M2roUGlEPTB;MD6wNFIh|ryP NY[3dWhPOjZ|OUKzN|I>
JURKAT NGDGR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnlNVRROTBvNUCwNEBvVQ>? NITpSVI4OiCq M4TCZ2ROW09? NELRSm9KSzVyPU[2JO69VQ>? NHTMZXAzPjN7MkOzNi=>
CEM R MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPucYIyOC13MECwJI5O NIXvcGI4OiCq NGjNcpZFVVOR NFq0eldKSzVyPUWuOEDPxE1? NXP6VotzOjZ|OUKzN|I>
CEM S MojmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu5NVAuPTByMDDuUS=> MVG3NkBp M2Gw[WROW09? NYO4OZhPUUN3ME2xNk4yKM7:TR?= MYSyOlM6OjN|Mh?=
MOLT-4 M3K2WGFxd3C2b4Ppd{BCe3OjeR?= NFfZN|QyOC1zMECwJI5O NGm4R|YzPCCq MnT4SG1UVw>? NVjVdY9T[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> NUPs[W9LOjZ|OUKzN|I>
CEM S MXXBdI9xfG:|aYOgRZN{[Xl? NUfOTYZTOTBvMUCwNEBvVQ>? MkHZNlQhcA>? MUPEUXNQ MU\jZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= M3;nPVI3Ozl{M{Oy
JURKAT M{TST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP4VINSOTByLUGwNFAhdk1? M{jjWVQ5KGh? NV3vOnJsTE2VTx?= NET5SVJKSzVyPUm1OeKyQS5|IH7N Mk\sNlYyPzJ{Nkm=
LOUCY MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3JNVAxNTFyMECgcm0> NYD6fJh{PDhiaB?= M3XzWGROW09? NWTEfGxrUUN3ME2zNk45yrFzMD65JI5O MYWyOlE4OjJ4OR?=
WM-115 NFfTeWdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVexNFDDqG6P NXHaVGFUPzJiaB?= NUXVZ2pJ\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= M{P0d|I3OTF4N{e2
B16 M37hcmNmdGxiVnnhZoltcXS7IFHzd4F6 MYCxNFDDqG6P MUm3NkBp MnrR[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? NXewdJl2OjZzMU[3O|Y>
HL-60  NFL6OGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYC3NkBp NHj3bXZKSzVywrC9JFExNjdibl2= NWHPZYVGOjZyNEW2NFk>
MOLM-13  NGPFOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnkO|IhcA>? MV;JR|UxyqB;IEK3Mlkhdk1? NEPaRmozPjB2NU[wPS=>
OCI-AML3 NIjtWFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHtemZ6PzJiaB?= M4rERmlEPTEEoE2gNVk2OCCwTR?= NGfkU|kzPjB2NU[wPS=>
BCWM.1 NGfqc3pCeG:ydH;zbZMhSXO|YYm= M{PQUlAuOS54IN88US=> MX2yOEBp M{fUUYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MkLpNlU5QTN{OUC=
MWCL-1 MkTlRZBweHSxc3nzJGF{e2G7 Mn7SNE0yNjZizszN MV6yOEBp MkTJbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NIWyUJMzPTh7M{K5NC=>
MM.1s M33zRWFxd3C2b4Ppd{BCe3OjeR?= NULGcnFSOC1zLk[g{txO Mmn5NlQhcA>? MoXmbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NF6yUZMzPTh7M{K5NC=>
HCT116 NXrNNZc5TnWwY4Tpc44hSXO|YYm= NHHSdJk{NzFyIN88US=> NXjvSlNIOTMEoHlCpC=> MnnTSG1UVw>? Mn3GbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w NWrBN5F1OjV5MUWwNlg>
HCT116 BAX BAK1 DKO NH33eHhHfW6ldHnvckBCe3OjeR?= NH3Ic4U{NzFyIN88US=> NYLselFwOTMEoHlCpC=> NF[zSIFFVVOR MWPpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? MkOxNlU4OTVyMki=
HCT116 M3Pn[mZ2dmO2aX;uJGF{e2G7 M3PmXVExKM7:TR?= NXjCUXdxOTMEoHlCpC=> NYO0fW9XTE2VTx?= MUPpcoNz\WG|ZYOgS2ZRNUyFM1KgdJVv[3Sj NFLhR4QzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO NFTW[GtHfW6ldHnvckBCe3OjeR?= NXTPdGZ5OTBizszN NWfrSGhkOTMEoHlCpC=> NHLrd3dFVVOR NF25e3lqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th Mke3NlU4OTVyMki=
HCT116 MWDBeZRweGijZ4mgRZN{[Xl? NV3SZYNzOTBizszN MVWxNuKhcMLi MkTDSG1UVw>? NIDJZodqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? M3r2WVI2PzF3MEK4
HCT116 BAX BAK1 DKO MoS3RZV1d3CqYXf5JGF{e2G7 MVmxNEDPxE1? NUDyOJZ{OTMEoHlCpC=> NELSbZVFVVOR M4XIXYlv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm NG\yXZAzPTdzNUCyPC=>
U937 NHizfJRCeG:ydH;zbZMhSXO|YYm= NITtcGIxNjF{NT2yJO69VQ>? Mmn3NlQhcA>? NYGydYw5\W6qYX7j[ZMhTEiDL2itNVEucW6mdXPl[EBieG:ydH;zbZM> Ml3pNlU4OTRyMkS=
U937  MWfBdI9xfG:|aYOgRZN{[Xl? NVXCdGUzOC53IN88US=> MUCyOEBp Mlr2[Y5p[W6lZYOgZ4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[U0{KGG|IIflcIwh[XNiTn;4ZUBt\X[nbB?= NFTETpAzPTdzNECyOC=>
HL-60 AAA-Bcl-2 MYDBdI9xfG:|aYOgRZN{[Xl? M1vNSFAuPSEQvF2= M2XxcFQ5KGh? NF3sTW1KSzVyPUCuPFch|ryv78{MbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYW2dIdYOjV5MUG0OlA>
HL-60 EEE-Bcl-2 NGX3TZJCeG:ydH;zbZMhSXO|YYm= Mmq0NE02KM7:TR?= M1L3clQ5KGh? M{C4N2lEPTB;NTFOwI3wxIxiaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Moe5NlU4OTF2NkC=
U87 M1K3Z2Z2dmO2aX;uJGF{e2G7 MmDOOVAh|ryP M2TI[VI1KGh? NEjI[Xhz\WS3Y3XzJJRp\SCvUl7BJIV5eHKnc4Ppc44hdGW4ZXzzJI9nKE2PUD2yMEBOVVBvMUSgZY5lKEKlbD2y NUO3[3g{OjV4Nke2OlM>
K562 NIPSenFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUexMVExKM7:TR?= MXO0PEBp MlnXSG1UVw>? NHjHUnBKSzVyPUK2Mlch|ryP MmXGNlU2QTZ3NkG=
K562/Mcl -1-IRESBim MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDrWoZCUUN3ME25MlMh|ryP NWi5d4lwOjV3M{W5NFA>
K562/Bcl- 2-IRESBim NH3tdZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXUO|dKSzVyPUCuN|Uh|ryP NUPlT45vOjV3M{W5NFA>
Jurkat MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m1eGlEPTB;MD62OkDPxE1? NX20bFd7OjV3M{W5NFA>
JurkatΔBak MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj2fW5DUUN3ME61NEDPxE1? NHrxTXYzPTV|NUmwNC=>
HL60/VCR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH3UYVVUUN3ME6xNFAh|ryP M1LiR|I2PTN3OUCw
Kasumi-1 NXjIdW9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonSTWM2OD1yLkCxJO69VQ>? Mm\ONlU2OzV7MEC=
Kasumi-1/ABT M3rsTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwNUGg{txO MorYNlU2OzV7MEC=
THP-1 M3jZdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGxTWM2OD1zLkK3JO69VQ>? MX6yOVU{PTlyMB?=
U937 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTXTWM2OD13LkK5JO69VQ>? NG\2T3UzPTV|NUmwNC=>
C1498 NInFe41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTGTWM2OD14LkGzJO69VQ>? NEfpNFEzPTV|NUmwNC=>
RPMI 8226 NIrVWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXJepBKSzVyPUCuNlUh|ryP M{fzZlI2PTN3OUCw
MM.1S MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvr[4xKSzVyPUCuOFAh|ryP M4rZV|I2PTN3OUCw
NCI-H929 M{e4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\KNGlEPTB;MUWuNlEh|ryP NHTEUY4zPTV|NUmwNC=>
U266 NXrMcGxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwNkig{txO NWL3[HdFOjV3M{W5NFA>
MCF-7 NYG5cZltS2WubDDWbYFjcWyrdImgRZN{[Xl? MUC1JO69VQ>? NGG0Z3I1QCCq NHrq[W9FVVOR NV;XbXN{\W6qYX7j[ZMhfGinIIPlcpNqfGm4aYT5JJRwKG:{IILh[IlifGmxbh?= NVPx[ItwOjV2MEmxNlQ>
MCF-7 MnqyRZBweHSxc3nzJGF{e2G7 NE\lNHM2KM7:TR?= M4rMUlQwOjRxNEigbC=> NEHoNmFFVVOR MmKybY5kemWjc3XzJJRp\SClbHXheoVlKFCDUmC= M2K5RVI2PDB7MUK0
MCF-7 MnTlSpVv[3Srb36gRZN{[Xl? MUi1JO69VQ>? MWGyOEBp Ml7xSG1UVw>? M2q4ZYVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NH;iWXozPTRyOUGyOC=>
MDA-MB 231  NInmTopHfW6ldHnvckBCe3OjeR?= NV\YNXVKPSEQvF2= MoPTNlQhcA>? MYDEUXNQ M2e2fIVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? M2fjVVI2PDB7MUK0
ZR-75-1  NYj1VnJJTnWwY4Tpc44hSXO|YYm= MnTTOUDPxE1? MoTsNlQhcA>? MnzQSG1UVw>? MVLlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> MlvuNlU1ODlzMkS=
A549 NIDBVppE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3r3ZVAuOjBizszN MWG3NkBp NGjmb|ZFVVOR NYrTSVJY\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NYPOfVg1OjV|OEi3OlI>
H1299 NUm2fY53S2WubDDWbYFjcWyrdImgRZN{[Xl? NVP5dZhFOC1{MDFOwG0> M3vpSVczKGh? M{OwS2ROW09? M3PsWoRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M4nrVVI2Ozh6N{[y
HO-8910 NUPaOldUS2WubDDWbYFjcWyrdImgRZN{[Xl? MYOwMVIxKM7:TR?= MXS3NkBp M1Pz[mROW09? M2TXOIRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M3fsXFI2Ozh6N{[y
HT-29 NFu0OpVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn3ENE0zOCEQvF2= MmPBO|IhcA>? NV7JPJQyTE2VTx?= NXL5bpVk\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= MXuyOVM5QDd4Mh?=
HCT-116 NHnwU5VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX3nc3g{OC1{MDFOwG0> MUm3NkBp M2fOUWROW09? NIDWUpll\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NFvYbnYzPTN6OEe2Ni=>
A549 NFTrb4FCeG:ydH;zbZMhSXO|YYm= NIGwVYYzOCEQvF2= MlWxOFghcA>? NHywbphFVVOR MY\pcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= M4\FdFI2Ozh6N{[y
H1299 NF33[nhCeG:ydH;zbZMhSXO|YYm= NHWzUZEzOCEQvF2= NIn1WIQ1QCCq MYfEUXNQ MX;pcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= MWSyOVM5QDd4Mh?=
Sc-1 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXWwMlAxODFvMTFOwG0> MoXDPVYhcA>? NFHlOIFl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnLSNlU{PzN3MEi=
OcI-LY18 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{O4T|AvODByMT2xJO69VQ>? MUi5OkBp M4HSb4Rm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlfqNlU{PzN3MEi=
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U266 M1fhT2Z2dmO2aX;uJGF{e2G7 NI\zbIM2ODBxN{WwJI5O MlnDNlQwPDhiaB?= NHjGUmNFVVOR MUDkc5dvemWpdXzheIV{KEKrbTygdJJqdmOrcHHscJkhfGinIFXMJIl{d2[xcn2= NIWwepgzPTJyOEi4PC=>
RPMI8226 MmHVSpVv[3Srb36gRZN{[Xl? MWm1NFAwPzVyIH7N NIK1SHEzPC92ODDo MX;EUXNQ MkW1[I94dnKnZ4XsZZRmeyCEaX2sJJBzcW6laYDhcIx6KHSqZTDFUEBqe2:ob4Lt NH;OWpEzPTJyOEi4PC=>
MM.1S NUnlRZRJTnWwY4Tpc44hSXO|YYm= MXK1NFAwPzVyIH7N NFLS[lgzPC92ODDo NVPjdFBMTE2VTx?= NVHt[Wk{\G:5boLl[5Vt[XSnczDCbY0tKHC{aX7jbZBidGy7IITo[UBGVCCrc3;mc5Ju MX:yOVIxQDh6OB?=
Clone A NUHUSFB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;NNE4z6oDVNkCg{txO MWe3NkBp NITRVYdFVVOR MoPlTWM2OD15LkWg{txO NFjRUHUzPTJyOEi4Ni=>
CX-1 MlPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvZUplMOC5{4pETOlAh|ryP M1nmWFczKGh? MlfWSG1UVw>? NG\FXmRKSzVyPUGuPEDPxE1? NYrkUZU3OjV{MEi4PFI>
LS174T MnXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nMZ|AvOuLCk{[wJO69VQ>? M3HzeVczKGh? M3;Je2ROW09? MlHBTWM2OD1zOD6zJO69VQ>? MnnPNlUzODh6OEK=
HT29 M4\FcWFxd3C2b4Ppd{BCe3OjeR?= M3m0SVEwPS9zMDFOwG0> MVe0PEBp MWnjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXqyOVE6OjF6OB?=
SW480 MoPJRZBweHSxc3nzJGF{e2G7 NHXmcWoyNzVxMUCg{txO NVjVV4h2PDhiaB?= MlzLZ4F2e2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MmjJNlUyQTJzOEi=
Colo205 MXHBdI9xfG:|aYOgRZN{[Xl? MWGxM|UwOTBizszN NGroRoU1QCCq M4O3eYNifXOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGjzZ3AzPTF7MkG4PC=>
Caco2 MlPLRZBweHSxc3nzJGF{e2G7 MUmxM|UwOTBizszN NVGyUVBtPDhiaB?= MYrjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NFq4UWgzPTF7MkG4PC=>
PCI-13 M4LVTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXuO|IhcA>? NUDaeWdMTE2VTx?= MUnHTVUxRTF3INMxJFEvQCEQvF2= MlSwNlUyOzl|OEe=
PCI-15B MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi4SFQ4OiCq NHTPcodFVVOR Mk\5S2k2OD1zMTFCtUA1NjVizszN NFLydJAzPTF|OUO4Oy=>
UM-SCC22B MkfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrMNlI4OiCq M1TVT2ROW09? NVHYNGpJT0l3ME2xPUDDuSB{Lkmg{txO M1TqPVI2OTN7M{i3
UM-SCC47 NF7COXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Lm[|czKGh? MmT3SG1UVw>? MkGxS2k2OD1zOTFCtUAyOi5|IN88US=> NGqxOJYzPTF|OUO4Oy=>
93-VU-147T NEPaOFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXxO|IhcA>? NEXm[2ZFVVOR NY\SWnVIT0l3ME20MlMhyrFiMz61JO69VQ>? M1nQbFI2OTN7M{i3
UD-SCC2 MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjac4ZyPzJiaB?= MofFSG1UVw>? MkGwS2k2OD1{ODFCtUAzNjlizszN NF\iVYozPTF|OUO4Oy=>
UPCI:SCC90 M1L3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XXZ|czKGh? MkKzSG1UVw>? NVvmVnF[T0l3ME22MlYhyrFiMT61JO69VQ>? M4jVdVI2OTN7M{i3
RPMI-8226  MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUSxNlUwOjVyL{WwNEBvVQ>? MYO0PIjDqA>? NETydpdFVVOR NVfsfFBS\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFG4[lAzPTByOEKwNi=>
OPM-2  NFS2WFBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4qwXVEzPS9{NUCvOVAxKG6P NXrDZ4k5PDiqwrC= MV;EUXNQ MlfG[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MVOyOVAxQDJyMh?=
RPMI-8226  NUCzUXFtSXCxcITvd4l{KEG|c3H5 MV6xNlUwOjVyL{WwNEBvVQ>? NX\xZZFrPDiqwrC= NUX2WY5TTE2VTx?= Mn3tbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV\GR2w6OjVyMEiyNFI>
OPM-2  NUTsUpFKSXCxcITvd4l{KEG|c3H5 MUOxNlUwOjVyL{WwNEBvVQ>? NE\TU2E1QGkEoB?= NWnm[ZYzTE2VTx?= M4Xab4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYH6PHVPOjVyMEiyNFI>
COG-LL-319 M3yxWWZ2dmO2aX;uJGF{e2G7 MljqNVAxKG6P M33kbFEwOy94IHi= MojZSG1UVw>? NVLaRYxMcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBO[2xvMTDjcIVifmGpZR?= MXiyOFk2OTR5Mh?=
RS4;11 MXfGeY5kfGmxbjDBd5NigQ>? M3P5UVExOCCwTR?= MWSxM|MwPiCq Mo\JSG1UVw>? NYLJNGhOcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBO[2xvMTDjcIVifmGpZR?= M1WzPVI1QTVzNEey

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PARP / c-PARP / cleaved caspase 3 ; 

PubMed: 21393866     


H146 cells were preincubated in normoxia or hypoxia (1% O2) for 18 hours prior to treatment with ABT-737 (89.1 nM ), after which cells were harvested for protein analysis by Western blot. 

Hif-1a; 

PubMed: 22006676     


Representative western blots for HIF-1α, PARP and cleaved caspase 3 in response to 24-72 hr exposure to ABT-737 in varying concentration in normoxia and hypoxia in 4 neuroblastoma cell lines. Actin is shown as a loading control. Blots are representative of 3 independent experiments.

γ-H2AX / p-ATM; 

PubMed: 21084274     


Induction of γ-H2AX and p-ATM by ABT-737. Cells were treated with 10 µmol/L ABT-737 for 24 hours and then maintained in fresh media for 1 or 2 more days prior to Western blot analysis.

21393866 22006676 21084274
Immunofluorescence
cytochrome C; 

PubMed: 26447615     


Immunocytochemistry revealed the release of mitochondrial cytochrome c (green) into the cytoplasm after ABT-737 exposure (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field.

Bax; 

PubMed: 26447615     


Immunocytochemistry revealed the mitochondrial translocation of Bax from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field C. To assess whether ABT-737 treatment has an effect on the dimerization of Bax, the levels of dimeric Bax were measured with or without ABT-737 treatment in MC-3 and HN22 cells.

Bim; 

PubMed: 26447615     


Immunocytochemistry revealed the mitochondrial translocation of Bim from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field.

AIF; 

PubMed: 25034785     


localization of apoptosis inducing factor (AIF) in LCSC pre-stained with Mitotracker Red and untreated or treated with 500 nM ABT-737 for 48 h. Magnification × 60, zoom × 3, bar 20 μm. 

p65 ; 

PubMed: 28846096     


BCL-xL dependent SVEC cells were treated with ABT-737 (10 μM) +/- Q-VD-Oph (30 μM) for 1 h, immunostained for p65 and analysed by confocal microscopy. TNF (20 ng/ml) was used as positive control for p65 nuclear translocation. Scale bar represents 30μM. Representative images from three independent experiments.

26447615 25034785 28846096
Growth inhibition assay
Cell viability; 

PubMed: 22311987     


Stably transfected K562 cells were treated with increasing concentrations of ABT-737, obatoclax, or maritoclax for 24 h. Cell viability was determined by measuring intracellular ATP levels with the CellTiter Glo assay.

22311987
ELISA
IL-6 / IL-8; 

PubMed: 21084274     


The secretion of IL-6 and IL-8 in PV-10 cells treated with DMSO, ABT-737 or enantiomer for 24 hours was determined by ELISA.

21084274
In vivo In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. [1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. [2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. [5]

Protocol

Kinase Assay:

[1]

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Fluorescence polarization assays:

Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.
Cell Research:

[4]

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  • Cell lines: SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
  • Concentrations: 0.001-10 μM
  • Incubation Time: 48 hours
  • Method:

    SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
  • Formulation: 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%)
  • Dosages: 20 and 30 mg/kg
  • Administration: For intraperitoneal (i.p.) every day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (122.93 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% Propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 813.43
Formula

C42H45ClN6O5S2

CAS No. 852808-04-9
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    What’s the recommended method about reconstitution of the compound for in vivo animal study?

  • Answer:

    For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, ABT-737 can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID