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 144 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  M2fuRmNmdGxiVnnhZoltcXS7IFHzd4F6 NXXMRZBnOjVyIH7NxsA> M{fnNlczKGh? MnH2SG1UVw>? MmOzZ4F2e2WmIEm3KUBtd3O|IH;mJJZq[WKrbHn0fUBqdiClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJGJEVDZic3nSUmE> NUjtb2N3OjZ4NUeyPFg>
KG1a NVfyOmRvS2WubDDWbYFjcWyrdImgRZN{[Xl? NIKwcY8xNTFyIN88US=> MYCyOEBp M3;pNWROW09? M33kOmlEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3fTNVI3PTV{N{Gy
Kasumi-1 Ml20R4VtdCCYaXHibYxqfHliQYPzZZk> NVzWeJJmOC1zMDFOwG0> NUm5fYpXOjRiaB?= MW\EUXNQ NVXKdJlnUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NILPcWIzPjV3MkexNi=>
KG1a M{TNcGFxd3C2b4Ppd{BCe3OjeR?= M3KwW|AuOTBizszN MX:yOEBp Mm\4SG1UVw>? M{ew[Ilv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MkLuNlY2PTJ5MUK=
Kasumi-1 M1;yUmFxd3C2b4Ppd{BCe3OjeR?= M3nNW|AuOTBizszN NVOxU5NPOjRiaB?= NXT6dXF[TE2VTx?= MnHZbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFfSd48zPjV3MkexNi=>
MC-3  M2PUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXtUmpCPS9zMD:yNEDPxE1? MomyNlQhcA>? NIPqN45FVVOR NVvLV5A3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NH;Lbo4zPjR2N{[xOS=>
HN22  M{LtO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;RSZczNjVxNz61M|IzNjVizszN M3vwUFI1KGh? MYnEUXNQ MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkOzNlY1PDd4MUW=
MC-3  NYXwWWtKSXCxcITvd4l{KEG|c3H5 NHGzPWQ2NzFyL{KwJO69VQ>? NGr6[4czPCCq NEfmOlFFVVOR MnnKbY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= NEfoSXUzPjR2N{[xOS=>
HN22  NWTzXnlpSXCxcITvd4l{KEG|c3H5 NXz6Z3lvOi53L{euOU8zOi53IN88US=> MnPrNlQhcA>? MW\EUXNQ MVnpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| M4HPVlI3PDR5NkG1
MOLT-4 NU\ZU|RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXZU5cyOC13MECwJI5O MXm3NkBp M37YXWROW09? MkPFTWM2OD1yLkG5PEDPxE1? M3uzR|I3Ozl{M{Oy
RS4;11 M3\1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW3b4Q{OTBvNUCwNEBvVQ>? NYjuTGxOPzJiaB?= MmjnSG1UVw>? MVHJR|UxRTBwMECyJO69VQ>? M{j5OVI3Ozl{M{Oy
JURKAT MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xNE02ODByIH7N MmDFO|IhcA>? NX7XU5l2TE2VTx?= MX7JR|UxRTZ4IN88US=> MnHFNlY{QTJ|M{K=
CEM R M120cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn30NVAuPTByMDDuUS=> MWK3NkBp NXHvVIhTTE2VTx?= MXPJR|UxRTVwNDFOwG0> MUCyOlM6OjN|Mh?=
CEM S MlewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvBNVAuPTByMDDuUS=> MYC3NkBp NU\POnZ7TE2VTx?= M1;RUmlEPTB;MUKuNUDPxE1? NEm1SZYzPjN7MkOzNi=>
MOLT-4 NEnMdotCeG:ydH;zbZMhSXO|YYm= MmXYNVAuOTByMDDuUS=> MkfqNlQhcA>? NWPQUXNKTE2VTx?= MYTjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= MWCyOlM6OjN|Mh?=
CEM S MUjBdI9xfG:|aYOgRZN{[Xl? NIXqW|EyOC1zMECwJI5O NY\JV4NDOjRiaB?= NWjoe3AzTE2VTx?= MXnjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= MlfQNlY{QTJ|M{K=
JURKAT MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjjNoxpOTByLUGwNFAhdk1? MUe0PEBp M{TmUWROW09? NGjHToRKSzVyPUm1OeKyQS5|IH7N NIP5c3kzPjF5MkK2PS=>
LOUCY NGX1R2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGzUGlWOTByLUGwNFAhdk1? NIH4[Ho1QCCq MlzISG1UVw>? M1TtUGlEPTB;M{KuPOKyOTBwOTDuUS=> MUeyOlE4OjJ4OR?=
WM-115 M3LlRWNmdGxiVnnhZoltcXS7IFHzd4F6 NVPIVmVYOTBywrDuUS=> MnLuO|IhcA>? NX:5cIk2\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= NGjsWmUzPjFzNke3Oi=>
B16 NGezToFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnqzNVAxyqCwTR?= NFq0bYs4OiCq MXnlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? M1TMSFI3OTF4N{e2
HL-60  NITkVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\JO|IhcA>? NHfzOZVKSzVywrC9JFExNjdibl2= M3;HcFI3ODR3NkC5
MOLM-13  MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jXVVczKGh? MoPiTWM2OMLiPTCyO{46KG6P Mn22NlYxPDV4MEm=
OCI-AML3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M135dVczKGh? M3HPWWlEPTEEoE2gNVk2OCCwTR?= M1fTT|I3ODR3NkC5
BCWM.1 NV3Ub3lOSXCxcITvd4l{KEG|c3H5 M{PBN|AuOS54IN88US=> MlTRNlQhcA>? M1TFR4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MnfLNlU5QTN{OUC=
MWCL-1 MnXjRZBweHSxc3nzJGF{e2G7 MV:wMVEvPiEQvF2= NH\ucXEzPCCq MV7pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MoC5NlU5QTN{OUC=
MM.1s M1PMW2Fxd3C2b4Ppd{BCe3OjeR?= MnHBNE0yNjZizszN NYDrfo1wOjRiaB?= M4PVfolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MoLiNlU5QTN{OUC=
HCT116 NIXycIRHfW6ldHnvckBCe3OjeR?= M4jMXFMwOTBizszN NFvRW44yOsLiaNMg MXfEUXNQ M2TR[Ilv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= NX;kXYZsOjV5MUWwNlg>
HCT116 BAX BAK1 DKO M4LaemZ2dmO2aX;uJGF{e2G7 NHvYOZY{NzFyIN88US=> MnW4NVLDqGkEoB?= MlnjSG1UVw>? M2HYS4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= NULOUZV7OjV5MUWwNlg>
HCT116 MYPGeY5kfGmxbjDBd5NigQ>? NYLnO|ZGOTBizszN NGj5e5QyOsLiaNMg MVnEUXNQ NGLCZndqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th MofrNlU4OTVyMki=
HCT116 BAX BAK1 DKO NWDiPYg5TnWwY4Tpc44hSXO|YYm= M3:0ZVExKM7:TR?= MlLnNVLDqGkEoB?= MWHEUXNQ NGX2[W9qdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th MXSyOVcyPTB{OB?=
HCT116 NH3VOlZCfXSxcHjh[5khSXO|YYm= NHfwZ4YyOCEQvF2= NWm3TZNqOTMEoHlCpC=> NFv4TFFFVVOR MWTpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> MXSyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO M3K4[mF2fG:yaHHnfUBCe3OjeR?= NGfBOI8yOCEQvF2= MYmxNuKhcMLi MVzEUXNQ MVrpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> Mn3wNlU4OTVyMki=
U937 MYnBdI9xfG:|aYOgRZN{[Xl? NVXnXY17OC5zMkWtNkDPxE1? Ml\hNlQhcA>? MVjlcohidmOnczDETGEwYC1zMT3pcoR2[2WmIHHwc5B1d3Orcx?= Mk\xNlU4OTRyMkS=
U937  MoXRRZBweHSxc3nzJGF{e2G7 NYfETnVwOC53IN88US=> NIPmbpUzPCCq MkHw[Y5p[W6lZYOgZ4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[U0{KGG|IIflcIwh[XNiTn;4ZUBt\X[nbB?= M2\EV|I2PzF2MEK0
HL-60 AAA-Bcl-2 MnuwRZBweHSxc3nzJGF{e2G7 NHzZO2UxNTVizszN NXnPbJdbPDhiaB?= M37iTmlEPTB;MD64O{DPxG4xvJzpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUeyOVcyOTR4MB?=
HL-60 EEE-Bcl-2 NWf3WFFJSXCxcITvd4l{KEG|c3H5 MXywMVUh|ryP NV7qXlk4PDhiaB?= NXL0UGp1UUN3ME21JO69de,:jDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnPGNlU4OTF2NkC=
U87 M1rsUmZ2dmO2aX;uJGF{e2G7 Mn7UOVAh|ryP Mnq2NlQhcA>? NY\XbploemWmdXPld{B1cGVibWLORUBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUG0JIFv\CCEY3ytNi=> Ml\lNlU3Pjd4NkO=
K562 M1jZemNmdGxiVnnhZoltcXS7IFHzd4F6 M3rxb|EuOTBizszN NVr1XZBHPDhiaB?= MmHJSG1UVw>? MnjwTWM2OD1{Nj63JO69VQ>? M1XyTVI2PTl4NU[x
K562/Mcl -1-IRESBim MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7VWZBKSzVyPUmuN{DPxE1? NEnXVYkzPTV|NUmwNC=>
K562/Bcl- 2-IRESBim NX;q[mtkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjhTWM2OD1yLkO1JO69VQ>? NFXkT5ozPTV|NUmwNC=>
Jurkat MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwNk[g{txO M3LLSVI2PTN3OUCw
JurkatΔBak NXjmdYlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELrXW9KSzVyPkWwJO69VQ>? NIG1PGYzPTV|NUmwNC=>
HL60/VCR Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DKSmlEPTB-MUCwJO69VQ>? NXTBO5pEOjV3M{W5NFA>
Kasumi-1 NVX0SGZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTZTmNKSzVyPUCuNFEh|ryP NWK5[4ZoOjV3M{W5NFA>
Kasumi-1/ABT MorRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwNUGg{txO MWCyOVU{PTlyMB?=
THP-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTFwMkeg{txO MnHGNlU2OzV7MEC=
U937 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2K4VGlEPTB;NT6yPUDPxE1? NUPaU|JqOjV3M{W5NFA>
C1498 MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIG4XWVKSzVyPU[uNVMh|ryP NELKU5czPTV|NUmwNC=>
RPMI 8226 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:wTWM2OD1yLkK1JO69VQ>? MmHTNlU2OzV7MEC=
MM.1S MkL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwNECg{txO NHTIOZczPTV|NUmwNC=>
NCI-H929 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF3LkKxJO69VQ>? NXjHV|BqOjV3M{W5NFA>
U266 M{P4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXGS4RKSzVyPUCuOlgh|ryP MXuyOVU{PTlyMB?=
MCF-7 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2TXeVUh|ryP MoTpOFghcA>? M2XtOmROW09? M3OxU4VvcGGwY3XzJJRp\SC|ZX7zbZRqfmm2eTD0c{BweiC{YXTpZZRqd25? NEnPWVczPTRyOUGyOC=>
MCF-7 MVHBdI9xfG:|aYOgRZN{[Xl? NWP6fXlPPSEQvF2= NEXJV281NzJ2L{S4JIg> M3LSZ2ROW09? NXTBPZFZcW6lcnXhd4V{KHSqZTDjcIVifmWmIGDBVnA> M3THW|I2PDB7MUK0
MCF-7 MW\GeY5kfGmxbjDBd5NigQ>? NX:2flVPPSEQvF2= MXWyOEBp NGrP[JhFVVOR Ml\h[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh MlvvNlU1ODlzMkS=
MDA-MB 231  NIS5RZFHfW6ldHnvckBCe3OjeR?= MmnQOUDPxE1? Mon3NlQhcA>? M4rCNGROW09? NG[4[|ZmdmijbnPld{B1cGWuZY\lcEBw\iCPY3ytNUBmgHC{ZYPzbY9vyqB? MXOyOVQxQTF{NB?=
ZR-75-1  M3TZcGZ2dmO2aX;uJGF{e2G7 MXK1JO69VQ>? NIm1d4EzPCCq MXvEUXNQ MmDv[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh NWfJdXpIOjV2MEmxNlQ>
A549 NELySWhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXywMVIxKM7:TR?= NGnaclM4OiCq NHe1Zo1FVVOR NXjpSIlI\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NYHjfYVrOjV|OEi3OlI>
H1299 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mo\FNE0zOCEQvF2= MWK3NkBp NXrEWVBmTE2VTx?= MWXk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv MVeyOVM5QDd4Mh?=
HO-8910 M{C4N2NmdGxiVnnhZoltcXS7IFHzd4F6 NV7me3I6OC1{MDFOwG0> M4W2UFczKGh? M1rYSmROW09? M4ezZoRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? MVOyOVM5QDd4Mh?=
HT-29 NFnjTZJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1XNdlAuOjBizszN Moj0O|IhcA>? Mmn5SG1UVw>? M{jSbIRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? NFjDd4ozPTN6OEe2Ni=>
HCT-116 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NF3tTpExNTJyIN88US=> M4DZWlczKGh? MYTEUXNQ NVL5O4t3\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NXW4RXhnOjV|OEi3OlI>
A549 M{m5cGFxd3C2b4Ppd{BCe3OjeR?= M3fXNVIxKM7:TR?= NH;oXVI1QCCq MYTEUXNQ MWXpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= MkfjNlU{QDh5NkK=
H1299 NEnDZ2lCeG:ydH;zbZMhSXO|YYm= MUWyNEDPxE1? NV;T[|RDPDhiaB?= NVLFfYF{TE2VTx?= MXrpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NGHsXoYzPTN6OEe2Ni=>
Sc-1 M1nYTmNmdGxiVnnhZoltcXS7IFHzd4F6 NVW0S|RjOC5yMECxMVEh|ryP MXG5OkBp MXvk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3e5U|I2Ozd|NUC4
OcI-LY18 NXrDO2hyS2WubDDWbYFjcWyrdImgRZN{[Xl? M1fFSlAvODByMT2xJO69VQ>? MVy5OkBp MX;k[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1viRlI2Ozd|NUC4
RL  MnnuR4VtdCCYaXHibYxqfHliQYPzZZk> NVGzRmRkOC5yMECxMVEh|ryP M3fMV|k3KGh? MWDk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGnsNGkzPTN5M{WwPC=>
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MM.1S M2nrWmZ2dmO2aX;uJGF{e2G7 NXH0d41{PTByL{e1NEBvVQ>? Mm[xNlQwPDhiaB?= NGLW[lRFVVOR MUfkc5dvemWpdXzheIV{KEKrbTygdJJqdmOrcHHscJkhfGinIFXMJIl{d2[xcn2= M2nHNFI2OjB6OEi4
Clone A NITZSpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zQcFAvOuLCk{[wJO69VQ>? M3\kVlczKGh? MXLEUXNQ NVjtSI1GUUN3ME23MlUh|ryP NH60WZAzPTJyOEi4Ni=>
CX-1 NUfmOJlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPzXGZLOC5{4pETOlAh|ryP NGjtXG84OiCq MUPEUXNQ MWLJR|UxRTFwODFOwG0> NGe1XoEzPTJyOEi4Ni=>
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HT29 M3;Pd2Fxd3C2b4Ppd{BCe3OjeR?= NHK1V|AyNzVxMUCg{txO MUK0PEBp Mnj3Z4F2e2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NHi5VZEzPTF7MkG4PC=>
SW480 NEXwSodCeG:ydH;zbZMhSXO|YYm= MVqxM|UwOTBizszN MnrjOFghcA>? NHvYV21k[XW|ZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnvRNlUyQTJzOEi=
Colo205 NFzJWmVCeG:ydH;zbZMhSXO|YYm= MW[xM|UwOTBizszN NYezfnVWPDhiaB?= MYHjZZV{\XNiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVSyOVE6OjF6OB?=
Caco2 NGnvellCeG:ydH;zbZMhSXO|YYm= MkfwNU82NzFyIN88US=> NE\sSJU1QCCq NIX0[Hhk[XW|ZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFHPTlMzPTF7MkG4PC=>
PCI-13 M373eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\Nd3Q4OiCq NG\vWI1FVVOR NIfIUJdIUTVyPUG1JOKyKDFwODFOwG0> MUWyOVE{QTN6Nx?=
PCI-15B Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\4O|IhcA>? NF;vPVZFVVOR NWm1PFA5T0l3ME2xNUDDuSB2LkWg{txO MYqyOVE{QTN6Nx?=
UM-SCC22B MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUm3NkBp M17HemROW09? MVLHTVUxRTF7INMxJFIvQSEQvF2= M2rFV|I2OTN7M{i3
UM-SCC47 M3XLVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fuT|czKGh? MWTEUXNQ MYfHTVUxRTF7INMxJFEzNjNizszN MX6yOVE{QTN6Nx?=
93-VU-147T NVnsPXNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[yO|IhcA>? MkLkSG1UVw>? MlPUS2k2OD12LkOgxtEhOy53IN88US=> NH;jOWozPTF|OUO4Oy=>
UD-SCC2 M1;JV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zNUVczKGh? NF3Wd|lFVVOR NYK2TndST0l3ME2yPEDDuSB{Lkmg{txO NWTGOo5POjVzM{mzPFc>
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RPMI-8226  NF[4NVlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXPUUVZ6OTJ3L{K1NE82ODBibl2= MXW0PIjDqA>? MkPFSG1UVw>? NV;jVoFN\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NVT4NWJ4OjVyMEiyNFI>
OPM-2  NVjGTpZ4S2WubDDWbYFjcWyrdImgRZN{[Xl? NUTXZYRCOTJ3L{K1NE82ODBibl2= MmL4OFhpyqB? MnfaSG1UVw>? Mn7P[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NH:ze5AzPTByOEKwNi=>
RPMI-8226  NV;2OYFRSXCxcITvd4l{KEG|c3H5 MV6xNlUwOjVyL{WwNEBvVQ>? MnfhOFhpyqB? M{DENGROW09? M{n1Uolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlPkNlUxODh{MEK=
OPM-2  MWTBdI9xfG:|aYOgRZN{[Xl? MUexNlUwOjVyL{WwNEBvVQ>? NUWxc5RxPDiqwrC= NXPTS|dRTE2VTx?= MWLpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mmr0NlUxODh{MEK=
COG-LL-319 M3LIOGZ2dmO2aX;uJGF{e2G7 M3fLdFExOCCwTR?= Mkf6NU8{NzZiaB?= NFq3[o5FVVOR MVPpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IF3jcE0yKGOuZXH2ZYdm MkD0NlQ6PTF2N{K=
RS4;11 NV6yU2pKTnWwY4Tpc44hSXO|YYm= M1OzSlExOCCwTR?= Ml3vNU8{NzZiaB?= NYO3THVQTE2VTx?= M3rWVolv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgUYNtNTFiY3zlZZZi\2V? NFnic2ozPDl3MUS3Ni=>

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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).

Dilution Calculator

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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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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