ABT-737

For research use only.

Catalog No.S1002

307 publications

ABT-737 Chemical Structure

CAS No. 852808-04-9

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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

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Selleck's ABT-737 has been cited by 307 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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. 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  Mne0R4VtdCCYaXHibYxqfHliQYPzZZk> NYn1cG83OjVyIH7NxsA> Mn;TO|IhcA>? M3vT[GROW09? MXPjZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRmNNPiC|aWLORS=> NWHlOmxYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVczQDhpPkK2OlU4Ojh6PD;hQi=>
KG1a NFrFbXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYH1PXM4OC1zMDFOwG0> MXSyOEBp Mn35SG1UVw>? NGPldmRKSzVyPUeuOlgh|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIHCbYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW1NlcyOid-Mk[1OVI4OTJ:L3G+
Kasumi-1 MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1XhWFAuOTBizszN MYSyOEBp NE\uXW5FVVOR M{DHfGlEPTB;ND64O{DPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3MkexNkc,OjZ3NUK3NVI9N2F-
KG1a NVjsOZh[SXCxcITvd4l{KEG|c3H5 NGrGUYYxNTFyIN88US=> MlXpNlQhcA>? M2L1RmROW09? NGH0O2NqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3MkexNkc,OjZ3NUK3NVI9N2F-
Kasumi-1 MWPBdI9xfG:|aYOgRZN{[Xl? MlzyNE0yOCEQvF2= M{PoPVI1KGh? NFXLbJFFVVOR MnnEbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3MkexNkc,OjZ3NUK3NVI9N2F-
MC-3  NYrs[3lGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzlOU8yOC9{MDFOwG0> MViyOEBp M3jxdWROW09? M2TyRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{nmTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O|YyPTxxYU6=
HN22  MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG3Nk42NzdwNT:yNk42KM7:TR?= MkT3NlQhcA>? MX;EUXNQ NIDXeFdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
MC-3  MYfBdI9xfG:|aYOgRZN{[Xl? NYm4XGI4PS9zMD:yNEDPxE1? M13se|I1KGh? NGPsPYNFVVOR Mlf6bY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
HN22  NH;kSnFCeG:ydH;zbZMhSXO|YYm= M4m2XlIvPS95LkWvNlIvPSEQvF2= MnzaNlQhcA>? MYjEUXNQ NE[3UmdqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz NXnlZVNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0OFc3OTVpPkK2OFQ4PjF3PD;hQi=>
MOLT-4 NF7qSJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPGNVAuPTByMDDuUS=> NITX[Xo4OiCq Mk\aSG1UVw>? MUDJR|UxRTBwMUm4JO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
RS4;11 NXmyV|I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jDS|ExNTVyMECgcm0> NIXodoU4OiCq MVzEUXNQ NEXhXFdKSzVyPUCuNFAzKM7:TR?= NW[wdZZtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVI{OzJpPkK2N|kzOzN{PD;hQi=>
JURKAT NG[0NHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\LTVExNTVyMECgcm0> M2G4[VczKGh? M1jqVWROW09? NH;0VlFKSzVyPU[2JO69VQ>? MkDnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
CEM R Mke3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3WSI9ROTBvNUCwNEBvVQ>? M33EcFczKGh? MkiwSG1UVw>? MYfJR|UxRTVwNDFOwG0> NYPvfWtpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVI{OzJpPkK2N|kzOzN{PD;hQi=>
CEM S NILH[GRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHHTos6OTBvNUCwNEBvVQ>? MXi3NkBp MkHuSG1UVw>? MYrJR|UxRTF{LkGg{txO NI\3VZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
MOLT-4 MmPJRZBweHSxc3nzJGF{e2G7 MVWxNE0yODByIH7N MYOyOEBp M{jV[GROW09? M17vTYNifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x M3\YTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
CEM S NXP5UFVSSXCxcITvd4l{KEG|c3H5 M1;ablExNTFyMECgcm0> MVqyOEBp M2\YZmROW09? NIX0TXdk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
JURKAT MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWxNFAuOTByMDDuUS=> MU[0PEBp M1PnOmROW09? Mn\hTWM2OD17NUZCtVkvOyCwTR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF5MkK2PUc,OjZzN{KyOlk9N2F-
LOUCY NXLscnA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEK1bJAyODBvMUCwNEBvVQ>? NGjwT|M1QCCq MkDpSG1UVw>? M1TwRmlEPTB;M{KuPOKyOTBwOTDuUS=> NIjmOZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG3NlI3QSd-Mk[xO|IzPjl:L3G+
WM-115 MnfMR4VtdCCYaXHibYxqfHliQYPzZZk> M1OyeFExOMLibl2= MlniO|IhcA>? NETSR3BmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNke3Okc,OjZzMU[3O|Y9N2F-
B16 MXHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoPyNVAxyqCwTR?= MVS3NkBp M{S1ZoVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi NFf4RWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlc4Pid-Mk[xNVY4PzZ:L3G+
HL-60  NYHuVmMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TsfFczKGh? MWLJR|UxyqB;IEGwMlchdk1? MojCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNEW2NFkoRjJ4MES1OlA6RC:jPh?=
MOLM-13  MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\OcZg4OiCq M2LM[2lEPTEEoE2gNlcvQSCwTR?= M1;6V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES1OlA6Lz5{NkC0OVYxQTxxYU6=
OCI-AML3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jt[|czKGh? Mn7vTWM2OMLiPTCxPVUxKG6P MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2NU[wPUc,OjZyNEW2NFk9N2F-
BCWM.1 NV[ze|FWSXCxcITvd4l{KEG|c3H5 M{Lre|AuOS54IN88US=> MUKyOEBp MofQbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MnrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6OUOyPVAoRjJ3OEmzNlkxRC:jPh?=
MWCL-1 NITYbYpCeG:ydH;zbZMhSXO|YYm= MUKwMVEvPiEQvF2= NFfTWFAzPCCq MlvHbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NV7NOZVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4PVMzQTBpPkK1PFk{OjlyPD;hQi=>
MM.1s MXfBdI9xfG:|aYOgRZN{[Xl? NGT3NIoxNTFwNjFOwG0> NVHHTZE1OjRiaB?= M1ToVYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MkfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6OUOyPVAoRjJ3OEmzNlkxRC:jPh?=
HCT116 NXz0doxsTnWwY4Tpc44hSXO|YYm= NVewfW5FOy9zMDFOwG0> NF;sbVQyOsLiaNMg NUTIepE2TE2VTx?= NVzhW4JTcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u MoPTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116 BAX BAK1 DKO NXWzdoh4TnWwY4Tpc44hSXO|YYm= MXezM|ExKM7:TR?= Mo\lNVLDqGkEoB?= MUfEUXNQ NHXN[IFqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= MmfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116 MmLqSpVv[3Srb36gRZN{[Xl? Mn3GNVAh|ryP NHTxeZAyOsLiaNMg M4DmTmROW09? MmrCbY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= NIPmeFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 BAX BAK1 DKO NHPLXpNHfW6ldHnvckBCe3OjeR?= MnHGNVAh|ryP M{XsfFEzyqCqwrC= M13ROGROW09? Mmq4bY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNUCyPEc,OjV5MUWwNlg9N2F-
HCT116 NHfTSZlCfXSxcHjh[5khSXO|YYm= NHfJN4oyOCEQvF2= MlXkNVLDqGkEoB?= M3XVUmROW09? NFfmTJlqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? NEHIO2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 BAX BAK1 DKO NXLzdoY4SXW2b4DoZYd6KEG|c3H5 MlrRNVAh|ryP MmXXNVLDqGkEoB?= NUDnbIlNTE2VTx?= M1rWRYlv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm NGTJdY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
U937 NXW1fnRxSXCxcITvd4l{KEG|c3H5 NXrOOo11OC5zMkWtNkDPxE1? MVuyOEBp NUPl[odT\W6qYX7j[ZMhTEiDL2itNVEucW6mdXPl[EBieG:ydH;zbZM> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNECyOEc,OjV5MUSwNlQ9N2F-
U937  M1:xO2Fxd3C2b4Ppd{BCe3OjeR?= NHP6XYExNjVizszN NFLsU2YzPCCq NWfxN3BQ\W6qYX7j[ZMh[2ynYY\h[4Uhd2ZiUFHSVEBidmRiY3HzdIF{\S1|IHHzJJdmdGxiYYOgUo95[SCuZY\lcC=> MmXrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUSwNlQoRjJ3N{G0NFI1RC:jPh?=
HL-60 AAA-Bcl-2 NIPFeoZCeG:ydH;zbZMhSXO|YYm= MnG0NE02KM7:TR?= MmXpOFghcA>? Mo\0TWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzMUS2NEc,OjV5MUG0OlA9N2F-
HL-60 EEE-Bcl-2 NELPcFdCeG:ydH;zbZMhSXO|YYm= M2X0SFAuPSEQvF2= NW\Ob5d1PDhiaB?= NVvvd4U{UUN3ME21JO69de,:jDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYrLO3poRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVE1PjBpPkK1O|EyPDZyPD;hQi=>
U87 Mkj2SpVv[3Srb36gRZN{[Xl? MWi1NEDPxE1? NYnRXXJYOjRiaB?= MUfy[YR2[2W|IITo[UBuWk6DIHX4dJJme3Orb36gcIV3\Wy|IH;mJG1OWC1{LDDNUXAuOTRiYX7kJGJkdC1{ NYrwOJBqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2Olc3PjNpPkK1OlY4PjZ|PD;hQi=>
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NB-EBc1 NE[5ZoVyUFSVIHHzd4F6 NXT5SZAyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 M4fFcZFJXFNiYYPzZZk> MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 MmrZdWhVWyCjc4PhfS=> NX;Mb|NpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= M1nEO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 M1XPT5FJXFNiYYPzZZk> NHL2bWtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSjF4NEOgZ4VtdHN? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MWjxTHRUKGG|c3H5 Ml74dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>? M3zrUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32 MWLxTHRUKGG|c3H5 MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz M{DSfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 NFjwR4ZyUFSVIHHzd4F6 NFvtfYJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{ M{TtT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 MXnxTHRUKGG|c3H5 MlzSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ NVHwVW9KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... 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
  • 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):
2%DMSO+40%PEG300+5%Tween80+53%ddH2O
For best results, use promptly after mixing.
2mg/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
Smiles CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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)

  • Mass
    Concentration
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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 )

  • C1
    V1
    C2
    V2

* 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):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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