ABT-737

For research use only.

Catalog No.S1002

272 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 272 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  M{XleWNmdGxiVnnhZoltcXS7IFHzd4F6 NXGyR5YxOjVyIH7NxsA> MYG3NkBp MVXEUXNQ MUjjZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRmNNPiC|aWLORS=> Mm\iNlY3PTd{OEi=
KG1a NGDEO5lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXLScolMOC1zMDFOwG0> MmK4NlQhcA>? NIK4TnJFVVOR Ml:yTWM2OD15Lk[4JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NITtN2szPjV3MkexNi=>
Kasumi-1 MoDUR4VtdCCYaXHibYxqfHliQYPzZZk> MYewMVExKM7:TR?= NHyzdnYzPCCq MV;EUXNQ NX[3foRJUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NILmVG8zPjV3MkexNi=>
KG1a M13CNGFxd3C2b4Ppd{BCe3OjeR?= NE[1U5AxNTFyIN88US=> NFTBNI8zPCCq NVjJXHQxTE2VTx?= NVK4S5l{cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Mn7kNlY2PTJ5MUK=
Kasumi-1 NITT[I1CeG:ydH;zbZMhSXO|YYm= NEjPco8xNTFyIN88US=> NUSzfVVwOjRiaB?= M1u5O2ROW09? MkPwbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYG1bpBHOjZ3NUK3NVI>
MC-3  NF22XmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq1dGs2NzFyL{KwJO69VQ>? NFPrOJkzPCCq MmS2SG1UVw>? MXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1zkS|I3PDR5NkG1
HN22  MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT5T|Q1Oi53L{euOU8zOi53IN88US=> MYSyOEBp MmDoSG1UVw>? MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYLodWRqOjZ2NEe2NVU>
MC-3  MXjBdI9xfG:|aYOgRZN{[Xl? MonuOU8yOC9{MDFOwG0> MV2yOEBp NVjzeIw4TE2VTx?= NGPzb2tqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz MYGyOlQ1PzZzNR?=
HN22  M2X0dmFxd3C2b4Ppd{BCe3OjeR?= NHv6cIEzNjVxNz61M|IzNjVizszN M1T5ZlI1KGh? M2C3RWROW09? NWi2WZBrcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> M1rCVlI3PDR5NkG1
MOLT-4 NIPlSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\3RpIyOC13MECwJI5O NHHXOm44OiCq MXjEUXNQ MmP6TWM2OD1yLkG5PEDPxE1? Mk\JNlY{QTJ|M{K=
RS4;11 NFzxS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTaNGZoOTBvNUCwNEBvVQ>? NUTxdnJ{PzJiaB?= NHPpS41FVVOR M4[2SGlEPTB;MD6wNFIh|ryP MUSyOlM6OjN|Mh?=
JURKAT NHXjXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK3NW4yOC13MECwJI5O MmTEO|IhcA>? MULEUXNQ MonCTWM2OD14NjFOwG0> MViyOlM6OjN|Mh?=
CEM R MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnzZpYyOC13MECwJI5O NU\xO2hOPzJiaB?= M3zWSmROW09? MXvJR|UxRTVwNDFOwG0> NVzaXYwzOjZ|OUKzN|I>
CEM S Mn\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3vXnRvOTBvNUCwNEBvVQ>? M33MdVczKGh? MY\EUXNQ NYLIS2F2UUN3ME2xNk4yKM7:TR?= MmD4NlY{QTJ|M{K=
MOLT-4 Mn;oRZBweHSxc3nzJGF{e2G7 MknTNVAuOTByMDDuUS=> MYKyOEBp NVyzeFl2TE2VTx?= NFvYS2pk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> NIDqSnEzPjN7MkOzNi=>
CEM S MV;BdI9xfG:|aYOgRZN{[Xl? MmO3NVAuOTByMDDuUS=> MX6yOEBp MWDEUXNQ NFTySY5k[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> M3jwVVI3Ozl{M{Oy
JURKAT MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYmxNFAuOTByMDDuUS=> MkXnOFghcA>? M1HPVmROW09? NEjORYdKSzVyPUm1OeKyQS5|IH7N NITVV3AzPjF5MkK2PS=>
LOUCY M1r0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDMPVE3OTByLUGwNFAhdk1? M{fKdVQ5KGh? NX;weoZMTE2VTx?= M{\vTmlEPTB;M{KuPOKyOTBwOTDuUS=> M{i5UVI3OTd{Mk[5
WM-115 M1XOPGNmdGxiVnnhZoltcXS7IFHzd4F6 M2P4[FExOMLibl2= MoW5O|IhcA>? NEn6[pdmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= MUSyOlEyPjd5Nh?=
B16 NUjoW3pSS2WubDDWbYFjcWyrdImgRZN{[Xl? NX7rOHk1OTBywrDuUS=> M3TIVVczKGh? M4\nUoVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi M1nLelI3OTF4N{e2
HL-60  MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\XdnE4OiCq MWPJR|UxyqB;IEGwMlchdk1? NX7ldW9iOjZyNEW2NFk>
MOLM-13  NH3EVphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjJbFU4OiCq M4XvemlEPTEEoE2gNlcvQSCwTR?= MUiyOlA1PTZyOR?=
OCI-AML3 MnnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTVO|IhcA>? NHXkXplKSzVywrC9JFE6PTBibl2= NHH1[2szPjB2NU[wPS=>
BCWM.1 NVH6VZZLSXCxcITvd4l{KEG|c3H5 MnG0NE0yNjZizszN NXHCTHdHOjRiaB?= M2r4VYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M1vSWlI2QDl|Mkmw
MWCL-1 NYjscJVmSXCxcITvd4l{KEG|c3H5 MX6wMVEvPiEQvF2= MnPjNlQhcA>? MoXBbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MVmyOVg6OzJ7MB?=
MM.1s M{HqZWFxd3C2b4Ppd{BCe3OjeR?= M1H6VFAuOS54IN88US=> MmjtNlQhcA>? MkTubY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? Mn\uNlU5QTN{OUC=
HCT116 NX6wW5VmTnWwY4Tpc44hSXO|YYm= MlWyN{8yOCEQvF2= M4LsfFEzyqCqwrC= Mn;5SG1UVw>? MWHpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? NYDo[3k2OjV5MUWwNlg>
HCT116 BAX BAK1 DKO NYXLUGxjTnWwY4Tpc44hSXO|YYm= MknON{8yOCEQvF2= MoDiNVLDqGkEoB?= Mk\SSG1UVw>? Mme0bY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w MnTRNlU4OTVyMki=
HCT116 NFW5W|dHfW6ldHnvckBCe3OjeR?= MXmxNEDPxE1? NFfYcZMyOsLiaNMg NEnmV2lFVVOR NU\qe41ScW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MkOyNlU4OTVyMki=
HCT116 BAX BAK1 DKO MXXGeY5kfGmxbjDBd5NigQ>? M{C1[|ExKM7:TR?= NIG0NnoyOsLiaNMg Ml3JSG1UVw>? M3O1RYlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= M1q0cFI2PzF3MEK4
HCT116 NW\vbJNUSXW2b4DoZYd6KEG|c3H5 MmXwNVAh|ryP MoP1NVLDqGkEoB?= M4jOTGROW09? MmCzbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> Mlm5NlU4OTVyMki=
HCT116 BAX BAK1 DKO NYKxbVBjSXW2b4DoZYd6KEG|c3H5 Ml\2NVAh|ryP NHH4R4cyOsLiaNMg MlzvSG1UVw>? NVSxSY12cW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? MYeyOVcyPTB{OB?=
U937 M1XYemFxd3C2b4Ppd{BCe3OjeR?= MlfVNE4yOjVvMjFOwG0> NUf5OlBLOjRiaB?= Ml\R[Y5p[W6lZYOgSGhCN1hvMUGtbY5lfWOnZDDhdI9xfG:|aYO= NVTmeVBXOjV5MUSwNlQ>
U937  NFnodIFCeG:ydH;zbZMhSXO|YYm= MVmwMlUh|ryP NWnudFZVOjRiaB?= MY\lcohidmOnczDjcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlMVMh[XNid3XscEBieyCQb4jhJIxmfmWu MWqyOVcyPDB{NB?=
HL-60 AAA-Bcl-2 Mnz3RZBweHSxc3nzJGF{e2G7 M{L5TlAuPSEQvF2= MV60PEBp MVjJR|UxRTBwOEeg{txu97zOaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV;V[W85OjV5MUG0OlA>
HL-60 EEE-Bcl-2 MlfNRZBweHSxc3nzJGF{e2G7 NILLSXExNTVizszN NFLKNZc1QCCq NYLwTGNqUUN3ME21JO69de,:jDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXjUe2ZOOjV5MUG0OlA>
U87 Ml[2SpVv[3Srb36gRZN{[Xl? NFLB[pI2OCEQvF2= M2fIclI1KGh? MVry[YR2[2W|IITo[UBuWk6DIHX4dJJme3Orb36gcIV3\Wy|IH;mJG1OWC1{LDDNUXAuOTRiYX7kJGJkdC1{ NHGzXHEzPTZ4N{[2Ny=>
K562 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NX;NSWEyOS1zMDFOwG0> MnPEOFghcA>? MYPEUXNQ MkK2TWM2OD1{Nj63JO69VQ>? NYTWZZY6OjV3OU[1OlE>
K562/Mcl -1-IRESBim NG\jTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DuVGlEPTB;OT6zJO69VQ>? M{H1TlI2PTN3OUCw
K562/Bcl- 2-IRESBim M3PlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LCeGlEPTB;MD6zOUDPxE1? NEPlSHIzPTV|NUmwNC=>
Jurkat NXToZ5BuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vO[GlEPTB;MD62OkDPxE1? M1q1dFI2PTN3OUCw
JurkatΔBak NWr2fGh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjVZoJKSzVyPkWwJO69VQ>? MX2yOVU{PTlyMB?=
HL60/VCR M17G[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTqc5lCUUN3ME6xNFAh|ryP Mm\NNlU2OzV7MEC=
Kasumi-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHhTWM2OD1yLkCxJO69VQ>? NYfYZYF3OjV3M{W5NFA>
Kasumi-1/ABT M3frNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PsPWlEPTB;MD61NUDPxE1? MVOyOVU{PTlyMB?=
THP-1 MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHOTWM2OD1zLkK3JO69VQ>? M{fUblI2PTN3OUCw
U937 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P3cGlEPTB;NT6yPUDPxE1? NWi1UXFMOjV3M{W5NFA>
C1498 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PNT2lEPTB;Nj6xN{DPxE1? NGmyPJYzPTV|NUmwNC=>
RPMI 8226 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwMkWg{txO M1HZ[FI2PTN3OUCw
MM.1S NVf2Z2hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfVPZA5UUN3ME2wMlQxKM7:TR?= NIXZNVQzPTV|NUmwNC=>
NCI-H929 NHvkZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPzTWM2OD1zNT6yNUDPxE1? NUTkNHM3OjV3M{W5NFA>
U266 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LYN2lEPTB;MD62PEDPxE1? MUOyOVU{PTlyMB?=
MCF-7 NUjBVJZ1S2WubDDWbYFjcWyrdImgRZN{[Xl? NH65Sm82KM7:TR?= MmX6OFghcA>? NWTMbZVrTE2VTx?= M13aUYVvcGGwY3XzJJRp\SC|ZX7zbZRqfmm2eTD0c{BweiC{YXTpZZRqd25? NXHpdXhMOjV2MEmxNlQ>
MCF-7 NE\qc2tCeG:ydH;zbZMhSXO|YYm= NYnaOVFxPSEQvF2= MXS0M|I1NzR6IHi= NIPrRmJFVVOR MWTpcoNz\WG|ZYOgeIhmKGOuZXH2[YQhWEGUUB?= NGLzNoQzPTRyOUGyOC=>
MCF-7 M4nXZWZ2dmO2aX;uJGF{e2G7 MYC1JO69VQ>? Mo\5NlQhcA>? NV\xdGNqTE2VTx?= NFy1WmNmdmijbnPld{B1cGWuZY\lcEBw\iCPY3ytNUBmgHC{ZYPzbY9vyqB? MnnrNlU1ODlzMkS=
MDA-MB 231  NWWw[Ip5TnWwY4Tpc44hSXO|YYm= M4W3flUh|ryP MVuyOEBp M4mwVWROW09? MYDlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> MlzZNlU1ODlzMkS=
ZR-75-1  MoDFSpVv[3Srb36gRZN{[Xl? NF;Beo02KM7:TR?= NWLVV3k6OjRiaB?= NHfscmxFVVOR NWmzZ5B5\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi M4rj[|I2PDB7MUK0
A549 NYrQdm5tS2WubDDWbYFjcWyrdImgRZN{[Xl? NIDwUpIxNTJyIN88US=> MUi3NkBp MkjwSG1UVw>? NF7oSHNl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw MmKwNlU{QDh5NkK=
H1299 MnTNR4VtdCCYaXHibYxqfHliQYPzZZk> NXy1bJQ5OC1{MDFOwG0> MVi3NkBp M1T2NmROW09? MW\k[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NXfNbGJIOjV|OEi3OlI>
HO-8910 NGHYOJNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3T1Z|AuOjBizszN Mn\vO|IhcA>? NGf0UY9FVVOR MXPk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv M1z6[|I2Ozh6N{[y
HT-29 MV\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH:5UZQxNTJyIN88US=> NFO1W5Q4OiCq MYjEUXNQ NEnaWIll\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NYPWRXlwOjV|OEi3OlI>
HCT-116 NEflR2ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX[1SWU{OC1{MDFOwG0> MoH0O|IhcA>? NXrpTmY1TE2VTx?= NEfjSJJl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw MXKyOVM5QDd4Mh?=
A549 NHj0NXdCeG:ydH;zbZMhSXO|YYm= NF3McHkzOCEQvF2= NX;0SZNKPDhiaB?= MVXEUXNQ MXPpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NVLZTYt5OjV|OEi3OlI>
H1299 MkTLRZBweHSxc3nzJGF{e2G7 M3fNbVIxKM7:TR?= MYS0PEBp NX31dVhETE2VTx?= MkHSbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoaXPhcpRtgSClb33ibY5m\CC5aYToJIF{eGm{aX6= M4XPOVI2Ozh6N{[y
Sc-1 NXPhUZZjS2WubDDWbYFjcWyrdImgRZN{[Xl? NHzwRmUxNjByMEGtNUDPxE1? MofpPVYhcA>? M2TT[YRm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWLjdFdUOjV|N{O1NFg>
OcI-LY18 NGD5[lFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUWwMlAxODFvMTFOwG0> MU[5OkBp NHrhSVBl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX3UfoxCOjV|N{O1NFg>
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Clone A NFr1TINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmwMlLjiJN4MDFOwG0> NWjnRWN3PzJiaB?= MWHEUXNQ MVPJR|UxRTdwNTFOwG0> MXSyOVIxQDh6Mh?=
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UM-SCC22B MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojCO|IhcA>? NHKzSoFFVVOR MkXZS2k2OD1zOTFCtUAzNjlizszN NIrtS|MzPTF|OUO4Oy=>
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OPM-2  M1rLSWNmdGxiVnnhZoltcXS7IFHzd4F6 M{T5VlEzPS9{NUCvOVAxKG6P MWm0PIjDqA>? NF;lb|ZFVVOR M17hVYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M3XVelI2ODB6MkCy
RPMI-8226  MVHBdI9xfG:|aYOgRZN{[Xl? NHTxSlEyOjVxMkWwM|UxOCCwTR?= NVLD[JJuPDiqwrC= NHL1XFlFVVOR MnS1bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWPENHVsOjVyMEiyNFI>
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COG-LL-319 NIHDT2hHfW6ldHnvckBCe3OjeR?= Mn;uNVAxKG6P MXqxM|MwPiCq MWHEUXNQ NW\yc4ZQcW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBO[2xvMTDjcIVifmGpZR?= Mn3rNlQ6PTF2N{K=
RS4;11 NIj1PZhHfW6ldHnvckBCe3OjeR?= MmrBNVAxKG6P NYTlT3RwOS9|L{[gbC=> MUnEUXNQ MXrpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IF3jcE0yKGOuZXH2ZYdm M4L1blI1QTVzNEey

... 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
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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
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    C2
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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):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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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

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

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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