ABT-737

For research use only. Not for use in humans.

Catalog No.S1002

212 publications

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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Selleck's ABT-737 has been 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  MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnLmNlUxKG6PwrC= NXuyVokxPzJiaB?= NUTxbpp7TE2VTx?= NFHpZXhk[XW|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>? NXrDVFZjOjZ4NUeyPFg>
KG1a M2rGNGNmdGxiVnnhZoltcXS7IFHzd4F6 M37ieVAuOTBizszN MV[yOEBp NV3FVGdxTE2VTx?= MonZTWM2OD15Lk[4JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWiyOlU2OjdzMh?=
Kasumi-1 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3fYRVAuOTBizszN NEjLVWEzPCCq M4HDbWROW09? NXnRfoY{UUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MV6yOlU2OjdzMh?=
KG1a MV3BdI9xfG:|aYOgRZN{[Xl? MkXrNE0yOCEQvF2= Mom5NlQhcA>? NE\HOmpFVVOR MnGybY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXOyOlU2OjdzMh?=
Kasumi-1 M3j6c2Fxd3C2b4Ppd{BCe3OjeR?= NV21ZVNtOC1zMDFOwG0> NYnXW|hLOjRiaB?= M2PnTmROW09? M1yzfolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFLsVHUzPjV3MkexNi=>
MC-3  MlHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVS1TpJFPS9zMD:yNEDPxE1? MnPVNlQhcA>? NYXBTGhpTE2VTx?= M1TzbolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NH\LPVIzPjR2N{[xOS=>
HN22  MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonyNk42NzdwNT:yNk42KM7:TR?= NV\TS4VqOjRiaB?= M1;M[WROW09? NXfCZ5dQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVTPOmxWOjZ2NEe2NVU>
MC-3  Ml7yRZBweHSxc3nzJGF{e2G7 MkXPOU8yOC9{MDFOwG0> NI\xUIIzPCCq MXXEUXNQ NYj4SngycW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> NGLNdHkzPjR2N{[xOS=>
HN22  NGT4[pVCeG:ydH;zbZMhSXO|YYm= MXSyMlUwPy53L{KyMlUh|ryP Ml[zNlQhcA>? MlPOSG1UVw>? NWPoT4djcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> M1i5ZVI3PDR5NkG1
MOLT-4 Mmr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLBNVAuPTByMDDuUS=> NFfuTG44OiCq MXzEUXNQ MWjJR|UxRTBwMUm4JO69VQ>? NFvEd4kzPjN7MkOzNi=>
RS4;11 NUXB[5l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{izS|ExNTVyMECgcm0> NYXpeFB1PzJiaB?= MXrEUXNQ MmHJTWM2OD1yLkCwNkDPxE1? MWOyOlM6OjN|Mh?=
JURKAT NVXzWW1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\mOJpHOTBvNUCwNEBvVQ>? MUe3NkBp NYPCenhDTE2VTx?= NIrzbolKSzVyPU[2JO69VQ>? NXqxbnY4OjZ|OUKzN|I>
CEM R MontS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTyNVAuPTByMDDuUS=> NXLxTIhUPzJiaB?= NEK3UXlFVVOR M3HGXGlEPTB;NT60JO69VQ>? M3LkR|I3Ozl{M{Oy
CEM S NHvmXYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2xNE02ODByIH7N MXy3NkBp NUjiRlg2TE2VTx?= M4\lWGlEPTB;MUKuNUDPxE1? M1PGRlI3Ozl{M{Oy
MOLT-4 M1v2XGFxd3C2b4Ppd{BCe3OjeR?= MnL1NVAuOTByMDDuUS=> NEnEbYMzPCCq MoHLSG1UVw>? NH3EdZZk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> MV6yOlM6OjN|Mh?=
CEM S MYnBdI9xfG:|aYOgRZN{[Xl? MWCxNE0yODByIH7N M4n2XlI1KGh? MnfwSG1UVw>? MUHjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= NYDMcIVqOjZ|OUKzN|I>
JURKAT MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfGc49[OTByLUGwNFAhdk1? M4rJZ|Q5KGh? NEjHcnRFVVOR MVTJR|UxRTl3NdMxPU4{KG6P MoKwNlYyPzJ{Nkm=
LOUCY MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3HXYQyODBvMUCwNEBvVQ>? MkTsOFghcA>? MYHEUXNQ MVvJR|UxRTN{LklCtVExNjlibl2= MkHFNlYyPzJ{Nkm=
WM-115 NFfxb|FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlT0NVAxyqCwTR?= M2PFN|czKGh? MmnK[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? NVK4S3hXOjZzMU[3O|Y>
B16 MljsR4VtdCCYaXHibYxqfHliQYPzZZk> NWXkRVZrOTBywrDuUS=> NH;BSJQ4OiCq NFPucIpmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= MlzUNlYyOTZ5N{[=
HL-60  NXjjTHNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nNOFczKGh? NGGzeFVKSzVywrC9JFExNjdibl2= NEPWTZIzPjB2NU[wPS=>
MOLM-13  M3\zbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFThfoI4OiCq Ml6zTWM2OMLiPTCyO{46KG6P NWLS[3BQOjZyNEW2NFk>
OCI-AML3 NIe4cYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\6O|IhcA>? MkLQTWM2OMLiPTCxPVUxKG6P MYSyOlA1PTZyOR?=
BCWM.1 NVfVTmF1SXCxcITvd4l{KEG|c3H5 MnmxNE0yNjZizszN MnXrNlQhcA>? M2O2N4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MViyOVg6OzJ7MB?=
MWCL-1 NVHUOFFOSXCxcITvd4l{KEG|c3H5 MYSwMVEvPiEQvF2= MmGzNlQhcA>? M4XUfIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NYPEb3FiOjV6OUOyPVA>
MM.1s M3vlNWFxd3C2b4Ppd{BCe3OjeR?= NHHEcFExNTFwNjFOwG0> NUHGOW9XOjRiaB?= MkTnbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NUG3boIyOjV6OUOyPVA>
HCT116 NHn1[YFHfW6ldHnvckBCe3OjeR?= NITjdnQ{NzFyIN88US=> MnTqNVLDqGkEoB?= MkLxSG1UVw>? NEX6WVZqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= M3zMS|I2PzF3MEK4
HCT116 BAX BAK1 DKO M1fRemZ2dmO2aX;uJGF{e2G7 NEniZZc{NzFyIN88US=> NHrxc4QyOsLiaNMg MY\EUXNQ MlfBbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w MUCyOVcyPTB{OB?=
HCT116 MVHGeY5kfGmxbjDBd5NigQ>? MlnPNVAh|ryP NVL2[JQ5OTMEoHlCpC=> MUfEUXNQ Mo\kbY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= NWXUPXE{OjV5MUWwNlg>
HCT116 BAX BAK1 DKO MWfGeY5kfGmxbjDBd5NigQ>? MXyxNEDPxE1? Mkm1NVLDqGkEoB?= M2Swb2ROW09? NVHwdFBRcW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MUSyOVcyPTB{OB?=
HCT116 MWPBeZRweGijZ4mgRZN{[Xl? MnrsNVAh|ryP NFHEUXoyOsLiaNMg NXjm[XVHTE2VTx?= M4nNV4lv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm NH[2TGEzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO MYfBeZRweGijZ4mgRZN{[Xl? NHraUVgyOCEQvF2= NHXpW2kyOsLiaNMg NEHwPGtFVVOR NVvUO5RUcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? NX3jeFBYOjV5MUWwNlg>
U937 NYfjcYdISXCxcITvd4l{KEG|c3H5 NIjLfm0xNjF{NT2yJO69VQ>? NWPvfJBjOjRiaB?= NFzPNopmdmijbnPld{BFUEFxWD2xNU1qdmS3Y3XkJIFxd3C2b4Ppdy=> M3[5XlI2PzF2MEK0
U937  NYWxe5R3SXCxcITvd4l{KEG|c3H5 M4DDZlAvPSEQvF2= NIjQS3MzPCCq MmfW[Y5p[W6lZYOgZ4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[U0{KGG|IIflcIwh[XNiTn;4ZUBt\X[nbB?= MWSyOVcyPDB{NB?=
HL-60 AAA-Bcl-2 NWToOYxFSXCxcITvd4l{KEG|c3H5 MV2wMVUh|ryP NEjleYQ1QCCq MWDJR|UxRTBwOEeg{txu97zOaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYn6NVJ4OjV5MUG0OlA>
HL-60 EEE-Bcl-2 MUPBdI9xfG:|aYOgRZN{[Xl? NV[wUFFkOC13IN88US=> M1jsZlQ5KGh? MUfJR|UxRTVizszt89yNKGmwZIXj[ZMh[2WubDDhdI9xfG:|aYOgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M3rvVVI2PzFzNE[w
U87 M2DWZWZ2dmO2aX;uJGF{e2G7 NE[yVpA2OCEQvF2= MXyyOEBp MYTy[YR2[2W|IITo[UBuWk6DIHX4dJJme3Orb36gcIV3\Wy|IH;mJG1OWC1{LDDNUXAuOTRiYX7kJGJkdC1{ NYH2V5ZVOjV4Nke2OlM>
K562 NWHTVFFTS2WubDDWbYFjcWyrdImgRZN{[Xl? M4jyT|EuOTBizszN M4TYOVQ5KGh? M1XWR2ROW09? NXv1c3FWUUN3ME2yOk44KM7:TR?= M4f1blI2PTl4NU[x
K562/Mcl -1-IRESBim NVy3dWp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L1emlEPTB;OT6zJO69VQ>? NIH6OoIzPTV|NUmwNC=>
K562/Bcl- 2-IRESBim NY\tUnJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTxeZVKSzVyPUCuN|Uh|ryP MkGzNlU2OzV7MEC=
Jurkat NUXH[|VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDtenpPUUN3ME2wMlY3KM7:TR?= M2TTclI2PTN3OUCw
JurkatΔBak NUPRcHJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnQeWg{UUN3ME61NEDPxE1? MWCyOVU{PTlyMB?=
HL60/VCR NGXScnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHGSoFKSzVyPkGwNEDPxE1? M4fXU|I2PTN3OUCw
Kasumi-1 MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvBRWdKSzVyPUCuNFEh|ryP MX6yOVU{PTlyMB?=
Kasumi-1/ABT NFzwNFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;xTWM2OD1yLkWxJO69VQ>? NIrESpozPTV|NUmwNC=>
THP-1 NYq4NGpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\WTWM2OD1zLkK3JO69VQ>? NH\kXJMzPTV|NUmwNC=>
U937 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLlWI5KSzVyPUWuNlkh|ryP MYKyOVU{PTlyMB?=
C1498 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjqepVYUUN3ME22MlE{KM7:TR?= MVSyOVU{PTlyMB?=
RPMI 8226 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnJ[YFKSzVyPUCuNlUh|ryP NGjKT|IzPTV|NUmwNC=>
MM.1S NInJV4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHZTWM2OD1yLkSwJO69VQ>? MmPFNlU2OzV7MEC=
NCI-H929 NHvjTYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nkNGlEPTB;MUWuNlEh|ryP M3zWNVI2PTN3OUCw
U266 M1nUSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:xbWVLUUN3ME2wMlY5KM7:TR?= M1rldlI2PTN3OUCw
MCF-7 NVXKR3VxS2WubDDWbYFjcWyrdImgRZN{[Xl? NUXEbZY2PSEQvF2= M{jUbFQ5KGh? MWXEUXNQ MWnlcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v M4ryb|I2PDB7MUK0
MCF-7 M{C5bGFxd3C2b4Ppd{BCe3OjeR?= MlnNOUDPxE1? NXTKSIpLPC9{ND:0PEBp NXe2e3JITE2VTx?= Mo\tbY5kemWjc3XzJJRp\SClbHXheoVlKFCDUmC= MXKyOVQxQTF{NB?=
MCF-7 MWPGeY5kfGmxbjDBd5NigQ>? M2fseVUh|ryP M17tXVI1KGh? M17EfmROW09? M2fzRoVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NWLFSpYxOjV2MEmxNlQ>
MDA-MB 231  Mn;4SpVv[3Srb36gRZN{[Xl? M3\3ZVUh|ryP NG[1OW8zPCCq M{X4W2ROW09? Mnj0[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh MnfjNlU1ODlzMkS=
ZR-75-1  Mn;PSpVv[3Srb36gRZN{[Xl? MmjDOUDPxE1? M2HvRVI1KGh? Mn;3SG1UVw>? M2PkXYVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? M{j5NFI2PDB7MUK0
A549 M133W2NmdGxiVnnhZoltcXS7IFHzd4F6 NIG3VJgxNTJyIN88US=> M4PyVVczKGh? MV\EUXNQ M2Swc4Rm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M{nte|I2Ozh6N{[y
H1299 M2DGUGNmdGxiVnnhZoltcXS7IFHzd4F6 NEewNHgxNTJyIN88US=> NYnOSXdwPzJiaB?= M{XicmROW09? MYPk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NWHqbmoyOjV|OEi3OlI>
HO-8910 M1XBWGNmdGxiVnnhZoltcXS7IFHzd4F6 MnPHNE0zOCEQvF2= NUTiPZZyPzJiaB?= M2X0WGROW09? M1zXU4Rm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? MUKyOVM5QDd4Mh?=
HT-29 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1vQWVAuOjBizszN M3XYbFczKGh? M{jQUmROW09? MUDk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NHfmWlQzPTN6OEe2Ni=>
HCT-116 MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHTJeZMxNTJyIN88US=> MoHiO|IhcA>? MmewSG1UVw>? MojM[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? MUKyOVM5QDd4Mh?=
A549 MmnxRZBweHSxc3nzJGF{e2G7 M1G0ZlIxKM7:TR?= M1LaNFQ5KGh? M3XGUmROW09? MWDpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NUjueHJROjV|OEi3OlI>
H1299 NIewNZVCeG:ydH;zbZMhSXO|YYm= MXWyNEDPxE1? MVS0PEBp MlvTSG1UVw>? NXXSZnZHcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> MojZNlU{QDh5NkK=
Sc-1 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFXjdlQxNjByMEGtNUDPxE1? M174NVk3KGh? MVXk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2f4dlI2Ozd|NUC4
OcI-LY18 NWjKXWhCS2WubDDWbYFjcWyrdImgRZN{[Xl? MYewMlAxODFvMTFOwG0> NIq3XVI6PiCq Mn:1[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmPrNlU{PzN3MEi=
RL  M3S1[mNmdGxiVnnhZoltcXS7IFHzd4F6 MVWwMlAxODFvMTFOwG0> Mn\tPVYhcA>? NEXsb4tl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mo\RNlU{PzN3MEi=
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Clone A MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF31VZQxNjMkgKO2NEDPxE1? M3PYb|czKGh? MnnaSG1UVw>? M33nW2lEPTB;Nz61JO69VQ>? MYmyOVIxQDh6Mh?=
CX-1 MnO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\0[nJiOC5{4pETOlAh|ryP NGixR2c4OiCq M2TYXGROW09? MnjRTWM2OD1zLkig{txO NYWxSHlWOjV{MEi4PFI>
LS174T MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnkNE4z6oDVNkCg{txO NHjJZW84OiCq NV3jb|BPTE2VTx?= MUPJR|UxRTF6LkOg{txO MUKyOVIxQDh6Mh?=
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SW480 MnrwRZBweHSxc3nzJGF{e2G7 MnHjNU82NzFyIN88US=> MV60PEBp M4nvSINifXOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MWqyOVE6OjF6OB?=
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UM-SCC22B NXrMNVZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvwWld4PzJiaB?= MWjEUXNQ NFPsbI1IUTVyPUG5JOKyKDJwOTFOwG0> MVKyOVE{QTN6Nx?=
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RPMI-8226  MlP2RZBweHSxc3nzJGF{e2G7 M164VFEzPS9{NUCvOVAxKG6P NGnqOI81QGkEoB?= NGHGSoJFVVOR M{[2O4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnvVNlUxODh{MEK=
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RS4;11 NVvnVFVOTnWwY4Tpc44hSXO|YYm= NYOyXmplOTByIH7N Mnv2NU8{NzZiaB?= NIHMN2RFVVOR MorGbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDNZ4wuOSClbHXheoFo\Q>? M{Do[VI1QTVzNEey

... 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
Smiles CN(C)CCC(CSC1=CC=CC=C1)NC2=CC=C(C=C2[N+]([O-])=O)[S](=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=C(C=CC=C5)C6=CC=C(Cl)C=C6

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
    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):
    C6=C5/X C6: LOG(C6):
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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