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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In DMSO USD 384 In stock
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Cited by 120 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  NVniZmlXS2WubDDWbYFjcWyrdImgRZN{[Xl? NHP2T4kzPTBibl5CpC=> NHy5[Zg4OiCq NUnQdm91TE2VTx?= MWPjZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRmNNPiC|aWLORS=> M{fPXFI3PjV5Mki4
KG1a NGnrS|RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVHadm86OC1zMDFOwG0> NF3uO4wzPCCq NHPPS4lFVVOR NU\IO4NuUUN3ME23MlY5KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NIjYd2IzPjV3MkexNi=>
Kasumi-1 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmDsNE0yOCEQvF2= MX2yOEBp MX7EUXNQ NU\IZnVJUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NVSzV4J2OjZ3NUK3NVI>
KG1a MYDBdI9xfG:|aYOgRZN{[Xl? MV:wMVExKM7:TR?= MVKyOEBp MYfEUXNQ NUjS[IN6cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MWSyOlU2OjdzMh?=
Kasumi-1 MUfBdI9xfG:|aYOgRZN{[Xl? NITqR4YxNTFyIN88US=> NF\6N3kzPCCq MYXEUXNQ M2PZeYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVyyOlU2OjdzMh?=
MC-3  M{L6UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7CeHk2NzFyL{KwJO69VQ>? MnmxNlQhcA>? MWHEUXNQ Mn\6bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWCwOI9bOjZ2NEe2NVU>
HN22  MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljxNk42NzdwNT:yNk42KM7:TR?= NFf2SY0zPCCq Mn7tSG1UVw>? NHP1ZWRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYiyOlQ1PzZzNR?=
MC-3  NHi2cnlCeG:ydH;zbZMhSXO|YYm= NUD6bmR7PS9zMD:yNEDPxE1? M1O0S|I1KGh? M3jZSmROW09? NUjIN4JXcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> NYPt[4tbOjZ2NEe2NVU>
HN22  NWPjW5pPSXCxcITvd4l{KEG|c3H5 MVqyMlUwPy53L{KyMlUh|ryP M2nONlI1KGh? M2LJO2ROW09? M2TidIlv\HWlZYOgZ4F{eGG|ZT3t[YRq[XSnZDDhdI9xfG:|aYO= NEDwW5AzPjR2N{[xOS=>
MOLT-4 NV;CdVRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnFNVAuPTByMDDuUS=> NUnjPXhLPzJiaB?= MoHXSG1UVw>? NIrneVdKSzVyPUCuNVk5KM7:TR?= M3PaR|I3Ozl{M{Oy
RS4;11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3GWldvOTBvNUCwNEBvVQ>? NELl[mU4OiCq MUjEUXNQ MkDyTWM2OD1yLkCwNkDPxE1? NGf3ZnIzPjN7MkOzNi=>
JURKAT MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKxNE02ODByIH7N Mo\xO|IhcA>? M2TTS2ROW09? MYrJR|UxRTZ4IN88US=> NWrQXJFROjZ|OUKzN|I>
CEM R NIHyfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4mxTlExNTVyMECgcm0> NFvGflg4OiCq MYXEUXNQ M4PUcWlEPTB;NT60JO69VQ>? NEPJdnEzPjN7MkOzNi=>
CEM S M2npPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\DcYUyOC13MECwJI5O MlrCO|IhcA>? NXrRd|J1TE2VTx?= MlfZTWM2OD1zMj6xJO69VQ>? NEDKUXYzPjN7MkOzNi=>
MOLT-4 Mo\4RZBweHSxc3nzJGF{e2G7 MnTuNVAuOTByMDDuUS=> NI\EVGozPCCq NIHPfXhFVVOR NHvSZ2Fk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> M{exWlI3Ozl{M{Oy
CEM S Mor6RZBweHSxc3nzJGF{e2G7 MmPUNVAuOTByMDDuUS=> NHjWWIIzPCCq M4PqSmROW09? M4rVUINifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x M2f3RlI3Ozl{M{Oy
JURKAT MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm3RYoxOTByLUGwNFAhdk1? Mn3rOFghcA>? NWTGXZE{TE2VTx?= Mn;lTWM2OD17NUZCtVkvOyCwTR?= NE\1TlgzPjF5MkK2PS=>
LOUCY M4rDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDMNVAxNTFyMECgcm0> MXq0PEBp M1\vPGROW09? NWjJSpZ6UUN3ME2zNk45yrFzMD65JI5O Mkj6NlYyPzJ{Nkm=
WM-115 NFTvO|RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVTnTmk2OTBywrDuUS=> MoPqO|IhcA>? MUTlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? MU[yOlEyPjd5Nh?=
B16 M{j5WWNmdGxiVnnhZoltcXS7IFHzd4F6 MlXvNVAxyqCwTR?= MmDjO|IhcA>? NHTLSXlmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= NX\tVohUOjZzMU[3O|Y>
HL-60  NHnjW5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV23NkBp M3jnTWlEPTEEoE2gNVAvPyCwTR?= M4XXXFI3ODR3NkC5
MOLM-13  MnTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHMcpBMPzJiaB?= NVzU[Wc6UUN3MNMgQUAzPy57IH7N NHXleVEzPjB2NU[wPS=>
OCI-AML3 MoPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HsRVczKGh? M12wUmlEPTEEoE2gNVk2OCCwTR?= Mm\5NlYxPDV4MEm=
BCWM.1 MkfBRZBweHSxc3nzJGF{e2G7 NW\NW3E3OC1zLk[g{txO MonaNlQhcA>? M3e4eIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MmHCNlU5QTN{OUC=
MWCL-1 M1\1VmFxd3C2b4Ppd{BCe3OjeR?= NGqxcHExNTFwNjFOwG0> M2PIR|I1KGh? MWjpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MnTPNlU5QTN{OUC=
MM.1s M2rNb2Fxd3C2b4Ppd{BCe3OjeR?= NG\me24xNTFwNjFOwG0> MkW1NlQhcA>? MWTpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NX7UeIVJOjV6OUOyPVA>
HCT116 M1HZXGZ2dmO2aX;uJGF{e2G7 M{DZcFMwOTBizszN NWDvWYVyOTMEoHlCpC=> MX\EUXNQ MUjpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? MWKyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO NWX1W246TnWwY4Tpc44hSXO|YYm= NIrjOok{NzFyIN88US=> M{[2TlEzyqCqwrC= M{fyc2ROW09? MnXWbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w NHG3PHkzPTdzNUCyPC=>
HCT116 M2n3ZmZ2dmO2aX;uJGF{e2G7 MVexNEDPxE1? MmrSNVLDqGkEoB?= MnjzSG1UVw>? NV\JRnpScW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MX[yOVcyPTB{OB?=
HCT116 BAX BAK1 DKO MVHGeY5kfGmxbjDBd5NigQ>? M2rBe|ExKM7:TR?= NGXWUYUyOsLiaNMg NF7ySmxFVVOR NXnDTG04cW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MVmyOVcyPTB{OB?=
HCT116 MkHLRZV1d3CqYXf5JGF{e2G7 NHnLdXAyOCEQvF2= M{DnXlEzyqCqwrC= NUXLVG5CTE2VTx?= NVL0VZJycW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? NEH3NoUzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO M1LFUWF2fG:yaHHnfUBCe3OjeR?= MUGxNEDPxE1? M2PCPVEzyqCqwrC= M4L4cGROW09? MXLpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> NWjlPY9iOjV5MUWwNlg>
U937 NWnKSlh1SXCxcITvd4l{KEG|c3H5 NUnNNJhnOC5zMkWtNkDPxE1? M4nkWFI1KGh? MYflcohidmOnczDETGEwYC1zMT3pcoR2[2WmIHHwc5B1d3Orcx?= MkTTNlU4OTRyMkS=
U937  NY\tUottSXCxcITvd4l{KEG|c3H5 NIThbZcxNjVizszN MV6yOEBp Mnj1[Y5p[W6lZYOgZ4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[U0{KGG|IIflcIwh[XNiTn;4ZUBt\X[nbB?= M13jdlI2PzF2MEK0
HL-60 AAA-Bcl-2 MX3BdI9xfG:|aYOgRZN{[Xl? MkjSNE02KM7:TR?= MVe0PEBp NYLjVXdbUUN3ME2wMlg4KM7:bf-8kIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVXTOXZQOjV5MUG0OlA>
HL-60 EEE-Bcl-2 NYL4[pl[SXCxcITvd4l{KEG|c3H5 MXqwMVUh|ryP MVG0PEBp NIX5PGhKSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUeyOVcyOTR4MB?=
U87 NVX5NndiTnWwY4Tpc44hSXO|YYm= MUW1NEDPxE1? NFXUUVkzPCCq MWfy[YR2[2W|IITo[UBuWk6DIHX4dJJme3Orb36gcIV3\Wy|IH;mJG1OWC1{LDDNUXAuOTRiYX7kJGJkdC1{ MonzNlU3Pjd4NkO=
K562 MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGnkTYwyNTFyIN88US=> MoLIOFghcA>? NIXKT|FFVVOR MWrJR|UxRTJ4Lkeg{txO Ml\ONlU2QTZ3NkG=
K562/Mcl -1-IRESBim MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XycWlEPTB;OT6zJO69VQ>? MXGyOVU{PTlyMB?=
K562/Bcl- 2-IRESBim NFHxbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwM{Wg{txO M3O3OlI2PTN3OUCw
Jurkat M3LHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrZd3NKSzVyPUCuOlYh|ryP NFrZ[XIzPTV|NUmwNC=>
JurkatΔBak MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i4R2lEPTB-NUCg{txO NGTFOWkzPTV|NUmwNC=>
HL60/VCR NI[yXmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjaOFAyUUN3ME6xNFAh|ryP NHPqcWozPTV|NUmwNC=>
Kasumi-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwMEGg{txO NGfNbYUzPTV|NUmwNC=>
Kasumi-1/ABT MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXDTWM2OD1yLkWxJO69VQ>? MojUNlU2OzV7MEC=
THP-1 NXnLVFJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Hrb2lEPTB;MT6yO{DPxE1? MW[yOVU{PTlyMB?=
U937 M1PRPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTlN|dtUUN3ME21MlI6KM7:TR?= M13QXVI2PTN3OUCw
C1498 NYrUVZpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzPdmxKSzVyPU[uNVMh|ryP NGXpXYczPTV|NUmwNC=>
RPMI 8226 NFjXfpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILtSlVKSzVyPUCuNlUh|ryP MXmyOVU{PTlyMB?=
MM.1S NFvqb4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXTW2pKSzVyPUCuOFAh|ryP NHf3cWgzPTV|NUmwNC=>
NCI-H929 M3PVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfxNmlKSzVyPUG1MlIyKM7:TR?= Mk\UNlU2OzV7MEC=
U266 NIHTTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DaWmlEPTB;MD62PEDPxE1? NYHrR2Y1OjV3M{W5NFA>
MCF-7 NYrGdo5yS2WubDDWbYFjcWyrdImgRZN{[Xl? NG\Dd4c2KM7:TR?= Ml\yOFghcA>? M2ju[GROW09? NWrrSY5w\W6qYX7j[ZMhfGinIIPlcpNqfGm4aYT5JJRwKG:{IILh[IlifGmxbh?= M4XY[VI2PDB7MUK0
MCF-7 MUHBdI9xfG:|aYOgRZN{[Xl? M{i0fVUh|ryP MYW0M|I1NzR6IHi= NYT2XY1NTE2VTx?= NVLiT5RScW6lcnXhd4V{KHSqZTDjcIVifmWmIGDBVnA> MmXlNlU1ODlzMkS=
MCF-7 NWHRRXRCTnWwY4Tpc44hSXO|YYm= MknxOUDPxE1? MlrXNlQhcA>? NXzMenIxTE2VTx?= M3G3b4VvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? M4fUS|I2PDB7MUK0
MDA-MB 231  M2T5dWZ2dmO2aX;uJGF{e2G7 M3\LcVUh|ryP M4ToOFI1KGh? NHHFcnlFVVOR NVvJPIdO\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi NFO4NXIzPTRyOUGyOC=>
ZR-75-1  M3XDcWZ2dmO2aX;uJGF{e2G7 MlTOOUDPxE1? M2LkclI1KGh? MWjEUXNQ NFWydHRmdmijbnPld{B1cGWuZY\lcEBw\iCPY3ytNUBmgHC{ZYPzbY9vyqB? NYfXVod4OjV2MEmxNlQ>
A549 NV7Db2RCS2WubDDWbYFjcWyrdImgRZN{[Xl? NH;BelgxNTJyIN88US=> NF3MZYs4OiCq NFPE[mFFVVOR NIjZZ4Nl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NITEb3QzPTN6OEe2Ni=>
H1299 MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NF3DOHMxNTJyIN88US=> NHfvVmY4OiCq M17FUWROW09? NIP6PYNl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NIfRR5AzPTN6OEe2Ni=>
HO-8910 M2n2N2NmdGxiVnnhZoltcXS7IFHzd4F6 M{LKSVAuOjBizszN MX[3NkBp M{DQfGROW09? MWTk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NEjJOZEzPTN6OEe2Ni=>
HT-29 MmPJR4VtdCCYaXHibYxqfHliQYPzZZk> MlnqNE0zOCEQvF2= NGDvPY84OiCq NWm5WI5kTE2VTx?= Mn7a[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? MnHuNlU{QDh5NkK=
HCT-116 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mk\GNE0zOCEQvF2= MXK3NkBp MnXQSG1UVw>? M1j3WYRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? MXyyOVM5QDd4Mh?=
A549 MX7BdI9xfG:|aYOgRZN{[Xl? M4HtSFIxKM7:TR?= NFjEXG01QCCq NI\iXGxFVVOR MlXBbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoaXPhcpRtgSClb33ibY5m\CC5aYToJIF{eGm{aX6= MVOyOVM5QDd4Mh?=
H1299 M4T2SWFxd3C2b4Ppd{BCe3OjeR?= NYrWUHdKOjBizszN MY[0PEBp MmO4SG1UVw>? MoTWbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoaXPhcpRtgSClb33ibY5m\CC5aYToJIF{eGm{aX6= MmD6NlU{QDh5NkK=
Sc-1 NVP5[lZZS2WubDDWbYFjcWyrdImgRZN{[Xl? NHLy[ooxNjByMEGtNUDPxE1? NU\GfYM{QTZiaB?= Ml;i[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHjqWmMzPTN5M{WwPC=>
OcI-LY18 MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUCwMlAxODFvMTFOwG0> MmPRPVYhcA>? MYHk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFHuUVAzPTN5M{WwPC=>
RL  M3[xcmNmdGxiVnnhZoltcXS7IFHzd4F6 NFfxZ5kxNjByMEGtNUDPxE1? NVXxXlFnQTZiaB?= MWXk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NEPzNXkzPTN5M{WwPC=>
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Clone A NX7iW5lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7EcpYxNjMkgKO2NEDPxE1? NFm0eXY4OiCq NUnpOFFETE2VTx?= M2XqbWlEPTB;Nz61JO69VQ>? NVTjb5BPOjV{MEi4PFI>
CX-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PPVlAvOuLCk{[wJO69VQ>? Mlf6O|IhcA>? MXPEUXNQ MX7JR|UxRTFwODFOwG0> NXnUO2llOjV{MEi4PFI>
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OPM-2  NHPUU3JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWP2UVBrOTJ3L{K1NE82ODBibl2= M3vGO|Q5cMLi M2HycGROW09? NFTlXlFl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWeyOVAxQDJyMh?=
RPMI-8226  NH3zR|NCeG:ydH;zbZMhSXO|YYm= M{W3V|EzPS9{NUCvOVAxKG6P NIe4Tlc1QGkEoB?= NYfNO24yTE2VTx?= NIfrfYdqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NVTtcWRHOjVyMEiyNFI>
OPM-2  Mk\ORZBweHSxc3nzJGF{e2G7 M4\yZVEzPS9{NUCvOVAxKG6P NFnzUGw1QGkEoB?= M3jLd2ROW09? MYPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWSyOVAxQDJyMh?=
COG-LL-319 NHnm[oJHfW6ldHnvckBCe3OjeR?= M33ZdFExOCCwTR?= NVjwR4huOS9|L{[gbC=> MnrKSG1UVw>? Ml;jbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDNZ4wuOSClbHXheoFo\Q>? NUm3NmN4OjR7NUG0O|I>
RS4;11 NWDIR5ZXTnWwY4Tpc44hSXO|YYm= MmP3NVAxKG6P NWPQUYFoOS9|L{[gbC=> NWfYUI11TE2VTx?= NELU[VJqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JG1kdC1zIHPs[YF3[Wen NEG2RVczPDl3MUS3Ni=>

... 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 (g) = Concentration (mol/L) × Volume (L) × 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

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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.

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID