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 101 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  M2rMfmNmdGxiVnnhZoltcXS7IFHzd4F6 NGLFU3gzPTBibl5CpC=> MkHaO|IhcA>? NYC5OXVvTE2VTx?= NYr4VnU1[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? NVXaZ3hVOjZ4NUeyPFg>
KG1a M2Pnb2NmdGxiVnnhZoltcXS7IFHzd4F6 NEDXWYsxNTFyIN88US=> MXeyOEBp NVvX[GIxTE2VTx?= M3WyV2lEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkLCNlY2PTJ5MUK=
Kasumi-1 MoDvR4VtdCCYaXHibYxqfHliQYPzZZk> NYrDTFlrOC1zMDFOwG0> M{L1bVI1KGh? NEHVSnNFVVOR NXLzT4pQUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MlHyNlY2PTJ5MUK=
KG1a NUD6OIV1SXCxcITvd4l{KEG|c3H5 M{mxclAuOTBizszN NV2zcVRGOjRiaB?= NUT4N|R4TE2VTx?= MYTpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHH3O3kzPjV3MkexNi=>
Kasumi-1 NHPMeI1CeG:ydH;zbZMhSXO|YYm= NHy3SpkxNTFyIN88US=> MkfkNlQhcA>? NU[wUlNqTE2VTx?= M{LpNolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NG\0cFAzPjV3MkexNi=>
MC-3  NUXjPJR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NECzd5Q2NzFyL{KwJO69VQ>? NGjncHEzPCCq Mke2SG1UVw>? NUTNcZE6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVmyOlQ1PzZzNR?=
HN22  NFLOW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG1[o13Oi53L{euOU8zOi53IN88US=> NFnmVHgzPCCq MY\EUXNQ M2rveIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkLNNlY1PDd4MUW=
MC-3  NHr2NFBCeG:ydH;zbZMhSXO|YYm= NWP1UlZOPS9zMD:yNEDPxE1? MV:yOEBp MmjsSG1UVw>? M2HJ[Ylv\HWlZYOgZ4F{eGG|ZT3t[YRq[XSnZDDhdI9xfG:|aYO= M1HoTlI3PDR5NkG1
HN22  MV;BdI9xfG:|aYOgRZN{[Xl? NXfLOYpQOi53L{euOU8zOi53IN88US=> M1TXT|I1KGh? M3;IXmROW09? MmHvbY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= MWCyOlQ1PzZzNR?=
MOLT-4 M4nme2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfBNVAuPTByMDDuUS=> MkLEO|IhcA>? Mn\3SG1UVw>? MU\JR|UxRTBwMUm4JO69VQ>? MYWyOlM6OjN|Mh?=
RS4;11 NUO0XYliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOxNE02ODByIH7N MnXZO|IhcA>? NHHHZ21FVVOR NWTxUHhXUUN3ME2wMlAxOiEQvF2= NFGxOFIzPjN7MkOzNi=>
JURKAT MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XEUFExNTVyMECgcm0> NYPRZXlpPzJiaB?= Ml;3SG1UVw>? Mm[1TWM2OD14NjFOwG0> NFvMPYozPjN7MkOzNi=>
CEM R M2rISWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYOwbnQ2OTBvNUCwNEBvVQ>? MoOzO|IhcA>? M2T2[WROW09? MnzkTWM2OD13LkSg{txO NGT4UpIzPjN7MkOzNi=>
CEM S M3X1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvBfGxHOTBvNUCwNEBvVQ>? NWnBfGJYPzJiaB?= MY\EUXNQ NWm0UVlIUUN3ME2xNk4yKM7:TR?= MVyyOlM6OjN|Mh?=
MOLT-4 MXfBdI9xfG:|aYOgRZN{[Xl? M2PGVFExNTFyMECgcm0> MXWyOEBp M3PhWGROW09? MofPZ4F2e2W|IITo[UBkdGWjdnHn[UBw\iCEY3ytNkBidmRidHjlJIRwf26{ZXf1cIF1cW:wIH;mJGJkdC26TDDhcoQhVWOuLUG= M4rBPVI3Ozl{M{Oy
CEM S Mmr4RZBweHSxc3nzJGF{e2G7 MVKxNE0yODByIH7N NV\WdZFkOjRiaB?= Mm\GSG1UVw>? NFjMVm9k[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> MUWyOlM6OjN|Mh?=
JURKAT NY\6b4lrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjaflh6OTByLUGwNFAhdk1? MWi0PEBp NUXJfGFYTE2VTx?= NV7xXo5kUUN3ME25OVXDuTlwMzDuUS=> MkDlNlYyPzJ{Nkm=
LOUCY Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOxNFAuOTByMDDuUS=> M2nSNVQ5KGh? MVzEUXNQ M2\VN2lEPTB;M{KuPOKyOTBwOTDuUS=> NHrpdVIzPjF5MkK2PS=>
WM-115 NYrlPVkxS2WubDDWbYFjcWyrdImgRZN{[Xl? MV6xNFDDqG6P Ml7XO|IhcA>? NH\mSotmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= NHfMVJQzPjFzNke3Oi=>
B16 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnXYNVAxyqCwTR?= M1ThVlczKGh? MVrlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NUTHPZVrOjZzMU[3O|Y>
HL-60  NYTtSJhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWS3NkBp MmHpTWM2OMLiPTCxNE44KG6P Ml;1NlYxPDV4MEm=
MOLM-13  NWfmeWF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe3NkBp M3HFWmlEPTEEoE2gNlcvQSCwTR?= M{XPOVI3ODR3NkC5
OCI-AML3 NI\hbnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHGPGlIPzJiaB?= M4PyfWlEPTEEoE2gNVk2OCCwTR?= NYXz[HJpOjZyNEW2NFk>
BCWM.1 NGruN45CeG:ydH;zbZMhSXO|YYm= NHfqbHgxNTFwNjFOwG0> NWPleolmOjRiaB?= M{HycYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NYT3NoZpOjV6OUOyPVA>
MWCL-1 NHG2e5lCeG:ydH;zbZMhSXO|YYm= NVnleZVmOC1zLk[g{txO MXyyOEBp MoHFbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MkXkNlU5QTN{OUC=
MM.1s MXPBdI9xfG:|aYOgRZN{[Xl? MYCwMVEvPiEQvF2= M1L0flI1KGh? Mk\abY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MWeyOVg6OzJ7MB?=
HCT116 NH3QUG1HfW6ldHnvckBCe3OjeR?= MUizM|ExKM7:TR?= NHXr[FgyOsLiaNMg MknXSG1UVw>? NFHLd45qdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= NEPDXXczPTdzNUCyPC=>
HCT116 BAX BAK1 DKO M{DETGZ2dmO2aX;uJGF{e2G7 NEmwWJg{NzFyIN88US=> MmPyNVLDqGkEoB?= NET1OnNFVVOR M3PPNolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= MY[yOVcyPTB{OB?=
HCT116 MUPGeY5kfGmxbjDBd5NigQ>? NUXDUmFKOTBizszN MnzhNVLDqGkEoB?= M1\VSGROW09? MmK2bY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= NYL0PJBkOjV5MUWwNlg>
HCT116 BAX BAK1 DKO NGrIV|RHfW6ldHnvckBCe3OjeR?= NV3ifmNwOTBizszN M1fFTFEzyqCqwrC= M1vmTmROW09? M36zXYlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= NGHqbWQzPTdzNUCyPC=>
HCT116 NV[yVZF7SXW2b4DoZYd6KEG|c3H5 NX7mSpZoOTBizszN NGXCdG4yOsLiaNMg NXHKbG9FTE2VTx?= M4TBfYlv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm MUKyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO MnLFRZV1d3CqYXf5JGF{e2G7 NIHmbZcyOCEQvF2= M1X0SVEzyqCqwrC= M3fuOGROW09? NWT1Z21ycW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? MXiyOVcyPTB{OB?=
U937 MortRZBweHSxc3nzJGF{e2G7 MoX0NE4yOjVvMjFOwG0> NY[0boNXOjRiaB?= MmSx[Y5p[W6lZYOgSGhCN1hvMUGtbY5lfWOnZDDhdI9xfG:|aYO= NWj4b3hsOjV5MUSwNlQ>
U937  NG\RN49CeG:ydH;zbZMhSXO|YYm= MWWwMlUh|ryP NHSzOWgzPCCq M3LVRoVvcGGwY3XzJINt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UuOyCjczD3[YxtKGG|IF7vfIEhdGW4ZXy= NXG0O2hkOjV5MUSwNlQ>
HL-60 AAA-Bcl-2 MWnBdI9xfG:|aYOgRZN{[Xl? NXTMbotMOC13IN88US=> NYThfI9SPDhiaB?= MlzjTWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEP5VGQzPTdzMUS2NC=>
HL-60 EEE-Bcl-2 NX\zd|EySXCxcITvd4l{KEG|c3H5 M3XVVlAuPSEQvF2= NXfLSnZuPDhiaB?= NWPROphEUUN3ME21JO69de,:jDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MX:yOVcyOTR4MB?=
U87 NV70XJVvTnWwY4Tpc44hSXO|YYm= M1v4NFUxKM7:TR?= MWqyOEBp NYP0VnFxemWmdXPld{B1cGVibWLORUBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUG0JIFv\CCEY3ytNi=> MmPSNlU3Pjd4NkO=
K562 NHW4ZZNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NITvSFgyNTFyIN88US=> NGnGb4Q1QCCq M2D3c2ROW09? M2DYTWlEPTB;Mk[uO{DPxE1? Ml[zNlU2QTZ3NkG=
K562/Mcl -1-IRESBim NVz4UlhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTlwMzFOwG0> M4m5eVI2PTN3OUCw
K562/Bcl- 2-IRESBim MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrwdYdKSzVyPUCuN|Uh|ryP NUXBOWk3OjV3M{W5NFA>
Jurkat NXXUVYtjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzZ[oQyUUN3ME2wMlY3KM7:TR?= NVK5OHFDOjV3M{W5NFA>
JurkatΔBak MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInhVJJKSzVyPkWwJO69VQ>? MnLnNlU2OzV7MEC=
HL60/VCR MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2CzbGlEPTB-MUCwJO69VQ>? MlzxNlU2OzV7MEC=
Kasumi-1 NHz5W5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwMEGg{txO MUiyOVU{PTlyMB?=
Kasumi-1/ABT Ml[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITCbWpKSzVyPUCuOVEh|ryP MWKyOVU{PTlyMB?=
THP-1 M1jkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[xW4xKSzVyPUGuNlch|ryP MmS4NlU2OzV7MEC=
U937 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK0VZA{UUN3ME21MlI6KM7:TR?= Ml\nNlU2OzV7MEC=
C1498 NF;SbXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT5b2hkUUN3ME22MlE{KM7:TR?= NVTHcld7OjV3M{W5NFA>
RPMI 8226 NUPrbmZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfvTWM2OD1yLkK1JO69VQ>? M2LmZ|I2PTN3OUCw
MM.1S NF\ZTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwNECg{txO Mkf4NlU2OzV7MEC=
NCI-H929 NInCeIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq4S5BbUUN3ME2xOU4zOSEQvF2= MWSyOVU{PTlyMB?=
U266 Mlu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjVSotKSzVyPUCuOlgh|ryP M{nrT|I2PTN3OUCw
MCF-7 NVLT[ZcyS2WubDDWbYFjcWyrdImgRZN{[Xl? MWm1JO69VQ>? MX[0PEBp MX7EUXNQ MoDa[Y5p[W6lZYOgeIhmKHOnboPpeIl3cXS7IITvJI9zKHKjZHnheIlwdg>? MnPhNlU1ODlzMkS=
MCF-7 NYnlUGVUSXCxcITvd4l{KEG|c3H5 NUPMem9RPSEQvF2= MnP2OE8zPC92ODDo M4TPfWROW09? Mn\LbY5kemWjc3XzJJRp\SClbHXheoVlKFCDUmC= NXi3emV7OjV2MEmxNlQ>
MCF-7 M{\TdGZ2dmO2aX;uJGF{e2G7 MX:1JO69VQ>? NYTZSJRrOjRiaB?= NGO0fmpFVVOR M3KySYVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? M4exRlI2PDB7MUK0
MDA-MB 231  M1jnTmZ2dmO2aX;uJGF{e2G7 NVrYTnZ6PSEQvF2= M{PTb|I1KGh? Mm\NSG1UVw>? MVLlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> MY[yOVQxQTF{NB?=
ZR-75-1  MoTnSpVv[3Srb36gRZN{[Xl? NFXSfVI2KM7:TR?= MWqyOEBp NHrjS3BFVVOR MVPlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> MWWyOVQxQTF{NB?=
A549 NVHLbXdyS2WubDDWbYFjcWyrdImgRZN{[Xl? MnT6NE0zOCEQvF2= NVvmeIhSPzJiaB?= MVHEUXNQ M2\YUIRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M{W1Z|I2Ozh6N{[y
H1299 MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV:wMVIxKM7:TR?= MkewO|IhcA>? M4rFN2ROW09? MnTD[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? MnPINlU{QDh5NkK=
HO-8910 NWjoO2VRS2WubDDWbYFjcWyrdImgRZN{[Xl? MXmwMVIxKM7:TR?= NYr6Uo8{PzJiaB?= NXPUe2oyTE2VTx?= NXXQ[4RY\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= MVmyOVM5QDd4Mh?=
HT-29 M1zTeWNmdGxiVnnhZoltcXS7IFHzd4F6 NWjJWZFtOC1{MDFOwG0> NWPXXYxUPzJiaB?= NGfZNG5FVVOR Mnvy[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? M4DPcFI2Ozh6N{[y
HCT-116 NY\3W5RyS2WubDDWbYFjcWyrdImgRZN{[Xl? MUCwMVIxKM7:TR?= MmXmO|IhcA>? MXXEUXNQ MnX4[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? M12yRlI2Ozh6N{[y
A549 M{\6O2Fxd3C2b4Ppd{BCe3OjeR?= NUTQTJpXOjBizszN NXPjWZNrPDhiaB?= MkLhSG1UVw>? M{\MU4lv\HWlZYOgZZBweHSxc3nzJJNq\26rZnnjZY51dHliY3;tZolv\WRid3n0bEBie3Crcnnu MVSyOVM5QDd4Mh?=
H1299 MoGwRZBweHSxc3nzJGF{e2G7 M1LjPFIxKM7:TR?= M4TmelQ5KGh? NFj6d3dFVVOR NV3DPIk1cW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> MUCyOVM5QDd4Mh?=
Sc-1 NHGzc3pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MV:wMlAxODFvMTFOwG0> M1XnbVk3KGh? NHm4PXVl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2nPTVI2Ozd|NUC4
OcI-LY18 NWOwRm5PS2WubDDWbYFjcWyrdImgRZN{[Xl? Moj4NE4xODBzLUGg{txO NFPSb|Q6PiCq MoC2[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnPtNlU{PzN3MEi=
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Clone A MlrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfX[IVbOC5{4pETOlAh|ryP MkLQO|IhcA>? M2TvemROW09? MWnJR|UxRTdwNTFOwG0> Ml\4NlUzODh6OEK=
CX-1 NYjudoVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXiNE4z6oDVNkCg{txO Mne1O|IhcA>? M{DScGROW09? NWjzR4ZUUUN3ME2xMlgh|ryP MlvPNlUzODh6OEK=
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HT29 MX7BdI9xfG:|aYOgRZN{[Xl? M4\xdVEwPS9zMDFOwG0> NF64NY41QCCq NEDhN4xk[XW|ZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX6yOVE6OjF6OB?=
SW480 NIn5Z|ZCeG:ydH;zbZMhSXO|YYm= M{D6clEwPS9zMDFOwG0> Ml\VOFghcA>? NUjLfJJj[2G3c3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX2yOVE6OjF6OB?=
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UM-SCC22B NWLheZpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGO3OJQ4OiCq NVLLUGluTE2VTx?= NYTCfJA1T0l3ME2xPUDDuSB{Lkmg{txO NVfxRXRuOjVzM{mzPFc>
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RPMI-8226  NWm0e4t6SXCxcITvd4l{KEG|c3H5 NXHpOVJxOTJ3L{K1NE82ODBibl2= NF;qR4s1QGkEoB?= NVHvTWFwTE2VTx?= NWfxPI5zcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MYqyOVAxQDJyMh?=
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... 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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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