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 92 Publications

17 Customer Reviews

  • Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.

    Nat Med 2013 19(11), 1478-88. ABT-737 purchased from Selleck.

    Release of mitochondrial cytochrome c and loss of mitochondrial membrane potential after exposure to ABT-737 (100nM) for 2 hours were assessed by immunohistochemistry and staining with TMRE (red, top panels) and anti-CD41/FITC (green, top panels). Bar represents 5 um. Note that control cells display spreading on glass slides, whereas ABT-737-treated cells do not.

    Blood 2011 17(26), 7145-54. ABT-737 purchased from Selleck.

  • Platelets were incubated in HBS with or without ABT-737 (100nM) for 2 hours before analysis by immunohistochemistry and confocal microscopy. Actin was stained using phalloidin/Alexa-488 (green), and tubulin was stained using anti-tubulin/phycoerythrin (red). Bar represents 5 uM.

    Blood 2011 17(26), 7145-54. ABT-737 purchased from Selleck.

    BCL-XL mediates human neutrophil survival. PMNs were preincubated with the BH3 mimetic ABT-737 (1–10 μM), then cultured in normoxia (gray bars) with or without GM-CSF (500 U/ml) or hypoxia (white bars)or 20 hours, and apoptosis was assessed by morphology (n = 4).

     

     

    J Clin Invest 2011 121, 1053-1063. ABT-737 purchased from Selleck.

  • Analysis of SW480 and SW620 cell sensitivity to the BH3-mimetic ABT-737. (a, b) Percentage of apoptosis in adherent or suspended SW480 (a) or SW620 (b) cells cultured in the presence (ABT-737) or absence (ctrl) of ABT-737 (1 uM).

    Cell Death Dis 2013 4, e801. ABT-737 purchased from Selleck.

    (B) The sensitivity (LD50) of CLL cells, assessed by annexin V staining after 48 h of treatment with ABT‐737, ABT‐263 or ABT‐199, was plotted against the pBcl‐2/Bcl‐2, Mcl‐1/Bcl‐2 and (pBcl‐2 + Mcl‐1)/Bcl‐2 ratios. Relative protein quantification was carried out with kodak carestream molecular imaging software and normalized to β‐actin. Spearman's correlation (r) and P values are shown. Data shown are representative of five independent experiments.

    Br J Pharmacol, 2016, 173(3):471-83. ABT-737 purchased from Selleck.

  • Bcl-XL/Bcl-2 inhibitor ABT-737 aggravates the proapoptotic effects of IL-1IFN-. INS-1E cells were transfected with single or smart Pool PUMA siRNAs and exposed to ABT-737 for 24 h. At this time point, cell death was measured by HO/PI, n  3. *, p  0.05; **, p  0.01.
     

     

     

    J Biol Chem 2010 285, 19919-19920. ABT-737 purchased from Selleck.

    Effect of ABT-737 on the cell viability of CCRF-CEM cells by treatments of AY4 (10 μg/ml), TRAIL (0.5 μg/ml), SAHA (1 μM),VPA (1 mM), or ABT-737 (10 μM) alone or in combination for 24 h prior to MTT assay.

     

     

    Apoptosis 2010 15, 1256-1269. ABT-737 purchased from Selleck.

  • Effects of ABT-737 and RES, applied alone and in combination, on the viability of MOLT-4 cells.

    Toxicol In Vitro, 2017, 42:38-46. ABT-737 purchased from Selleck.

    Upper panel ABT-737 inhibits TFK-1 and EGI-1 cell growth.Cells were exposed to ABT-737 at a concentration ranging from 1 to 50 lM. Following 72 h of incubation, growth inhibition was analyzed by crystal violet assay. Dose–effect plot of ABT-737 treatment is presented.

     

     

    Cancer Chemoth Pharm 2011 67, 557-567. ABT-737 purchased from Selleck.

  • Lower panel detection of PARP-1, cleaved caspase-9 and caspase-3, BCL-2 and MCL-1 in TFK-1 and EGI-1 cells after 72 h of ABT-737 treatment (1, 3, 10, 25,50 μM). Cell lysates were analyzed on Western blotting.

     

     

    Cancer Chemoth Pharm 2011 67, 557-567. ABT-737 purchased from Selleck.

    GSIXII synergized with ABT-737 to trigger apoptosis in breast cancer cells . Breast cancer cell lines were incubate d for 48 hours with 10μM GSIXII or DMSO (Ct) in combination or not with ABT-737, 1 μM. Then apoptosis was evaluated with Apo2.7 or Annexin-V staining and flow-cytometry analysis. Represented data are the means of positive cells ± SEM, from three independent experiments.(A) Suboptimal concentrations of GSIXII (5 μM) and 1 μM ABT-737 were used alone or in combination in MFU assay in MCF7 and BT549 cell lines. Results were obtained from three independent experiments and compared with mock-treated condition. (B) The 20 μM SAHM1 was used alone or in combination in MFU assay in MCF7 and BT549 cell lines. Results were obtained from three independent experiments and compared with the mock-treated condition.

    Biochem Biophys Res Commun 2013 408, 344-9. ABT-737 purchased from Selleck.

  • Apoptosis induced by BCL2-inhibitors in P-glycoprotein expressing cells. MDCKII wild type or MDR1 cells were exposed to different concentrations of ABT-737 (C) or ABT-263 (D) for 24 h before apoptosis was assessed by flow cytometry using externalization of phosphatidylserine.

    Biochem Biophys Res Commun 2012 408, 344-9. ABT-737 purchased from Selleck.

    3 μM ABT737 inhibited growth and viability of TF-1 cells and potentiated proapoptotic effects of 1 μM BIO after 72 hours treatment. TF-1 cells treated with both drugs exhibited more apoptotic cells compared to those treated with each single drug. ABT737 abrogated the protection from BIO-induced apoptosis provided by MS5 coculture.

     

     

    Exp Hematol 2010 38, 908-921. ABT-737 purchased from Selleck.

  • The combined use of ABT-737 and sorafenib changes the apoptotic effect. MC-3 cells were treated with the indicated compounds for 48 h. (A) Nuclear condensation and fragmentation were evaluated in DAPI-stained cells as described in the Materials and Methods (X400). (B) Live (green) and dead (red) cells were qualified using the Live/dead assay kit as described in the Materials and Methods (X200). (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article.)

    Arch Oral Biol, 2017, 73:1-6. ABT-737 purchased from Selleck.

    MEF wt and MEF Mcl-1 ko mice activating active caspase-3 using 1um ABT for 24h

     

     

    Dr. Arnim Weber of Medizinische Mikrobiologie und Hygiene Universitatsklinikum Freiburg. ABT-737 purchased from Selleck.

  • MDB-MA-231 cells were exposed to 30 um cisplatin in the absence or in thepresence of 100nm ABT-737.The cell were stained with Hoechst 33342,MitoTracker Red and Yo-pro-1.

     

     

    Dr. Zhang of Tianjin Medical University. ABT-737 purchased from Selleck.

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  NGnnW2tE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlLsNlUxKG6PwrC= M1jnW|czKGh? NX7pV3N4TE2VTx?= NY\L[YpU[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? NYfCTWVvOjZ4NUeyPFg>
KG1a MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3\NPFAuOTBizszN M{XTOFI1KGh? M1zYcmROW09? MYPJR|UxRTdwNkig{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX:2U|k{OjZ3NUK3NVI>
Kasumi-1 NFjvVYxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXu3NoE{OC1zMDFOwG0> MU[yOEBp NELmWWFFVVOR NUjrVJF2UUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M1;YNlI3PTV{N{Gy
KG1a MmHPRZBweHSxc3nzJGF{e2G7 NELiRYUxNTFyIN88US=> NUPhXpNuOjRiaB?= NFrrN5dFVVOR NUnUN2ZZcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGLrSoIzPjV3MkexNi=>
Kasumi-1 MVvBdI9xfG:|aYOgRZN{[Xl? MoXMNE0yOCEQvF2= NFrubHAzPCCq NVHyNJpvTE2VTx?= NFvIU|hqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M4TWPVI3PTV{N{Gy
MC-3  M1vaXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrzOU8yOC9{MDFOwG0> M3jEZVI1KGh? Ml;kSG1UVw>? NFT5UGNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVvaT2hIOjZ2NEe2NVU>
HN22  M{PKV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHGVpIzNjVxNz61M|IzNjVizszN MmLXNlQhcA>? M2m4XGROW09? MnPFbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWD6RY9TOjZ2NEe2NVU>
MC-3  MX7BdI9xfG:|aYOgRZN{[Xl? M2HFbVUwOTBxMkCg{txO MY[yOEBp M1juOmROW09? MXrpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| NHXHfY0zPjR2N{[xOS=>
HN22  MmrpRZBweHSxc3nzJGF{e2G7 M{iwelIvPS95LkWvNlIvPSEQvF2= NH3IcGYzPCCq MXTEUXNQ NU[3e|BCcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> NHPIb|czPjR2N{[xOS=>
MOLT-4 Mor1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfjTVQyOC13MECwJI5O Ml7EO|IhcA>? MX3EUXNQ NUjJclVPUUN3ME2wMlE6QCEQvF2= NGPBVoozPjN7MkOzNi=>
RS4;11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjLNVAuPTByMDDuUS=> MlXVO|IhcA>? NEPUUXVFVVOR M3flbWlEPTB;MD6wNFIh|ryP M3HpRVI3Ozl{M{Oy
JURKAT NWPIZYNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHDS2QyOC13MECwJI5O NUTZNIYzPzJiaB?= MXTEUXNQ MkTBTWM2OD14NjFOwG0> NEDndIUzPjN7MkOzNi=>
CEM R MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXRPWZnOTBvNUCwNEBvVQ>? NEC1[Hc4OiCq NFj3ZmNFVVOR NEe3V4pKSzVyPUWuOEDPxE1? NV3kOohDOjZ|OUKzN|I>
CEM S MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\lU3I5OTBvNUCwNEBvVQ>? MkLQO|IhcA>? MV;EUXNQ MYTJR|UxRTF{LkGg{txO M1zLWVI3Ozl{M{Oy
MOLT-4 M2XyN2Fxd3C2b4Ppd{BCe3OjeR?= M3i1UlExNTFyMECgcm0> M1S3ZVI1KGh? Mn:0SG1UVw>? NY\Nbo5P[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> MnvYNlY{QTJ|M{K=
CEM S M4\jRWFxd3C2b4Ppd{BCe3OjeR?= MYWxNE0yODByIH7N NEnqWY4zPCCq NE\kfVBFVVOR M{DLU4NifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x NVLpbGdIOjZ|OUKzN|I>
JURKAT MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVyxNFAuOTByMDDuUS=> MUO0PEBp M1nvc2ROW09? MUXJR|UxRTl3NdMxPU4{KG6P NUezT2ZoOjZzN{KyOlk>
LOUCY MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHvVHRYOTByLUGwNFAhdk1? M{PtbFQ5KGh? NX\uXoFFTE2VTx?= Mn3vTWM2OD1|Mj64xtEyOC57IH7N MViyOlE4OjJ4OR?=
WM-115 M1nqV2NmdGxiVnnhZoltcXS7IFHzd4F6 NEe4SngyODEEoH7N MXu3NkBp M2H0cYVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi M4fVZlI3OTF4N{e2
B16 NIG2ZphE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn;DNVAxyqCwTR?= NHnrN2I4OiCq NWfVZZZH\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= MlXGNlYyOTZ5N{[=
HL-60  NYHndpB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\rWlczKGh? NFLtU4RKSzVywrC9JFExNjdibl2= Ml7kNlYxPDV4MEm=
MOLM-13  Ml\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUi3NkBp NFXNS5JKSzVywrC9JFI4Njlibl2= MXuyOlA1PTZyOR?=
OCI-AML3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLuO|IhcA>? M4jTOmlEPTEEoE2gNVk2OCCwTR?= NUTSXY9TOjZyNEW2NFk>
BCWM.1 MoD6RZBweHSxc3nzJGF{e2G7 NYfpTVU2OC1zLk[g{txO NXzQbXlROjRiaB?= M3HzXolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MV[yOVg6OzJ7MB?=
MWCL-1 M4C2UWFxd3C2b4Ppd{BCe3OjeR?= MXGwMVEvPiEQvF2= M3XH[lI1KGh? NUfnW2hWcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NX3JZ4dYOjV6OUOyPVA>
MM.1s NYHvXpZPSXCxcITvd4l{KEG|c3H5 NHLqU3UxNTFwNjFOwG0> MX6yOEBp M2jiSIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NVLqO3dLOjV6OUOyPVA>
HCT116 NXP1dpkxTnWwY4Tpc44hSXO|YYm= NGK3T4Y{NzFyIN88US=> MY[xNuKhcMLi MlPnSG1UVw>? NEfONZhqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= NX;TRVZuOjV5MUWwNlg>
HCT116 BAX BAK1 DKO M17qdWZ2dmO2aX;uJGF{e2G7 NXrPbm1COy9zMDFOwG0> M1fOcVEzyqCqwrC= NFPtRoJFVVOR NH7MemtqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= NXqxUHBIOjV5MUWwNlg>
HCT116 Mmj4SpVv[3Srb36gRZN{[Xl? MUixNEDPxE1? NYTZZ|FZOTMEoHlCpC=> MkjtSG1UVw>? MXvpcoNz\WG|ZYOgS2ZRNUyFM1KgdJVv[3Sj MnrqNlU4OTVyMki=
HCT116 BAX BAK1 DKO M4LaWWZ2dmO2aX;uJGF{e2G7 MXmxNEDPxE1? NHW2VmcyOsLiaNMg NHjLU5JFVVOR NYrEUYR3cW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MVSyOVcyPTB{OB?=
HCT116 NE\sfI1CfXSxcHjh[5khSXO|YYm= NG\VUGsyOCEQvF2= MnHaNVLDqGkEoB?= M132bGROW09? MXHpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> NVLUdWZDOjV5MUWwNlg>
HCT116 BAX BAK1 DKO NHryZ3NCfXSxcHjh[5khSXO|YYm= NFHvR3UyOCEQvF2= NUnRbZNWOTMEoHlCpC=> M3n2dmROW09? MlzZbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> NHPKNIszPTdzNUCyPC=>
U937 MmrkRZBweHSxc3nzJGF{e2G7 Mne3NE4yOjVvMjFOwG0> M3rvc|I1KGh? NHjXUWdmdmijbnPld{BFUEFxWD2xNU1qdmS3Y3XkJIFxd3C2b4Ppdy=> NXW5NIJ4OjV5MUSwNlQ>
U937  NFXKW5pCeG:ydH;zbZMhSXO|YYm= M3\COFAvPSEQvF2= MV2yOEBp M3\odIVvcGGwY3XzJINt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UuOyCjczD3[YxtKGG|IF7vfIEhdGW4ZXy= MVOyOVcyPDB{NB?=
HL-60 AAA-Bcl-2 NUfLNFhHSXCxcITvd4l{KEG|c3H5 MXewMVUh|ryP M4nYPVQ5KGh? NWfyU4llUUN3ME2wMlg4KM7:bf-8kIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVGyOVcyOTR4MB?=
HL-60 EEE-Bcl-2 NFvncWpCeG:ydH;zbZMhSXO|YYm= NVv5[4RJOC13IN88US=> M1P2SFQ5KGh? MoXTTWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2CyVVI2PzFzNE[w
U87 NEj5XnBHfW6ldHnvckBCe3OjeR?= MYW1NEDPxE1? MlrCNlQhcA>? NFjmWGtz\WS3Y3XzJJRp\SCvUl7BJIV5eHKnc4Ppc44hdGW4ZXzzJI9nKE2PUD2yMEBOVVBvMUSgZY5lKEKlbD2y NIjaU3UzPTZ4N{[2Ny=>
K562 M2rUZ2NmdGxiVnnhZoltcXS7IFHzd4F6 M{PnblEuOTBizszN NYfnSXc4PDhiaB?= MXrEUXNQ NIfiNFJKSzVyPUK2Mlch|ryP Mmq2NlU2QTZ3NkG=
K562/Mcl -1-IRESBim NIn0emtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zSSWlEPTB;OT6zJO69VQ>? NWm4fG1LOjV3M{W5NFA>
K562/Bcl- 2-IRESBim M4K4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DGT2lEPTB;MD6zOUDPxE1? M{\oeVI2PTN3OUCw
Jurkat NGTUT|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XoU2lEPTB;MD62OkDPxE1? NWPNVIlzOjV3M{W5NFA>
JurkatΔBak MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRjVyIN88US=> NY\tbZpTOjV3M{W5NFA>
HL60/VCR M4m5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rDXGlEPTB-MUCwJO69VQ>? NHPnUWMzPTV|NUmwNC=>
Kasumi-1 MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMEGg{txO NV25fXBzOjV3M{W5NFA>
Kasumi-1/ABT MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TON2lEPTB;MD61NUDPxE1? MljzNlU2OzV7MEC=
THP-1 NUnwS29{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fFVmlEPTB;MT6yO{DPxE1? NXXMeY1POjV3M{W5NFA>
U937 Mn3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H6RmlEPTB;NT6yPUDPxE1? NEXKS4szPTV|NUmwNC=>
C1498 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHrXYozUUN3ME22MlE{KM7:TR?= MkPONlU2OzV7MEC=
RPMI 8226 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HKTGlEPTB;MD6yOUDPxE1? NX63SYY1OjV3M{W5NFA>
MM.1S MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET5VY5KSzVyPUCuOFAh|ryP NU\YU2JuOjV3M{W5NFA>
NCI-H929 NFzEcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlixTWM2OD1zNT6yNUDPxE1? M3Hqc|I2PTN3OUCw
U266 MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\lfGlEPTB;MD62PEDPxE1? NIm5b2QzPTV|NUmwNC=>
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... Click to View More Cell Line Experimental Data

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

  • C1=C0/X C1: LOG(C1):
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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01440504 Completed Ovarian Cancer Centre Francois Baclesse|GRECAN April 2010 --

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID