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 90 Publications

16 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.

    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.

  • 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.

  • (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.

    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.

  • 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.

  • 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.

  • 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.

    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.

    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)
Bfl-1 [1]
(Cell-free assay)
30.3 nM(EC50) 78.7 nM(EC50) 197.8 nM(EC50) 1.82 μM(EC50) >10 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  MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXfGOoljOjVyIH7NxsA> M2jvRVczKGh? NVi0UVZGTE2VTx?= NEDvO4Nk[XW|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>? NIHHfXUzPjZ3N{K4PC=>
KG1a NX3nZmw6S2WubDDWbYFjcWyrdImgRZN{[Xl? MUOwMVExKM7:TR?= MWGyOEBp NYjDdVZWTE2VTx?= MlzITWM2OD15Lk[4JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXnYUIl1OjZ3NUK3NVI>
Kasumi-1 NGDjdIVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUiwMVExKM7:TR?= NUSxZYZKOjRiaB?= NVq2RXhJTE2VTx?= NV;wXIlnUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MnXWNlY2PTJ5MUK=
KG1a MVfBdI9xfG:|aYOgRZN{[Xl? NWX4WHBUOC1zMDFOwG0> MmrBNlQhcA>? MoHvSG1UVw>? MWrpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXrTTI1kOjZ3NUK3NVI>
Kasumi-1 MUfBdI9xfG:|aYOgRZN{[Xl? NFzEPZAxNTFyIN88US=> Mn3mNlQhcA>? NFH0ZYNFVVOR NHqzZ3lqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MX[yOlU2OjdzMh?=
MC-3  M17Jemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXGOU8yOC9{MDFOwG0> M332ZVI1KGh? MlThSG1UVw>? NGf4Z|FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnjLNlY1PDd4MUW=
HN22  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrxNk42NzdwNT:yNk42KM7:TR?= M2Pw[FI1KGh? NXHiPGlQTE2VTx?= M3XLd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M33XOVI3PDR5NkG1
MC-3  NWXhfm5LSXCxcITvd4l{KEG|c3H5 MVW1M|ExNzJyIN88US=> Mki0NlQhcA>? M{fU[GROW09? MXXpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| M3;HTVI3PDR5NkG1
HN22  NVfRbo5qSXCxcITvd4l{KEG|c3H5 NWnINWJpOi53L{euOU8zOi53IN88US=> NWrQWoJIOjRiaB?= MojHSG1UVw>? MnfabY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= MXqyOlQ1PzZzNR?=
MOLT-4 NV7yXmR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr4UHVoOTBvNUCwNEBvVQ>? MknDO|IhcA>? NWDB[nVqTE2VTx?= M{OxdGlEPTB;MD6xPVgh|ryP MYWyOlM6OjN|Mh?=
RS4;11 NWnoNmgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrFNVAuPTByMDDuUS=> M1TielczKGh? NXzyNIlMTE2VTx?= Mlf2TWM2OD1yLkCwNkDPxE1? NUTIWVBCOjZ|OUKzN|I>
JURKAT MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrz[I0yOC13MECwJI5O MYe3NkBp MUTEUXNQ M{\RS2lEPTB;Nk[g{txO MUCyOlM6OjN|Mh?=
CEM R NGX3ZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDHb3EyOC13MECwJI5O NXrhPVlrPzJiaB?= M4rz[GROW09? MWnJR|UxRTVwNDFOwG0> MYiyOlM6OjN|Mh?=
CEM S NWPrWHlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHpNVAuPTByMDDuUS=> NFPyVYY4OiCq MnLXSG1UVw>? MWLJR|UxRTF{LkGg{txO NEjmVoszPjN7MkOzNi=>
MOLT-4 NIXNV41CeG:ydH;zbZMhSXO|YYm= NY[4e3Q6OTBvMUCwNEBvVQ>? M4LaZVI1KGh? M2TtXGROW09? MmHNZ4F2e2W|IITo[UBkdGWjdnHn[UBw\iCEY3ytNkBidmRidHjlJIRwf26{ZXf1cIF1cW:wIH;mJGJkdC26TDDhcoQhVWOuLUG= MXqyOlM6OjN|Mh?=
CEM S MUfBdI9xfG:|aYOgRZN{[Xl? MU[xNE0yODByIH7N NEDoNXIzPCCq M132O2ROW09? MYXjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= M1u3fFI3Ozl{M{Oy
JURKAT MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3sNVAxNTFyMECgcm0> MV[0PEBp NIfzfGhFVVOR MVvJR|UxRTl3NdMxPU4{KG6P MVGyOlE4OjJ4OR?=
LOUCY MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXTRWE3OTByLUGwNFAhdk1? MlLqOFghcA>? M1fmXWROW09? NF\1VGhKSzVyPUOyMljDuTFyLkmgcm0> NIjTSXIzPjF5MkK2PS=>
WM-115 NH3ZVIhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIXkPYEyODEEoH7N MmftO|IhcA>? NH63c5lmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= MUSyOlEyPjd5Nh?=
B16 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFjGT|kyODEEoH7N MmjDO|IhcA>? MnXK[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? NF7uVoozPjFzNke3Oi=>
HL-60  NGrPbY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXOwOYhNPzJiaB?= NIDtc2NKSzVywrC9JFExNjdibl2= NV:3Z3drOjZyNEW2NFk>
MOLM-13  MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTyO|IhcA>? M2rNbmlEPTEEoE2gNlcvQSCwTR?= M1XOelI3ODR3NkC5
OCI-AML3 NUKzXll4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfqeYg4OiCq MX\JR|UxyqB;IEG5OVAhdk1? M{HCRlI3ODR3NkC5
BCWM.1 NWHFPZY5SXCxcITvd4l{KEG|c3H5 M1L6WVAuOS54IN88US=> NXrhfFk4OjRiaB?= Mk\UbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MlOwNlU5QTN{OUC=
MWCL-1 NFfYNYJCeG:ydH;zbZMhSXO|YYm= MYKwMVEvPiEQvF2= M3m5T|I1KGh? NGmxO|FqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NGDPb4wzPTh7M{K5NC=>
MM.1s M2LyZWFxd3C2b4Ppd{BCe3OjeR?= Mn7SNE0yNjZizszN MUWyOEBp NV3aWlVwcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NEnhV20zPTh7M{K5NC=>
HCT116 MnrWSpVv[3Srb36gRZN{[Xl? M3f4RVMwOTBizszN M3PqPFEzyqCqwrC= M3W0SmROW09? NHnOcmRqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= NHP5SHIzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO M{fv[2Z2dmO2aX;uJGF{e2G7 MnuzN{8yOCEQvF2= MYixNuKhcMLi MWTEUXNQ MYDpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? NHnqPW4zPTdzNUCyPC=>
HCT116 MX7GeY5kfGmxbjDBd5NigQ>? MoPzNVAh|ryP NHH0cHYyOsLiaNMg M4LRUWROW09? MkHVbY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= MlfENlU4OTVyMki=
HCT116 BAX BAK1 DKO MXPGeY5kfGmxbjDBd5NigQ>? NYLEWY1pOTBizszN NVfFXVVuOTMEoHlCpC=> Mm\aSG1UVw>? NXzldlNmcW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> NYT1bJpHOjV5MUWwNlg>
HCT116 NHLBe4RCfXSxcHjh[5khSXO|YYm= M2nTWFExKM7:TR?= MnyyNVLDqGkEoB?= MYXEUXNQ Mnr6bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> NHTQemMzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO M4rwcWF2fG:yaHHnfUBCe3OjeR?= MlfJNVAh|ryP MY[xNuKhcMLi NFTKTVVFVVOR MWrpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> M4DaSFI2PzF3MEK4
U937 MUPBdI9xfG:|aYOgRZN{[Xl? MnnsNE4yOjVvMjFOwG0> M{HEO|I1KGh? NXfhcFlP\W6qYX7j[ZMhTEiDL2itNVEucW6mdXPl[EBieG:ydH;zbZM> NEDTcnYzPTdzNECyOC=>
U937  MoD5RZBweHSxc3nzJGF{e2G7 NXvOcXlOOC53IN88US=> M4f0clI1KGh? NFfQe|hmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs MkezNlU4OTRyMkS=
HL-60 AAA-Bcl-2 MVXBdI9xfG:|aYOgRZN{[Xl? NVLH[FFyOC13IN88US=> MX:0PEBp MYLJR|UxRTBwOEeg{txu97zOaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkjnNlU4OTF2NkC=
HL-60 EEE-Bcl-2 MoDFRZBweHSxc3nzJGF{e2G7 MnK4NE02KM7:TR?= MWO0PEBp M3nCWWlEPTB;NTFOwI3wxIxiaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1TKOVI2PzFzNE[w
U87 MWXGeY5kfGmxbjDBd5NigQ>? MUm1NEDPxE1? NWHZOm1tOjRiaB?= MmO3doVlfWOnczD0bIUhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?= NGLYdFMzPTZ4N{[2Ny=>
K562 M{DBT2NmdGxiVnnhZoltcXS7IFHzd4F6 NYjybGRFOS1zMDFOwG0> MWC0PEBp NYPIcnRKTE2VTx?= MV;JR|UxRTJ4Lkeg{txO NWHNdopQOjV3OU[1OlE>
K562/Mcl -1-IRESBim MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfhV|ByUUN3ME25MlMh|ryP MknwNlU2OzV7MEC=
K562/Bcl- 2-IRESBim MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LyemlEPTB;MD6zOUDPxE1? Ml;YNlU2OzV7MEC=
Jurkat NEPWN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjFNpg3UUN3ME2wMlY3KM7:TR?= M4fMfFI2PTN3OUCw
JurkatΔBak NEDQZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3XNGxqUUN3ME61NEDPxE1? MWWyOVU{PTlyMB?=
HL60/VCR MmrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\LZoZKSzVyPkGwNEDPxE1? NW\LeoN5OjV3M{W5NFA>
Kasumi-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[1VGlEPTB;MD6wNUDPxE1? NX\RW5NGOjV3M{W5NFA>
Kasumi-1/ABT MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;VbGlEPTB;MD61NUDPxE1? M3;NW|I2PTN3OUCw
THP-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXPcXZKSzVyPUGuNlch|ryP MWmyOVU{PTlyMB?=
U937 MnPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTnTWM2OD13LkK5JO69VQ>? MUKyOVU{PTlyMB?=
C1498 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvzV3p2UUN3ME22MlE{KM7:TR?= Ml;HNlU2OzV7MEC=
RPMI 8226 Mom1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G0WGlEPTB;MD6yOUDPxE1? NVrkV4VLOjV3M{W5NFA>
MM.1S M4XhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFztbXlKSzVyPUCuOFAh|ryP NIHyU|kzPTV|NUmwNC=>
NCI-H929 NVTtR5JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHSNIY6UUN3ME2xOU4zOSEQvF2= MknBNlU2OzV7MEC=
U266 MnL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPZOHJKSzVyPUCuOlgh|ryP Mlq3NlU2OzV7MEC=
MCF-7 NUHrfHB4S2WubDDWbYFjcWyrdImgRZN{[Xl? NH7zN2c2KM7:TR?= M2jIfFQ5KGh? NGrZblZFVVOR NVXYbmRQ\W6qYX7j[ZMhfGinIIPlcpNqfGm4aYT5JJRwKG:{IILh[IlifGmxbh?= NXLVW4Y5OjV2MEmxNlQ>
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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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W 30mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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.

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID