ABT-737

製品コードS1002

ABT-737化学構造

分子量(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.

サイズ 価格(税別)  
JPY 63744.00
JPY 19920.00
JPY 33200.00
JPY 94620.00
JPY 161020.00

文献中Selleckの製品使用例(94)

カスタマーフィードバック(17)

  • 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.

    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.

  • 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.

    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.

製品安全説明書

Bcl-2阻害剤の選択性比較

生物活性

製品説明 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.
特性 First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
ターゲット
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)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OCI-Ly1  MoDvR4VtdCCYaXHibYxqfHliQYPzZZk> MnLSNlUxKG6PwrC= NGXOT2I4OiCq M1SyTmROW09? NUPPSXpy[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? MmKyNlY3PTd{OEi=
KG1a NIPmb4xE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{nRUVAuOTBizszN MXGyOEBp Mlf3SG1UVw>? NEL5SZpKSzVyPUeuOlgh|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFvTdnczPjV3MkexNi=>
Kasumi-1 NVPz[FRrS2WubDDWbYFjcWyrdImgRZN{[Xl? M{LhUlAuOTBizszN Mo\ZNlQhcA>? NYnKbI13TE2VTx?= NEPG[2hKSzVyPUSuPFch|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWOyOlU2OjdzMh?=
KG1a MnO5RZBweHSxc3nzJGF{e2G7 NHS2UYkxNTFyIN88US=> M3zNe|I1KGh? NVm0Z5Z6TE2VTx?= NVLLZlB{cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVLjZpdrOjZ3NUK3NVI>
Kasumi-1 NI[xTINCeG:ydH;zbZMhSXO|YYm= NXz4NXhUOC1zMDFOwG0> NX32V5hUOjRiaB?= M1zsV2ROW09? NGHjfGdqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXn6foxmOjZ3NUK3NVI>
MC-3  NUTjV|ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDqfIY2NzFyL{KwJO69VQ>? MmLSNlQhcA>? NUK0UmpWTE2VTx?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoriNlY1PDd4MUW=
HN22  NEe5SmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XJcFIvPS95LkWvNlIvPSEQvF2= NXO2ZppQOjRiaB?= MnPXSG1UVw>? MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVmyOlQ1PzZzNR?=
MC-3  NYP6Oo84SXCxcITvd4l{KEG|c3H5 NFzoV4s2NzFyL{KwJO69VQ>? NW\UVm9ROjRiaB?= M3HTRmROW09? MnrLbY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= M3TCR|I3PDR5NkG1
HN22  NUTpWZc3SXCxcITvd4l{KEG|c3H5 MlXGNk42NzdwNT:yNk42KM7:TR?= MoPsNlQhcA>? MofySG1UVw>? NEnlPHpqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz MkfLNlY1PDd4MUW=
MOLT-4 NWTxe|Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCxNE02ODByIH7N MlLLO|IhcA>? M3r6R2ROW09? MUHJR|UxRTBwMUm4JO69VQ>? M4L6cVI3Ozl{M{Oy
RS4;11 NXLJdnZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;pbHlKOTBvNUCwNEBvVQ>? MnjoO|IhcA>? M136fWROW09? MnnVTWM2OD1yLkCwNkDPxE1? NV\EdXA{OjZ|OUKzN|I>
JURKAT NVvkZW9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofmNVAuPTByMDDuUS=> M13CTFczKGh? NXfIUnp{TE2VTx?= M4Dy[2lEPTB;Nk[g{txO NYTMNplbOjZ|OUKzN|I>
CEM R MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3XNVAuPTByMDDuUS=> M{LnU|czKGh? NH;YcnVFVVOR NIDXNWxKSzVyPUWuOEDPxE1? M1P5dlI3Ozl{M{Oy
CEM S NES0cVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:wNVAuPTByMDDuUS=> NUfCUHZ2PzJiaB?= MlrrSG1UVw>? Mm\STWM2OD1zMj6xJO69VQ>? Mm\nNlY{QTJ|M{K=
MOLT-4 MUXBdI9xfG:|aYOgRZN{[Xl? M4jxbVExNTFyMECgcm0> NIm5NW0zPCCq Ml\TSG1UVw>? MUPjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= M4T0WlI3Ozl{M{Oy
CEM S NF;MTo5CeG:ydH;zbZMhSXO|YYm= MlPkNVAuOTByMDDuUS=> MkT5NlQhcA>? Mnr2SG1UVw>? M2nV[oNifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x NX;2VFlzOjZ|OUKzN|I>
JURKAT NE\mWJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[xNFAuOTByMDDuUS=> MnLOOFghcA>? M2C4[2ROW09? NVLsUIpHUUN3ME25OVXDuTlwMzDuUS=> NH3XUFEzPjF5MkK2PS=>
LOUCY MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf2b|AyODBvMUCwNEBvVQ>? NFzlUXo1QCCq M1SyOGROW09? MX3JR|UxRTN{LklCtVExNjlibl2= NEf6cGUzPjF5MkK2PS=>
WM-115 NVGxdYN4S2WubDDWbYFjcWyrdImgRZN{[Xl? Mk\PNVAxyqCwTR?= M2SzOlczKGh? MlrX[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? NGfOcIwzPjFzNke3Oi=>
B16 MnLiR4VtdCCYaXHibYxqfHliQYPzZZk> NVu2cHBiOTBywrDuUS=> Ml7XO|IhcA>? NHfDOWNmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= NITYdmwzPjFzNke3Oi=>
HL-60  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWG3NkBp MnzkTWM2OMLiPTCxNE44KG6P MViyOlA1PTZyOR?=
MOLM-13  MlLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[0RYtXPzJiaB?= NEPzVm1KSzVywrC9JFI4Njlibl2= MXmyOlA1PTZyOR?=
OCI-AML3 NHnuRZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUK3NkBp NGfrW5FKSzVywrC9JFE6PTBibl2= M1u5b|I3ODR3NkC5
BCWM.1 MVPBdI9xfG:|aYOgRZN{[Xl? NH7qN3ExNTFwNjFOwG0> M4na[|I1KGh? MnT5bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MXOyOVg6OzJ7MB?=
MWCL-1 MkPyRZBweHSxc3nzJGF{e2G7 MWmwMVEvPiEQvF2= Mk\UNlQhcA>? M13hZYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NXrEb5JROjV6OUOyPVA>
MM.1s M{[wZmFxd3C2b4Ppd{BCe3OjeR?= M1y0XlAuOS54IN88US=> NGTFWYEzPCCq MlvJbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NHW5fIgzPTh7M{K5NC=>
HCT116 MmH4SpVv[3Srb36gRZN{[Xl? MV2zM|ExKM7:TR?= NF7Qd3YyOsLiaNMg M{TybWROW09? NVzMdGRncW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u MWmyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO Mom2SpVv[3Srb36gRZN{[Xl? NHrMOVQ{NzFyIN88US=> MVKxNuKhcMLi MV;EUXNQ MWLpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? NUHoeFhIOjV5MUWwNlg>
HCT116 M1fNfWZ2dmO2aX;uJGF{e2G7 NFzVU|IyOCEQvF2= NXX2XGF5OTMEoHlCpC=> MYPEUXNQ M{TWSolv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= NIHNPFczPTdzNUCyPC=>
HCT116 BAX BAK1 DKO MlToSpVv[3Srb36gRZN{[Xl? MlzpNVAh|ryP MkjJNVLDqGkEoB?= M3HxO2ROW09? NUnNbW5JcW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> NWH6Sod[OjV5MUWwNlg>
HCT116 NFTIO3dCfXSxcHjh[5khSXO|YYm= MlXGNVAh|ryP NH\OcocyOsLiaNMg M3vYR2ROW09? MoDSbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> M{DVZlI2PzF3MEK4
HCT116 BAX BAK1 DKO M2\QTGF2fG:yaHHnfUBCe3OjeR?= MWCxNEDPxE1? MX[xNuKhcMLi MUDEUXNQ NGPpNHVqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? M321[lI2PzF3MEK4
U937 MlTERZBweHSxc3nzJGF{e2G7 NYjXe5dzOC5zMkWtNkDPxE1? M{fPclI1KGh? MmfI[Y5p[W6lZYOgSGhCN1hvMUGtbY5lfWOnZDDhdI9xfG:|aYO= MYCyOVcyPDB{NB?=
U937  NXfpW5RmSXCxcITvd4l{KEG|c3H5 MVewMlUh|ryP MnHoNlQhcA>? M4CyV4VvcGGwY3XzJINt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UuOyCjczD3[YxtKGG|IF7vfIEhdGW4ZXy= NYnS[mtSOjV5MUSwNlQ>
HL-60 AAA-Bcl-2 MVPBdI9xfG:|aYOgRZN{[Xl? NXLSOnFHOC13IN88US=> NIjTbnk1QCCq NYDC[YtyUUN3ME2wMlg4KM7:bf-8kIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXTNUHVVOjV5MUG0OlA>
HL-60 EEE-Bcl-2 M3;4fWFxd3C2b4Ppd{BCe3OjeR?= MljlNE02KM7:TR?= NFHGSYo1QCCq MkLTTWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlvSNlU4OTF2NkC=
U87 M3zHXGZ2dmO2aX;uJGF{e2G7 NHG2[IY2OCEQvF2= MoTVNlQhcA>? MojndoVlfWOnczD0bIUhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?= Mmr2NlU3Pjd4NkO=
K562 MmHSR4VtdCCYaXHibYxqfHliQYPzZZk> NFTXfpgyNTFyIN88US=> NE\DfoU1QCCq MmfiSG1UVw>? MmX6TWM2OD1{Nj63JO69VQ>? NUDtbGt3OjV3OU[1OlE>
K562/Mcl -1-IRESBim NGmxUI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17wUWlEPTB;OT6zJO69VQ>? MYCyOVU{PTlyMB?=
K562/Bcl- 2-IRESBim M4HjXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTMTWM2OD1yLkO1JO69VQ>? NIfwZmwzPTV|NUmwNC=>
Jurkat Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXWOVNXUUN3ME2wMlY3KM7:TR?= Mlv3NlU2OzV7MEC=
JurkatΔBak M1G3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvoVndKSzVyPkWwJO69VQ>? NVLkXoFYOjV3M{W5NFA>
HL60/VCR M1\Sdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj0TWM2OD5zMECg{txO MUiyOVU{PTlyMB?=
Kasumi-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnqVYlxUUN3ME2wMlAyKM7:TR?= MnW2NlU2OzV7MEC=
Kasumi-1/ABT NWTXUmRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwNUGg{txO NGS3VXkzPTV|NUmwNC=>
THP-1 Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTFwMkeg{txO NHvsO4IzPTV|NUmwNC=>
U937 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\SN2lEPTB;NT6yPUDPxE1? MUOyOVU{PTlyMB?=
C1498 NVfWeJVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTZwMUOg{txO MX2yOVU{PTlyMB?=
RPMI 8226 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\nTWM2OD1yLkK1JO69VQ>? NEPUe2QzPTV|NUmwNC=>
MM.1S MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjETWM2OD1yLkSwJO69VQ>? NUfrRYR5OjV3M{W5NFA>
NCI-H929 Mo[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HCUWlEPTB;MUWuNlEh|ryP NFftVGQzPTV|NUmwNC=>
U266 NXnQNFV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjRTWM2OD1yLk[4JO69VQ>? MYCyOVU{PTlyMB?=
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[4]

+ 展開
  • 細胞株: SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
  • 濃度: 0.001-10 μM
  • 反応時間: 48 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
  • 製剤: 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%)
  • 投薬量: 20 and 30 mg/kg
  • 投与方法: For intraperitoneal (i.p.) every day
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (122.93 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% Propylene glycol, 5% Tween 80, 65% D5W
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 813.43
化学式

C42H45ClN6O5S2

CAS No. 852808-04-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What’s the recommended method about reconstitution of the compound for in vivo animal study?

  • 回答:

    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シグナル伝達経路

Bcl-2 Inhibitors with Unique Features

相関Bcl-2製品

Tags: ABT-737を買う | ABT-737 ic50 | ABT-737供給者 | ABT-737を購入する | ABT-737費用 | ABT-737生産者 | オーダーABT-737 | ABT-737化学構造 | ABT-737分子量 | ABT-737代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID