ABT-737

製品コードS1002

ABT-737化学構造

分子量(MW):813.43

ABT-737は一種のBH3模倣の阻害剤で、無細胞試験でBcl-xL、Bcl-2とBcl-wに作用する時のEC50値が78.7 nM、30.3 nMと197.8 nMにそれぞれ分かれることですが、Mcl-1、Bcl-BとBfl-1を抑制する作用がありません。臨床2期。

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カスタマーフィードバック(16)

  • 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.

    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.

    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は一種のBH3模倣の阻害剤で、無細胞試験でBcl-xL、Bcl-2とBcl-wに作用する時のEC50値が78.7 nM、30.3 nMと197.8 nMにそれぞれ分かれることですが、Mcl-1、Bcl-BとBfl-1を抑制する作用がありません。臨床2期。
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)
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)
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  MkK4R4VtdCCYaXHibYxqfHliQYPzZZk> MVuyOVAhdk4EoB?= MoLLO|IhcA>? NHrO[4ZFVVOR MVjjZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRmNNPiC|aWLORS=> MUiyOlY2PzJ6OB?=
KG1a Mn3JR4VtdCCYaXHibYxqfHliQYPzZZk> M3LBTlAuOTBizszN M4\0PFI1KGh? NETh[4FFVVOR M3jic2lEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MV[yOlU2OjdzMh?=
Kasumi-1 NXyzXnpvS2WubDDWbYFjcWyrdImgRZN{[Xl? NFW0OYkxNTFyIN88US=> MoXYNlQhcA>? Mlm3SG1UVw>? MVnJR|UxRTRwOEeg{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M4HmVVI3PTV{N{Gy
KG1a MYjBdI9xfG:|aYOgRZN{[Xl? MXKwMVExKM7:TR?= NYPjOFVUOjRiaB?= NE\lO5pFVVOR NHnGOodqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NEj1SJgzPjV3MkexNi=>
Kasumi-1 MVzBdI9xfG:|aYOgRZN{[Xl? M160VlAuOTBizszN NXjkO4hLOjRiaB?= NVzhSZA5TE2VTx?= NH3ReIZqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M1nBe|I3PTV{N{Gy
MC-3  MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC5OU8yOC9{MDFOwG0> NGLuSFQzPCCq M1f2bGROW09? MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWD0TJF7OjZ2NEe2NVU>
HN22  MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm3NpBmOi53L{euOU8zOi53IN88US=> NUH4WpBTOjRiaB?= MWHEUXNQ NHPs[2NqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXTuem0zOjZ2NEe2NVU>
MC-3  MlHuRZBweHSxc3nzJGF{e2G7 M3rE[FUwOTBxMkCg{txO NUjTTm9pOjRiaB?= NI\Ne45FVVOR MWjpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| NXu3b4NCOjZ2NEe2NVU>
HN22  MYPBdI9xfG:|aYOgRZN{[Xl? MVqyMlUwPy53L{KyMlUh|ryP NFHwNHQzPCCq MlzCSG1UVw>? NEfuSHpqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz NFjKd24zPjR2N{[xOS=>
MOLT-4 MmDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlThNVAuPTByMDDuUS=> Ml3iO|IhcA>? NE\6d3NFVVOR MYDJR|UxRTBwMUm4JO69VQ>? NW\qRol3OjZ|OUKzN|I>
RS4;11 M33pTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljlNVAuPTByMDDuUS=> NXXIOHV3PzJiaB?= NIPRNGZFVVOR MmnSTWM2OD1yLkCwNkDPxE1? MWOyOlM6OjN|Mh?=
JURKAT NYLkVXJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnWdJkyOC13MECwJI5O NWPhV4I{PzJiaB?= NVz0fJhNTE2VTx?= MmDJTWM2OD14NjFOwG0> NEDQb4szPjN7MkOzNi=>
CEM R NGLnNJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnuOYVYOTBvNUCwNEBvVQ>? NFHmVZg4OiCq NUXGVo1iTE2VTx?= MXTJR|UxRTVwNDFOwG0> MmDlNlY{QTJ|M{K=
CEM S MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe2V5JkOTBvNUCwNEBvVQ>? MkDhO|IhcA>? MoS5SG1UVw>? NWjy[ZA2UUN3ME2xNk4yKM7:TR?= MoDhNlY{QTJ|M{K=
MOLT-4 MWXBdI9xfG:|aYOgRZN{[Xl? MUWxNE0yODByIH7N NEftbHUzPCCq MlnzSG1UVw>? MkPyZ4F2e2W|IITo[UBkdGWjdnHn[UBw\iCEY3ytNkBidmRidHjlJIRwf26{ZXf1cIF1cW:wIH;mJGJkdC26TDDhcoQhVWOuLUG= NWDpUmdvOjZ|OUKzN|I>
CEM S MWTBdI9xfG:|aYOgRZN{[Xl? MVSxNE0yODByIH7N NHi2RmwzPCCq NF[zcVVFVVOR MYfjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= NXHmRYxlOjZ|OUKzN|I>
JURKAT M3X5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTCfHFTOTByLUGwNFAhdk1? MkXMOFghcA>? MVzEUXNQ NXr1c3FmUUN3ME25OVXDuTlwMzDuUS=> M{HEc|I3OTd{Mk[5
LOUCY MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7jRXM1OTByLUGwNFAhdk1? M2X6PVQ5KGh? NXTOdmlSTE2VTx?= Mn3ZTWM2OD1|Mj64xtEyOC57IH7N NETaUnEzPjF5MkK2PS=>
WM-115 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnLpNVAxyqCwTR?= MWq3NkBp MnzD[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? M2X5U|I3OTF4N{e2
B16 NYP1SYY{S2WubDDWbYFjcWyrdImgRZN{[Xl? NX\ITHAyOTBywrDuUS=> NEficpU4OiCq M{S3V4VvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi MmPpNlYyOTZ5N{[=
HL-60  M3zINGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\XO403PzJiaB?= NH6wZohKSzVywrC9JFExNjdibl2= MnHwNlYxPDV4MEm=
MOLM-13  NGrrPI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\NXGhyPzJiaB?= MoS0TWM2OMLiPTCyO{46KG6P MlnENlYxPDV4MEm=
OCI-AML3 NYXNSmRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEntd|M4OiCq MoX5TWM2OMLiPTCxPVUxKG6P NEPyVWIzPjB2NU[wPS=>
BCWM.1 M2nTVGFxd3C2b4Ppd{BCe3OjeR?= M1LlU|AuOS54IN88US=> NVH0bGplOjRiaB?= NWXSSpZ4cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NYTOUYVjOjV6OUOyPVA>
MWCL-1 NVjSRXpDSXCxcITvd4l{KEG|c3H5 MVSwMVEvPiEQvF2= M1H5[FI1KGh? M1rJOolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MUCyOVg6OzJ7MB?=
MM.1s M2nMVmFxd3C2b4Ppd{BCe3OjeR?= MYCwMVEvPiEQvF2= M{TYWFI1KGh? NYmy[od5cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NX3WPJJUOjV6OUOyPVA>
HCT116 MoPHSpVv[3Srb36gRZN{[Xl? M17q[|MwOTBizszN MWWxNuKhcMLi M4fnPGROW09? NH[1RoJqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= MoHsNlU4OTVyMki=
HCT116 BAX BAK1 DKO MlexSpVv[3Srb36gRZN{[Xl? MVSzM|ExKM7:TR?= M3zuUlEzyqCqwrC= MX\EUXNQ NUDOb5ZJcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u NELwVFEzPTdzNUCyPC=>
HCT116 MmPTSpVv[3Srb36gRZN{[Xl? M33OZlExKM7:TR?= MXOxNuKhcMLi NVS2VVFkTE2VTx?= M1rZXIlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= MnvQNlU4OTVyMki=
HCT116 BAX BAK1 DKO M3PndGZ2dmO2aX;uJGF{e2G7 M3vKXFExKM7:TR?= MUexNuKhcMLi NXv2UJFnTE2VTx?= MkL2bY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= MWKyOVcyPTB{OB?=
HCT116 Mn7aRZV1d3CqYXf5JGF{e2G7 NX3FeJBwOTBizszN NGjQblQyOsLiaNMg MofxSG1UVw>? NEjoe4lqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? M1\3PFI2PzF3MEK4
HCT116 BAX BAK1 DKO NVnVXHNZSXW2b4DoZYd6KEG|c3H5 MoPzNVAh|ryP NVzadG5SOTMEoHlCpC=> NIHmephFVVOR MkHWbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> M363clI2PzF3MEK4
U937 NG\jW4dCeG:ydH;zbZMhSXO|YYm= M2q0c|AvOTJ3LUKg{txO NFnYS4YzPCCq M1fwboVvcGGwY3XzJGRJSS:[LUGxMYlv\HWlZXSgZZBweHSxc3nz MY[yOVcyPDB{NB?=
U937  NFnFNIJCeG:ydH;zbZMhSXO|YYm= MXiwMlUh|ryP NVzvVHpVOjRiaB?= NHrxWohmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs NESwNnUzPTdzNECyOC=>
HL-60 AAA-Bcl-2 MVHBdI9xfG:|aYOgRZN{[Xl? Mnr5NE02KM7:TR?= MUm0PEBp MWPJR|UxRTBwOEeg{txu97zOaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoHRNlU4OTF2NkC=
HL-60 EEE-Bcl-2 MX;BdI9xfG:|aYOgRZN{[Xl? M1HLd|AuPSEQvF2= NETKNW81QCCq MoTITWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NU\zXJd5OjV5MUG0OlA>
U87 NIKxSXZHfW6ldHnvckBCe3OjeR?= MXq1NEDPxE1? M1XHblI1KGh? MorZdoVlfWOnczD0bIUhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?= NHfXPWIzPTZ4N{[2Ny=>
K562 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYLxPWUxOS1zMDFOwG0> MX[0PEBp M{L5UGROW09? MUfJR|UxRTJ4Lkeg{txO NGTRSnYzPTV7NkW2NS=>
K562/Mcl -1-IRESBim MnzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvjTWM2OD17LkOg{txO MljjNlU2OzV7MEC=
K562/Bcl- 2-IRESBim NUHxV5FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwM{Wg{txO NV;JPXhPOjV3M{W5NFA>
Jurkat NInNcG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\HPHVKSzVyPUCuOlYh|ryP M3zw[VI2PTN3OUCw
JurkatΔBak NUO4RVlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PVW2lEPTB-NUCg{txO Mn[3NlU2OzV7MEC=
HL60/VCR NGPV[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUW1S|R6UUN3ME6xNFAh|ryP NEDlSZgzPTV|NUmwNC=>
Kasumi-1 NFPvSG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\OTWM2OD1yLkCxJO69VQ>? NGjNSWwzPTV|NUmwNC=>
Kasumi-1/ABT NEj6VoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rDXWlEPTB;MD61NUDPxE1? MlrrNlU2OzV7MEC=
THP-1 NYnnW3ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXYVGxKSzVyPUGuNlch|ryP MWeyOVU{PTlyMB?=
U937 M3y0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\KVJFQUUN3ME21MlI6KM7:TR?= NXjoSXFJOjV3M{W5NFA>
C1498 M3;QNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTZwMUOg{txO NVfze3hnOjV3M{W5NFA>
RPMI 8226 M1v6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn6TWM2OD1yLkK1JO69VQ>? MVmyOVU{PTlyMB?=
MM.1S NIrrdFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfxPXFKSzVyPUCuOFAh|ryP MUGyOVU{PTlyMB?=
NCI-H929 Mo\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzVTWM2OD1zNT6yNUDPxE1? MXyyOVU{PTlyMB?=
U266 M3PXcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTBwNkig{txO M2TmWlI2PTN3OUCw
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多くの細胞株試験データを見る場合、クリックしてください

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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% Propylene glycol, 5% Tween 80, 65% D5W
30mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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信号経路図

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