ABT-737

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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ABT-737 化学構造
分子量: 813.43

高品質保証

文献中の引用(88)

カスタマーフィードバック(14)

MSDS

製品説明

  • Compare Bcl-2 Inhibitors
    Bcl-2製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • ABT-737のメカニズム

製品の説明

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。
ターゲット

Bcl-xL

Bcl-2

Bcl-w

IC50

78.7 nM (EC50)

30.3 nM (EC50)

197.8 nM (EC50) [1]

In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
OCI-Ly1  MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGqxco4zPTBibl5CpC=> NVvpT4JTPzJiaB?= M4ftXmROW09? NXvBb3hl[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? MoH4NlY3PTd{OEi=
KG1a MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mof6NE0yOCEQvF2= MlXPNlQhcA>? M4HOPWROW09? NVj5coR4UUN3ME23MlY5KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M4f4TlI3PTV{N{Gy
Kasumi-1 NIDTN|hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXPJRotqOC1zMDFOwG0> M3PmS|I1KGh? NGHmd49FVVOR M37GdGlEPTB;ND64O{DPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVvzZnBGOjZ3NUK3NVI>
KG1a MlXIRZBweHSxc3nzJGF{e2G7 MYmwMVExKM7:TR?= NHHORnIzPCCq NWXqfY5HTE2VTx?= NGrYSnFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MoLYNlY2PTJ5MUK=
Kasumi-1 MnPQRZBweHSxc3nzJGF{e2G7 NHzTc2oxNTFyIN88US=> Mlq1NlQhcA>? NYrHZ|F{TE2VTx?= NUPE[5BOcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NHfZPGgzPjV3MkexNi=>
MC-3  M4CxZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DWS|UwOTBxMkCg{txO NFv0TYMzPCCq NHez[5dFVVOR M1n5dYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NI\oToIzPjR2N{[xOS=>
HN22  MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\vNk42NzdwNT:yNk42KM7:TR?= NIPrd4MzPCCq NYH2V3k3TE2VTx?= MmS1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWXtZYJTOjZ2NEe2NVU>
MC-3  M{PsVWFxd3C2b4Ppd{BCe3OjeR?= MlXXOU8yOC9{MDFOwG0> NW\zPG5POjRiaB?= MojySG1UVw>? NH3xXWhqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz MkTpNlY1PDd4MUW=
HN22  MmXYRZBweHSxc3nzJGF{e2G7 M1LJUFIvPS95LkWvNlIvPSEQvF2= NVnXUmFlOjRiaB?= M4[z[mROW09? NFfCb5VqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz NV7zeoM5OjZ2NEe2NVU>
MOLT-4 MknLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfENVAuPTByMDDuUS=> M1\wPFczKGh? NF;DV3dFVVOR MXvJR|UxRTBwMUm4JO69VQ>? NYThVZlLOjZ|OUKzN|I>
RS4;11 Ml7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfMbWEyOC13MECwJI5O MVi3NkBp NWHKNItJTE2VTx?= M{LuNmlEPTB;MD6wNFIh|ryP M1zFS|I3Ozl{M{Oy
JURKAT M4fLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf3NVAuPTByMDDuUS=> MlvOO|IhcA>? MnXkSG1UVw>? M2e3UWlEPTB;Nk[g{txO NUDxSJVzOjZ|OUKzN|I>
CEM R NETmNWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fR[|ExNTVyMECgcm0> MoDIO|IhcA>? MWHEUXNQ MkHtTWM2OD13LkSg{txO NUnHVYFROjZ|OUKzN|I>
CEM S MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TTelExNTVyMECgcm0> MlnDO|IhcA>? NGHhW2ZFVVOR MlL0TWM2OD1zMj6xJO69VQ>? Mn;MNlY{QTJ|M{K=
MOLT-4 MlPyRZBweHSxc3nzJGF{e2G7 NWjScVQyOTBvMUCwNEBvVQ>? NUC5XIdSOjRiaB?= NX7pT3JiTE2VTx?= NFz3O3hk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> MlHPNlY{QTJ|M{K=
CEM S MWHBdI9xfG:|aYOgRZN{[Xl? NY\DVVdOOTBvMUCwNEBvVQ>? NXuxbZBqOjRiaB?= M2fwe2ROW09? MW\jZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= MVqyOlM6OjN|Mh?=
JURKAT M{HPUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7ubFU1OTByLUGwNFAhdk1? M{H5O|Q5KGh? NF;xOFhFVVOR Mkf5TWM2OD17NUZCtVkvOyCwTR?= NHy2WnIzPjF5MkK2PS=>
LOUCY NXXWdHhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITO[GsyODBvMUCwNEBvVQ>? MVq0PEBp NEXsfHBFVVOR M3qwRWlEPTB;M{KuPOKyOTBwOTDuUS=> Mmi2NlYyPzJ{Nkm=
WM-115 M{T0VGNmdGxiVnnhZoltcXS7IFHzd4F6 NFr0epcyODEEoH7N MmfkO|IhcA>? NVTRbHNW\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= NWr3bWxkOjZzMU[3O|Y>
B16 NUS4S|VZS2WubDDWbYFjcWyrdImgRZN{[Xl? MVOxNFDDqG6P NX;me5dkPzJiaB?= MkTP[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? Mm\QNlYyOTZ5N{[=
HL-60  M17ROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWC3NkBp NWXLU|ZuUUN3MNMgQUAyOC55IH7N NGfxSIYzPjB2NU[wPS=>
MOLM-13  M3LBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYX4fo86PzJiaB?= MlXWTWM2OMLiPTCyO{46KG6P M1\mTFI3ODR3NkC5
OCI-AML3 NYjmbGV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XUR|czKGh? MUPJR|UxyqB;IEG5OVAhdk1? M37xWlI3ODR3NkC5
BCWM.1 Moi2RZBweHSxc3nzJGF{e2G7 NF\kbI0xNTFwNjFOwG0> NUHZS|llOjRiaB?= Ml7hbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MlXkNlU5QTN{OUC=
MWCL-1 M3HwNmFxd3C2b4Ppd{BCe3OjeR?= MljTNE0yNjZizszN MnLINlQhcA>? MYXpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NV30OpdvOjV6OUOyPVA>
MM.1s M17k[WFxd3C2b4Ppd{BCe3OjeR?= MWSwMVEvPiEQvF2= MVOyOEBp MXjpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MVuyOVg6OzJ7MB?=
HCT116 MljUSpVv[3Srb36gRZN{[Xl? M4TSXFMwOTBizszN NFXheVAyOsLiaNMg NWKyeXhMTE2VTx?= Mo\TbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w MlviNlU4OTVyMki=
HCT116 BAX BAK1 DKO NULhUHluTnWwY4Tpc44hSXO|YYm= MmHrN{8yOCEQvF2= M4PoWFEzyqCqwrC= NUnRfYM4TE2VTx?= NXm4flM2cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u NXzpcGlLOjV5MUWwNlg>
HCT116 NXXSfZd6TnWwY4Tpc44hSXO|YYm= NGDkZ3EyOCEQvF2= MnruNVLDqGkEoB?= MofwSG1UVw>? NIfLVGFqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th MkHSNlU4OTVyMki=
HCT116 BAX BAK1 DKO MlzJSpVv[3Srb36gRZN{[Xl? MX[xNEDPxE1? M4nCZVEzyqCqwrC= NIWyRY1FVVOR MYjpcoNz\WG|ZYOgS2ZRNUyFM1KgdJVv[3Sj MmDGNlU4OTVyMki=
HCT116 M2m1UmF2fG:yaHHnfUBCe3OjeR?= M{HyOVExKM7:TR?= NWHHSIR6OTMEoHlCpC=> MmPjSG1UVw>? NEHmcYRqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? MUKyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO NWXRV4JNSXW2b4DoZYd6KEG|c3H5 M{DEWVExKM7:TR?= MYWxNuKhcMLi Mln2SG1UVw>? M4PYbolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm M{i2c|I2PzF3MEK4
U937 M{noU2Fxd3C2b4Ppd{BCe3OjeR?= M4j6bFAvOTJ3LUKg{txO NHvuUmUzPCCq MkT2[Y5p[W6lZYOgSGhCN1hvMUGtbY5lfWOnZDDhdI9xfG:|aYO= M2mwdlI2PzF2MEK0
U937  NHrhbmtCeG:ydH;zbZMhSXO|YYm= NHHJV3MxNjVizszN Mnf1NlQhcA>? MWTlcohidmOnczDjcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlMVMh[XNid3XscEBieyCQb4jhJIxmfmWu MVWyOVcyPDB{NB?=
HL-60 AAA-Bcl-2 M3zpUmFxd3C2b4Ppd{BCe3OjeR?= NXfxNopLOC13IN88US=> MV20PEBp Mn;ZTWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1HzfFI2PzFzNE[w
HL-60 EEE-Bcl-2 M13IfmFxd3C2b4Ppd{BCe3OjeR?= NFjIXIQxNTVizszN MXq0PEBp MkHjTWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYSyOVcyOTR4MB?=
U87 M3z4OGZ2dmO2aX;uJGF{e2G7 NXy3dXkyPTBizszN Mn\1NlQhcA>? M{fqUpJm\HWlZYOgeIhmKG2UTlGg[ZhxemW|c3nvckBt\X[nbIOgc4YhVU2SLUKsJG1OWC1zNDDhcoQhSmOuLUK= MkXRNlU3Pjd4NkO=
K562 NWDWcFRMS2WubDDWbYFjcWyrdImgRZN{[Xl? MnLyNU0yOCEQvF2= M1;NZ|Q5KGh? NH7jbpZFVVOR MVjJR|UxRTJ4Lkeg{txO Mn75NlU2QTZ3NkG=
K562/Mcl -1-IRESBim M3ntdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn1b|hKSzVyPUmuN{DPxE1? NW\vdFg{OjV3M{W5NFA>
K562/Bcl- 2-IRESBim M3nMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfmPXNKSzVyPUCuN|Uh|ryP M2i1TFI2PTN3OUCw
Jurkat NWXpb3JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1eyNmlEPTB;MD62OkDPxE1? MVyyOVU{PTlyMB?=
JurkatΔBak NVjIWZRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRjVyIN88US=> NEi3VmwzPTV|NUmwNC=>
HL60/VCR M3XRfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LHW2lEPTB-MUCwJO69VQ>? Ml65NlU2OzV7MEC=
Kasumi-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwMEGg{txO NI\4U5ozPTV|NUmwNC=>
Kasumi-1/ABT MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\DTWM2OD1yLkWxJO69VQ>? MnPUNlU2OzV7MEC=
THP-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFwMkeg{txO MlK0NlU2OzV7MEC=
U937 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nWeWlEPTB;NT6yPUDPxE1? NGHUPZMzPTV|NUmwNC=>
C1498 MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPXVHVtUUN3ME22MlE{KM7:TR?= MWCyOVU{PTlyMB?=
RPMI 8226 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHTZ5ZUUUN3ME2wMlI2KM7:TR?= Mm\aNlU2OzV7MEC=
MM.1S M1r4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwNECg{txO M3z5RVI2PTN3OUCw
NCI-H929 M2LWTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnlPItoUUN3ME2xOU4zOSEQvF2= MYqyOVU{PTlyMB?=
U266 MkLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHwUmFKSzVyPUCuOlgh|ryP NWXCNmNYOjV3M{W5NFA>
MCF-7 NWm0XYVxS2WubDDWbYFjcWyrdImgRZN{[Xl? M1nkXVUh|ryP NHnsXos1QCCq MYrEUXNQ MVrlcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v NUW2ZWJ[OjV2MEmxNlQ>
MCF-7 MoPIRZBweHSxc3nzJGF{e2G7 M2PvVFUh|ryP MX20M|I1NzR6IHi= NI\6SZRFVVOR MnLKbY5kemWjc3XzJJRp\SClbHXheoVlKFCDUmC= NXnnPVE{OjV2MEmxNlQ>
MCF-7 NXr1UZBGTnWwY4Tpc44hSXO|YYm= Ml31OUDPxE1? MlLVNlQhcA>? M3vwNWROW09? NXrmZnhW\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi NVzPXIlTOjV2MEmxNlQ>
MDA-MB 231  Mlr5SpVv[3Srb36gRZN{[Xl? MYS1JO69VQ>? MViyOEBp NHnwS5hFVVOR NXrTVXNU\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi NHywNXYzPTRyOUGyOC=>
ZR-75-1  NIPIcZRHfW6ldHnvckBCe3OjeR?= M4nORVUh|ryP NGXHfGozPCCq Mn7tSG1UVw>? M2DLe4VvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NGewbHczPTRyOUGyOC=>
A549 M2DkRmNmdGxiVnnhZoltcXS7IFHzd4F6 MYOwMVIxKM7:TR?= MX[3NkBp NES2NJBFVVOR NHmyXIpl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw MV6yOVM5QDd4Mh?=
H1299 NYrZRXROS2WubDDWbYFjcWyrdImgRZN{[Xl? MkG3NE0zOCEQvF2= NXvnfYJWPzJiaB?= MlrUSG1UVw>? NEfIdZZl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NXvJcItPOjV|OEi3OlI>
HO-8910 NWjBVnJmS2WubDDWbYFjcWyrdImgRZN{[Xl? MnTiNE0zOCEQvF2= M3e1eFczKGh? MXTEUXNQ NX\YZ3R6\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= M1zKPVI2Ozh6N{[y
HT-29 M2P3WWNmdGxiVnnhZoltcXS7IFHzd4F6 M3zydlAuOjBizszN MlyyO|IhcA>? NFTHfZZFVVOR MWDk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NIHSZlEzPTN6OEe2Ni=>
HCT-116 NWT3ZVR{S2WubDDWbYFjcWyrdImgRZN{[Xl? MUewMVIxKM7:TR?= NUTGSlVNPzJiaB?= MYrEUXNQ NH;6PWll\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NXPrN3RMOjV|OEi3OlI>
A549 MVzBdI9xfG:|aYOgRZN{[Xl? MkLENlAh|ryP NEL6d3Q1QCCq NYrGZmJ2TE2VTx?= NYrURYx2cW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> NYq3XlNUOjV|OEi3OlI>
H1299 M{DsVWFxd3C2b4Ppd{BCe3OjeR?= M2PQc|IxKM7:TR?= M1HzTVQ5KGh? MofOSG1UVw>? MVTpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NHLIeFgzPTN6OEe2Ni=>
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... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験 ABT-737, associated with Platinum, is currently under Phase II clinical trials in ovarian tumors.
特集 First-generation inhibitor of anti-apoptotic Bcl-2 proteins.

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

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.

細胞アッセイ:

[4]

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.

動物実験:

[1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download ABT-737 SDF
分子量 813.43
化学式

C42H45ClN6O5S2

CAS No. 852808-04-9
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (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.
化学名 Benzamide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]-

文献中の引用 (88)

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.

技術サポート&よくある質問(FAQ)

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。

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他の質問がある場合は、お気軽くお問合せください。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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