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、Bcl-xL、Bcl-2とBcl-wのBH3模倣の阻害剤で、EC50 がそれぞれ78.7 nM、30.3 nM 、197.8 nMになる。
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  MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NX\tZ2Y4OjVyIH7NxsA> NUPmZ3E{PzJiaB?= NX7oNWs3TE2VTx?= M3PwV4NifXOnZDC5O{UhdG:|czDv[kB3cWGkaXzpeJkhcW5iY3XscJMhfHKjboPm[YN1\WRid3n0bEBDS0x4IIPpVm5C NWfHfFBwOjZ4NUeyPFg>
KG1a M3jjRmNmdGxiVnnhZoltcXS7IFHzd4F6 M1vER|AuOTBizszN MWmyOEBp MkTXSG1UVw>? MWXJR|UxRTdwNkig{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2HVVFI3PTV{N{Gy
Kasumi-1 Moq4R4VtdCCYaXHibYxqfHliQYPzZZk> NVXxO4lpOC1zMDFOwG0> NH\BT4MzPCCq NH;JSIZFVVOR MWfJR|UxRTRwOEeg{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGXabnQzPjV3MkexNi=>
KG1a M1m5XmFxd3C2b4Ppd{BCe3OjeR?= MXqwMVExKM7:TR?= MVqyOEBp NYjoeGM1TE2VTx?= NFjyOZBqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MoHPNlY2PTJ5MUK=
Kasumi-1 NGT3TWhCeG:ydH;zbZMhSXO|YYm= NVrq[otyOC1zMDFOwG0> MXmyOEBp MYjEUXNQ M2PzZolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MljUNlY2PTJ5MUK=
MC-3  M2r4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HScFUwOTBxMkCg{txO NIrVc2MzPCCq NFfEdVVFVVOR MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHL2TnEzPjR2N{[xOS=>
HN22  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L5V|IvPS95LkWvNlIvPSEQvF2= MYCyOEBp NWjybpF3TE2VTx?= Mm\4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NISxW4gzPjR2N{[xOS=>
MC-3  MXPBdI9xfG:|aYOgRZN{[Xl? M1G3blUwOTBxMkCg{txO M{fsTlI1KGh? NXLBSmNxTE2VTx?= MlWzbY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= M3zYblI3PDR5NkG1
HN22  NFK3b2tCeG:ydH;zbZMhSXO|YYm= MVOyMlUwPy53L{KyMlUh|ryP M2LEfVI1KGh? MojrSG1UVw>? NIfofGhqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz NGe1dI0zPjR2N{[xOS=>
MOLT-4 NGC3cW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{GxO|ExNTVyMECgcm0> M125XFczKGh? M2fYS2ROW09? NV\2b2xFUUN3ME2wMlE6QCEQvF2= MVSyOlM6OjN|Mh?=
RS4;11 M2\CUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnxNVAuPTByMDDuUS=> M1jxUFczKGh? NX[2VVk5TE2VTx?= M1;5OmlEPTB;MD6wNFIh|ryP NWjXcVU5OjZ|OUKzN|I>
JURKAT MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknkNVAuPTByMDDuUS=> MYC3NkBp NYqyNm45TE2VTx?= NHK0O3ZKSzVyPU[2JO69VQ>? M1\PWVI3Ozl{M{Oy
CEM R MkGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfMNVAuPTByMDDuUS=> Mn\yO|IhcA>? MY\EUXNQ MmHVTWM2OD13LkSg{txO MYSyOlM6OjN|Mh?=
CEM S NWfVNWpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxNE02ODByIH7N M4PVOlczKGh? NFXoc5hFVVOR NUTCcI5iUUN3ME2xNk4yKM7:TR?= NFvi[VEzPjN7MkOzNi=>
MOLT-4 MUnBdI9xfG:|aYOgRZN{[Xl? Mle1NVAuOTByMDDuUS=> NFmwZ|czPCCq M37y[WROW09? MULjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= NEfhXnMzPjN7MkOzNi=>
CEM S NIL6UJRCeG:ydH;zbZMhSXO|YYm= NHjRR4EyOC1zMECwJI5O MU[yOEBp NIPEcmVFVVOR MULjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= MXGyOlM6OjN|Mh?=
JURKAT MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxNFAuOTByMDDuUS=> NXrBVHJ3PDhiaB?= NUnUO2dLTE2VTx?= MXfJR|UxRTl3NdMxPU4{KG6P MXWyOlE4OjJ4OR?=
LOUCY NWPKWYFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Hj[VExOC1zMECwJI5O NELHdmo1QCCq NHX0d|hFVVOR NV3mVol5UUN3ME2zNk45yrFzMD65JI5O MlWyNlYyPzJ{Nkm=
WM-115 Ml;LR4VtdCCYaXHibYxqfHliQYPzZZk> MWmxNFDDqG6P MWW3NkBp MVjlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? M4H4VlI3OTF4N{e2
B16 MkXBR4VtdCCYaXHibYxqfHliQYPzZZk> MoLoNVAxyqCwTR?= M3zpOVczKGh? Mmnz[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? NI\Fe3gzPjFzNke3Oi=>
HL-60  Mkf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DPUFczKGh? NWnOW4ZtUUN3MNMgQUAyOC55IH7N NWnvT3pZOjZyNEW2NFk>
MOLM-13  MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorzO|IhcA>? NG\WNVBKSzVywrC9JFI4Njlibl2= MYqyOlA1PTZyOR?=
OCI-AML3 NX[wemVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTiW|Q4OiCq MWLJR|UxyqB;IEG5OVAhdk1? NGj5fYYzPjB2NU[wPS=>
BCWM.1 M3;qPGFxd3C2b4Ppd{BCe3OjeR?= NFTQfJQxNTFwNjFOwG0> MluyNlQhcA>? NIWzZZlqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M{Dmd|I2QDl|Mkmw
MWCL-1 NWfFUHYySXCxcITvd4l{KEG|c3H5 NWHx[3ZVOC1zLk[g{txO MnrQNlQhcA>? NYD1ZYZMcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MYeyOVg6OzJ7MB?=
MM.1s NVjGXodWSXCxcITvd4l{KEG|c3H5 M3y0flAuOS54IN88US=> M4\ydFI1KGh? MoHrbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? Ml7VNlU5QTN{OUC=
HCT116 NVH4VmRzTnWwY4Tpc44hSXO|YYm= MYOzM|ExKM7:TR?= NV;KfJJ2OTMEoHlCpC=> M4X6N2ROW09? MVnpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? MofaNlU4OTVyMki=
HCT116 BAX BAK1 DKO NWe3bJFPTnWwY4Tpc44hSXO|YYm= MVyzM|ExKM7:TR?= NX7CeXNGOTMEoHlCpC=> M2jK[2ROW09? NXLWeZJKcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u NVSwVW1jOjV5MUWwNlg>
HCT116 Ml;0SpVv[3Srb36gRZN{[Xl? NHmybYsyOCEQvF2= NGj5OYIyOsLiaNMg MmTqSG1UVw>? NIXOemJqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th Mn3zNlU4OTVyMki=
HCT116 BAX BAK1 DKO MlHwSpVv[3Srb36gRZN{[Xl? NH74cpEyOCEQvF2= MmTQNVLDqGkEoB?= MVHEUXNQ NXzOcWgycW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MX[yOVcyPTB{OB?=
HCT116 MXfBeZRweGijZ4mgRZN{[Xl? MkXqNVAh|ryP M1myRVEzyqCqwrC= NXO0WIxbTE2VTx?= NX\Cc25ScW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? MVSyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO MXjBeZRweGijZ4mgRZN{[Xl? M322fVExKM7:TR?= MX[xNuKhcMLi MnPQSG1UVw>? NG\UcXRqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? NHvUdVEzPTdzNUCyPC=>
U937 M4PlW2Fxd3C2b4Ppd{BCe3OjeR?= MYmwMlEzPS1{IN88US=> NFTzWpMzPCCq Mo[0[Y5p[W6lZYOgSGhCN1hvMUGtbY5lfWOnZDDhdI9xfG:|aYO= NE\4RpEzPTdzNECyOC=>
U937  MYfBdI9xfG:|aYOgRZN{[Xl? MXmwMlUh|ryP NXOxNm5IOjRiaB?= NVzpWGdU\W6qYX7j[ZMh[2ynYY\h[4Uhd2ZiUFHSVEBidmRiY3HzdIF{\S1|IHHzJJdmdGxiYYOgUo95[SCuZY\lcC=> MojXNlU4OTRyMkS=
HL-60 AAA-Bcl-2 NWLNeYY2SXCxcITvd4l{KEG|c3H5 NIP5bZYxNTVizszN NV;EPXhrPDhiaB?= M2nIWmlEPTB;MD64O{DPxG4xvJzpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmP0NlU4OTF2NkC=
HL-60 EEE-Bcl-2 MUHBdI9xfG:|aYOgRZN{[Xl? MUGwMVUh|ryP MoPHOFghcA>? MnHQTWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnjENlU4OTF2NkC=
U87 MmT3SpVv[3Srb36gRZN{[Xl? MYe1NEDPxE1? NVf5SoNlOjRiaB?= NIj4Z5dz\WS3Y3XzJJRp\SCvUl7BJIV5eHKnc4Ppc44hdGW4ZXzzJI9nKE2PUD2yMEBOVVBvMUSgZY5lKEKlbD2y NVTHW5ZkOjV4Nke2OlM>
K562 M4LFbmNmdGxiVnnhZoltcXS7IFHzd4F6 M4niVVEuOTBizszN MYe0PEBp MYrEUXNQ Mnz3TWM2OD1{Nj63JO69VQ>? MXOyOVU6PjV4MR?=
K562/Mcl -1-IRESBim NWf6OnhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLoU29KSzVyPUmuN{DPxE1? NXnnfpNIOjV3M{W5NFA>
K562/Bcl- 2-IRESBim M1;PeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDWN3FKSzVyPUCuN|Uh|ryP MorPNlU2OzV7MEC=
Jurkat NHHDS|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTXOmI3UUN3ME2wMlY3KM7:TR?= MUGyOVU{PTlyMB?=
JurkatΔBak NFG1e3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi2[mtKSzVyPkWwJO69VQ>? M4TLSlI2PTN3OUCw
HL60/VCR M37ObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\5V3NKSzVyPkGwNEDPxE1? MlPwNlU2OzV7MEC=
Kasumi-1 NFrMZVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XVfGlEPTB;MD6wNUDPxE1? MX6yOVU{PTlyMB?=
Kasumi-1/ABT M2rIbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz5TWM2OD1yLkWxJO69VQ>? NE\JUXgzPTV|NUmwNC=>
THP-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWizOHVTUUN3ME2xMlI4KM7:TR?= M2PSXVI2PTN3OUCw
U937 M3LTR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTVwMkmg{txO NVHISo51OjV3M{W5NFA>
C1498 M1Pl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLGT|BKSzVyPU[uNVMh|ryP MV2yOVU{PTlyMB?=
RPMI 8226 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHkTJlKSzVyPUCuNlUh|ryP MoDNNlU2OzV7MEC=
MM.1S NEDyd3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnNeVJKSzVyPUCuOFAh|ryP MlLUNlU2OzV7MEC=
NCI-H929 M4W4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3WwemlEPTB;MUWuNlEh|ryP MUSyOVU{PTlyMB?=
U266 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3hdok6UUN3ME2wMlY5KM7:TR?= NYrMXndYOjV3M{W5NFA>
MCF-7 NGD6SodE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NF\Q[VA2KM7:TR?= MonMOFghcA>? M{Kxb2ROW09? MV\lcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v MYSyOVQxQTF{NB?=
MCF-7 MUXBdI9xfG:|aYOgRZN{[Xl? NX;OeIVnPSEQvF2= MYm0M|I1NzR6IHi= MVzEUXNQ MkTobY5kemWjc3XzJJRp\SClbHXheoVlKFCDUmC= MUeyOVQxQTF{NB?=
MCF-7 MX7GeY5kfGmxbjDBd5NigQ>? MnvFOUDPxE1? NUnOOnhFOjRiaB?= MVzEUXNQ NWfGVpZp\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi M{fLeVI2PDB7MUK0
MDA-MB 231  MXLGeY5kfGmxbjDBd5NigQ>? NU\zUo96PSEQvF2= M1PyNlI1KGh? NH\nb2ZFVVOR M{fWO4VvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? Mmf4NlU1ODlzMkS=
ZR-75-1  NH\HTWJHfW6ldHnvckBCe3OjeR?= NXjxOmpYPSEQvF2= NGHwcWozPCCq MY\EUXNQ MUHlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> MmfTNlU1ODlzMkS=
A549 M1;CUWNmdGxiVnnhZoltcXS7IFHzd4F6 NIHGNlUxNTJyIN88US=> MkfXO|IhcA>? NFX5RnFFVVOR MlTu[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? Mlv3NlU{QDh5NkK=
H1299 MmDhR4VtdCCYaXHibYxqfHliQYPzZZk> NGXzc4YxNTJyIN88US=> Mk\iO|IhcA>? MnnFSG1UVw>? NVrtdmZK\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= MXiyOVM5QDd4Mh?=
HO-8910 MnLFR4VtdCCYaXHibYxqfHliQYPzZZk> MXewMVIxKM7:TR?= NV;nW4NtPzJiaB?= NGnNPGdFVVOR MW\k[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NIHHZ2MzPTN6OEe2Ni=>
HT-29 NHntRVVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX60WWhEOC1{MDFOwG0> M3;FRVczKGh? MlXnSG1UVw>? NFzMUoll\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NXewcYVzOjV|OEi3OlI>
HCT-116 NGrJ[49E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYqwMVIxKM7:TR?= MV[3NkBp MXrEUXNQ NGPmXmVl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw MmDXNlU{QDh5NkK=
A549 MVPBdI9xfG:|aYOgRZN{[Xl? NGrqOXEzOCEQvF2= Mk[5OFghcA>? MXzEUXNQ MWXpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigZZNxcXKrbh?= MlK1NlU{QDh5NkK=
H1299 NXHPXJVMSXCxcITvd4l{KEG|c3H5 NEjNfogzOCEQvF2= Ml36OFghcA>? MUDEUXNQ MmfrbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoaXPhcpRtgSClb33ibY5m\CC5aYToJIF{eGm{aX6= M4rCcVI2Ozh6N{[y
Sc-1 MoLzR4VtdCCYaXHibYxqfHliQYPzZZk> NW\ibnBROC5yMECxMVEh|ryP NH3QdGQ6PiCq M3vIe4Rm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NV;VTHpmOjV|N{O1NFg>
OcI-LY18 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWCwMlAxODFvMTFOwG0> NHjDSYM6PiCq MVvk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MVOyOVM4OzVyOB?=
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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。

* 必須

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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