ABT-737 化学構造
分子量: 813.43

高品質保証

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カスタマーフィードバック(14)

Quality Control & 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  MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWWyOVAhdk4EoB?= NUD5O2VyPzJiaB?= NFnGOpNFVVOR NHSyWoxk[XW|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>? MVKyOlY2PzJ6OB?=
KG1a NHvDW4FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHf1[oExNTFyIN88US=> M3\kXFI1KGh? NXnQc2lSTE2VTx?= NUf4[mg2UUN3ME23MlY5KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MlL5NlY2PTJ5MUK=
Kasumi-1 NVv0cFl5S2WubDDWbYFjcWyrdImgRZN{[Xl? NW\adpc4OC1zMDFOwG0> MojzNlQhcA>? NGnlcm9FVVOR MnTmTWM2OD12Lki3JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXyyOlU2OjdzMh?=
KG1a M{DHR2Fxd3C2b4Ppd{BCe3OjeR?= NXr2fXF1OC1zMDFOwG0> M4e4ZVI1KGh? NH7U[nVFVVOR MWTpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkHQNlY2PTJ5MUK=
Kasumi-1 NGezVIZCeG:ydH;zbZMhSXO|YYm= Mn\JNE0yOCEQvF2= NVHmVW9mOjRiaB?= MV7EUXNQ NYLhdGp7cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M{n1clI3PTV{N{Gy
MC-3  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfsRWxUPS9zMD:yNEDPxE1? MYSyOEBp M{XZW2ROW09? MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MU[yOlQ1PzZzNR?=
HN22  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjVTXgzNjVxNz61M|IzNjVizszN MUOyOEBp M2HifWROW09? NGTZOY5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mk[4NlY1PDd4MUW=
MC-3  MnPhRZBweHSxc3nzJGF{e2G7 NWDZNnNwPS9zMD:yNEDPxE1? MXyyOEBp NFXuTXhFVVOR MVfpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| MnfXNlY1PDd4MUW=
HN22  MoHsRZBweHSxc3nzJGF{e2G7 M4jGfVIvPS95LkWvNlIvPSEQvF2= M1q0fVI1KGh? MkT0SG1UVw>? NGDEdmhqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz M2O2N|I3PDR5NkG1
MOLT-4 NXiwW5pKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Dy[FExNTVyMECgcm0> NV7kU2FGPzJiaB?= NYrQW2FNTE2VTx?= MonWTWM2OD1yLkG5PEDPxE1? M3XkN|I3Ozl{M{Oy
RS4;11 NWLWSnU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDzUIVwOTBvNUCwNEBvVQ>? MVO3NkBp NVzQPG43TE2VTx?= Ml7UTWM2OD1yLkCwNkDPxE1? NGnvTnkzPjN7MkOzNi=>
JURKAT MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxNE02ODByIH7N NGTwSGQ4OiCq NYDjVmVjTE2VTx?= NILjZ5lKSzVyPU[2JO69VQ>? M3z2[VI3Ozl{M{Oy
CEM R NYDGVoJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWixNE02ODByIH7N MYC3NkBp MUTEUXNQ Mln6TWM2OD13LkSg{txO M1:5c|I3Ozl{M{Oy
CEM S NYfodGRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn4R2hROTBvNUCwNEBvVQ>? M3zQTlczKGh? MWrEUXNQ NVi3c2JrUUN3ME2xNk4yKM7:TR?= NGrrUnEzPjN7MkOzNi=>
MOLT-4 NFO0SmdCeG:ydH;zbZMhSXO|YYm= M1TKRlExNTFyMECgcm0> M2jpZ|I1KGh? M1n4[WROW09? M{P1U4NifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x NXHkRpp3OjZ|OUKzN|I>
CEM S NWf6W21NSXCxcITvd4l{KEG|c3H5 MY[xNE0yODByIH7N NXXwVoVbOjRiaB?= M33qV2ROW09? NVvrbW5t[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> M4fMblI3Ozl{M{Oy
JURKAT M3PIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XTeVExOC1zMECwJI5O NFPycGY1QCCq NWH1cJBETE2VTx?= MUTJR|UxRTl3NdMxPU4{KG6P Mk\ZNlYyPzJ{Nkm=
LOUCY NYLI[mlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnq4NVAxNTFyMECgcm0> NI[2PHU1QCCq M1vkPWROW09? NVT3OZc4UUN3ME2zNk45yrFzMD65JI5O M1T4c|I3OTd{Mk[5
WM-115 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVfhbo9jOTBywrDuUS=> M2nsSFczKGh? NVLPWnk{\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= NEXoXWszPjFzNke3Oi=>
B16 M3LDVGNmdGxiVnnhZoltcXS7IFHzd4F6 MVexNFDDqG6P NUfxelg6PzJiaB?= NHyxe5dmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= NETwXGQzPjFzNke3Oi=>
HL-60  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYS3NkBp NVzWS2NKUUN3MNMgQUAyOC55IH7N Mlj2NlYxPDV4MEm=
MOLM-13  MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUe3NkBp M3HqSGlEPTEEoE2gNlcvQSCwTR?= NX:3U4ZsOjZyNEW2NFk>
OCI-AML3 M2DzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC3NkBp M1XSemlEPTEEoE2gNVk2OCCwTR?= MVOyOlA1PTZyOR?=
BCWM.1 NHzRWXdCeG:ydH;zbZMhSXO|YYm= NXPQboxZOC1zLk[g{txO NHPneogzPCCq NITVWW1qdmS3Y3XzJINmdGxiYYDvdJRwe2m| MonDNlU5QTN{OUC=
MWCL-1 MXzBdI9xfG:|aYOgRZN{[Xl? NEK4UpIxNTFwNjFOwG0> M1PmVlI1KGh? M4nSZYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NVHJRYtwOjV6OUOyPVA>
MM.1s NWq0TmtRSXCxcITvd4l{KEG|c3H5 NYrjUIJiOC1zLk[g{txO M{S4[FI1KGh? MVnpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NIjaV5czPTh7M{K5NC=>
HCT116 NUC2U295TnWwY4Tpc44hSXO|YYm= M17Bc|MwOTBizszN NInZSowyOsLiaNMg MYDEUXNQ Ml\tbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w MlO0NlU4OTVyMki=
HCT116 BAX BAK1 DKO MVvGeY5kfGmxbjDBd5NigQ>? MUCzM|ExKM7:TR?= M2rvbFEzyqCqwrC= MmTvSG1UVw>? M{LyV4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= MlHhNlU4OTVyMki=
HCT116 NEPwTZFHfW6ldHnvckBCe3OjeR?= M4K4N|ExKM7:TR?= NUH5TVlpOTMEoHlCpC=> MYrEUXNQ M2P3Wolv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= MnrvNlU4OTVyMki=
HCT116 BAX BAK1 DKO NXjY[VNQTnWwY4Tpc44hSXO|YYm= M{e2d|ExKM7:TR?= M3PMZ|EzyqCqwrC= NGm4O4pFVVOR NFr1elVqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th MlX5NlU4OTVyMki=
HCT116 NH;K[2dCfXSxcHjh[5khSXO|YYm= MXuxNEDPxE1? M{DZVlEzyqCqwrC= NV7oNGhETE2VTx?= NVLHVVBJcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? NGjSOlUzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO MV3BeZRweGijZ4mgRZN{[Xl? NGXvfFMyOCEQvF2= NX;1bIVIOTMEoHlCpC=> NIPpR29FVVOR NVrFOpFvcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? MoPvNlU4OTVyMki=
U937 M4DIW2Fxd3C2b4Ppd{BCe3OjeR?= M4jwZ|AvOTJ3LUKg{txO NFjmbVAzPCCq M3\1SIVvcGGwY3XzJGRJSS:[LUGxMYlv\HWlZXSgZZBweHSxc3nz MoXVNlU4OTRyMkS=
U937  MnizRZBweHSxc3nzJGF{e2G7 NEnycYoxNjVizszN M4\n[lI1KGh? NW\UbY5J\W6qYX7j[ZMh[2ynYY\h[4Uhd2ZiUFHSVEBidmRiY3HzdIF{\S1|IHHzJJdmdGxiYYOgUo95[SCuZY\lcC=> MVyyOVcyPDB{NB?=
HL-60 AAA-Bcl-2 NEj6XpFCeG:ydH;zbZMhSXO|YYm= MV:wMVUh|ryP MlX1OFghcA>? MWHJR|UxRTBwOEeg{txu97zOaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MljMNlU4OTF2NkC=
HL-60 EEE-Bcl-2 MoD3RZBweHSxc3nzJGF{e2G7 MmrjNE02KM7:TR?= NGn2Rok1QCCq Mm\rTWM2OD13IN88cg+9lCCrbnT1Z4V{KGOnbHygZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1nCZ|I2PzFzNE[w
U87 NFTvZ4tHfW6ldHnvckBCe3OjeR?= M4GwPFUxKM7:TR?= M3HhRlI1KGh? NFPpb29z\WS3Y3XzJJRp\SCvUl7BJIV5eHKnc4Ppc44hdGW4ZXzzJI9nKE2PUD2yMEBOVVBvMUSgZY5lKEKlbD2y M{fZSVI2PjZ5Nk[z
K562 NFvkRoVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NU\uTXp[OS1zMDFOwG0> M3PFbVQ5KGh? NFPob49FVVOR M1jUZWlEPTB;Mk[uO{DPxE1? M4W1TVI2PTl4NU[x
K562/Mcl -1-IRESBim MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTlwMzFOwG0> NVTRVZFKOjV3M{W5NFA>
K562/Bcl- 2-IRESBim MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljDTWM2OD1yLkO1JO69VQ>? M2TQVFI2PTN3OUCw
Jurkat NXLvcZFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;NTWM2OD1yLk[2JO69VQ>? NVntTlJUOjV3M{W5NFA>
JurkatΔBak MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfiTWM2OD53MDFOwG0> MVSyOVU{PTlyMB?=
HL60/VCR NGmxb2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojyTWM2OD5zMECg{txO MUCyOVU{PTlyMB?=
Kasumi-1 NEPYd5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfBfXBoUUN3ME2wMlAyKM7:TR?= M3LVd|I2PTN3OUCw
Kasumi-1/ABT NGq1cIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljETWM2OD1yLkWxJO69VQ>? M{SweFI2PTN3OUCw
THP-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PRd2lEPTB;MT6yO{DPxE1? NUXyPZlTOjV3M{W5NFA>
U937 NIrydlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzFV5kyUUN3ME21MlI6KM7:TR?= NVfrT2gyOjV3M{W5NFA>
C1498 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXtdFlKSzVyPU[uNVMh|ryP MUKyOVU{PTlyMB?=
RPMI 8226 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH3Z3RKSzVyPUCuNlUh|ryP MofYNlU2OzV7MEC=
MM.1S NFXNVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDpTWM2OD1yLkSwJO69VQ>? M4nUfFI2PTN3OUCw
NCI-H929 NH;vXndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\0VmlEPTB;MUWuNlEh|ryP MU[yOVU{PTlyMB?=
U266 NEX0cpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3q1O2lEPTB;MD62PEDPxE1? MYSyOVU{PTlyMB?=
MCF-7 NH;CeHdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVS1JO69VQ>? M1HjOVQ5KGh? MnHiSG1UVw>? MU\lcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v NU\ofZA3OjV2MEmxNlQ>
MCF-7 NES4cIVCeG:ydH;zbZMhSXO|YYm= MoW2OUDPxE1? MYq0M|I1NzR6IHi= MYXEUXNQ M{fB[Ylv[3KnYYPld{B1cGViY3zlZZZm\CCSQWLQ MmDvNlU1ODlzMkS=
MCF-7 NV7zXllvTnWwY4Tpc44hSXO|YYm= NHjGXG42KM7:TR?= NUfMXXRoOjRiaB?= NGnZemhFVVOR NWHJXVg{\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi NVvIOnBlOjV2MEmxNlQ>
MDA-MB 231  NILXZo9HfW6ldHnvckBCe3OjeR?= NH;zemM2KM7:TR?= NFq3e5QzPCCq NGP3SHlFVVOR MnXL[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh M2jiUlI2PDB7MUK0
ZR-75-1  NEL0OIZHfW6ldHnvckBCe3OjeR?= MXe1JO69VQ>? NVnnV4pPOjRiaB?= NITN[nVFVVOR NVLnW5Bw\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi MV2yOVQxQTF{NB?=
A549 NIrG[VBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NILrUVExNTJyIN88US=> MlG3O|IhcA>? MorySG1UVw>? MWTk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NIPLNWEzPTN6OEe2Ni=>
H1299 MoH0R4VtdCCYaXHibYxqfHliQYPzZZk> MVGwMVIxKM7:TR?= M2HaZVczKGh? MmjZSG1UVw>? NWnoV3BS\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NIS1dWUzPTN6OEe2Ni=>
HO-8910 NX65RXRJS2WubDDWbYFjcWyrdImgRZN{[Xl? M{jvcFAuOjBizszN MUW3NkBp NX63SIZtTE2VTx?= NYfDO|dK\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= M1;uXVI2Ozh6N{[y
HT-29 NFHqVnlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2DMOFAuOjBizszN NYD2Z45lPzJiaB?= NWfC[JdGTE2VTx?= NWC0bWZV\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= M4XqUVI2Ozh6N{[y
HCT-116 NECwcZlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGLGXJExNTJyIN88US=> NW\NXox2PzJiaB?= M2frcmROW09? MVfk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NGn2[mYzPTN6OEe2Ni=>
A549 NF\1RpBCeG:ydH;zbZMhSXO|YYm= NXXvO4l2OjBizszN NIH3c|c1QCCq Mn:1SG1UVw>? NWnpZYNKcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> MWOyOVM5QDd4Mh?=
H1299 NHO4ZVlCeG:ydH;zbZMhSXO|YYm= M3nRdFIxKM7:TR?= Mk\aOFghcA>? NFvPdWhFVVOR M2DjWYlv\HWlZYOgZZBweHSxc3nzJJNq\26rZnnjZY51dHliY3;tZolv\WRid3n0bEBie3Crcnnu M3nFNlI2Ozh6N{[y
Sc-1 MoDkR4VtdCCYaXHibYxqfHliQYPzZZk> MoTVNE4xODBzLUGg{txO MWC5OkBp M{PoNoRm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWDrTGtFOjV|N{O1NFg>
OcI-LY18 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYWwMlAxODFvMTFOwG0> NV35S4xRQTZiaB?= M1LhcYRm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmfYNlU{PzN3MEi=
RL  NHLuZm9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{\JeFAvODByMT2xJO69VQ>? M{DmdFk3KGh? MXnk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3O4flI2Ozd|NUC4
RKO M1HFcWNmdGxiVnnhZoltcXS7IFHzd4F6 NH\FTJkxNTFyIN88US=> MnT2NlTjiImqwrC= MUnEUXNQ NXrOWIZuUUN3ME9ihKkzPeLCidM1US=> MWWyOVMxPDN6Mx?=
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HaCaT MnzQSpVv[3Srb36gRZN{[Xl? NGS5e|IyOOLCid88US=> NFTvOmQzPC92ODDo M1\qeWROW09? NUXlXWs5cW6mdXPld{BOVVBiYX7kJGRPSSCocnHncYVvfGG2aX;u NVe2T|lsOjV{MUC3PVU>
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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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (122.93 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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]-

カスタマーフィードバック (14)


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Rating
Source Nat Med, 2013, 19(11), 1478-88. ABT-737 purchased from Selleck
Method Western blot
Cell Lines MCF-7 cells
Concentrations 0/0.1/1/10 uM
Incubation Time 12 h
Results Mst1 inhibition of autophagy was dose-dependently reversed by treatment with ABT-737.

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Rating
Source J Clin Invest, 2011, 121, 1053-1063. ABT-737 purchased from Selleck
Method Apoptosis assays
Cell Lines PMNs
Concentrations 1-10 μM
Incubation Time 20 h
Results ABT-737 completely abrogated the enhanced survival of neutrophils under hypoxia at a concentration that also reversed the survival effect of GM-CSF, a pro-survival stimulus known to induce BCL-XL but was without effect upon constitutive apoptosis.

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Rating
Source Blood, 2011, 17(26), 7145-54. ABT-737 purchased from Selleck
Method Immunohistochemistry
Cell Lines Platelets
Concentrations 100nM
Incubation Time 2 h
Results There has been considerable discussion on the involvement of apoptotic signaling events in platelet activation. Therefore, we investigated apoptosis pathways after exposure to platelet agonists or BCL2 inhibition. Exposure to ABT-737 induced release of TMRE, and caspase cleavage, in agreement with activation of the intrinsic apoptotic pathway.

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Rating
Source Blood, 2011, 17(26), 7145-54. ABT-737 purchased from Selleck
Method Immunohistochemistry
Cell Lines Platelets
Concentrations 100nM
Incubation Time 2 h
Results Further characterization of the ABT-737-induced cytoskeletal changes was performed on glass coverslips, which induced a spontaneous activation and spreading of the control platelets but not of ABT-737-treated platelets. Activated control platelets displayed a tubulin ring close to the cell center with actin fibers surrounding it. After exposure to ABT-737, a marked condensation of actin structures and inhibition of tubulin ring formation were observed in those cells that were apoptotic.

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Source Cell death dis, 2013, 4, e801. ABT-737 purchased from Selleck
Method Flow cytometry
Cell Lines SW480, SW620
Concentrations 1 uM
Incubation Time 24 h, 48 h , 72 h
Results a)adherent SW480 cells were totally resistant to ABT-737 (1 uM). However, in suspended cells, the presence of ABT-737 was found to greatly increase the level of anoikis. (b)The same type of experiments were performed in SW620 cells. Again, adherent cells were resistant to ABT-737.Surprisingly, SW620 cells cultured in suspension, despite their resistance to anoikis, died in significant numbers in the presence of ABT-737.

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Rating
Source J Biol Chem, 2010, 285, 19919-19920. ABT-737 purchased from Selleck
Method Cell Viability
Cell Lines INS-1E cells
Concentrations 10 μM
Incubation Time 24 h
Results Knockdown of PUMA partially prevented the proapoptotic action of ABT-737.

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Rating
Source Apoptosis, 2010, 15, 1256-1269. ABT-737 purchased from Selleck
Method MTT assay
Cell Lines CCRF-CEM cells
Concentrations 10 μM
Incubation Time 24 h
Results Co-treatment of AY4 or TRAIL with a subtoxic dosage of ABT-737 (10 μM) showed reasonably increased cell death-inducing efficiency in CCRF-CEM cells by the additive effects of the two agents, compared with those of the single agent alone.The combinations of SAHA (1 μM) or VPA (1 mM) with ABT-737 (10 μM) also showed only additively enhanced cytotoxicity by the two agents. However, the presence of ABT-737 did not further potentiate the synergistic cytotoxicity induced by the combined treatment of AY4 or TRAIL with either SAHA or VPA.

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Rating
Source Cancer Chemoth Pharm, 2011, 67, 557-567. ABT-737 purchased from Selleck
Method Crystal violet assay
Cell Lines TFK-1 cell/EGI-1 cell
Concentrations 1-40 μM
Incubation Time 72 h
Results ABT-737 potently inhibited the survival of cholangiocarcinoma cells only at high concentrations.

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Rating
Source Cancer Chemoth Pharm, 2011, 67, 557-567. ABT-737 purchased from Selleck
Method Western blot
Cell Lines TFK-1 cell, EGI-1 cell
Concentrations 1-50 μM
Incubation Time 72 h
Results Combination experiments using drug concentrations close to IC50 (15 μM ZOL and 3 μM ABT-737 in EGI-1 cells; 30 μM ZOL and 10 μM ABT-737 in TFK-1 cells) were performed. The above-mentioned molecules when used as single agent at the same concentration determined moderate modification of proliferation pattern.

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Rating
Source Exp Hematol , 2010, 38, 908-921. ABT-737 purchased from Selleck
Method Analysis of cell cycle and apoptosis
Cell Lines TF-1 cells
Concentrations 3 μM
Incubation Time 72 h
Results Bcl2 ablation using small molecule inhibitor ABT737 induced apoptosis in TF-1 cells in suspension and cocultures with MS5 stroma cells. We also show that the combination of two reagents, ABT737 and BIO, both downregulating Bcl2 in TF-1 cells, is more efficient than the effect of each single reagent used at the same dose.

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Rating
Source Biochem Biophys Res Commun, 2012, 408, 344-9. ABT-737 purchased from Selleck
Method Flow cytometry
Cell Lines MDCKII wild type cells/MDR1 cells
Concentrations 50 nM
Incubation Time 24 h
Results MDCKII cells transfected with MDR1 showed significantly less apoptosis inducedby ABT-737 (Fig. C) and ABT-263 (Fig. D) than wild type cells.

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Rating
Source Biochem Biophys Res Commun, 2013, 408, 344-9. ABT-737 purchased from Selleck
Method flow cytometry analysis/Annexin-V staining
Cell Lines Breast cancer cell lines
Concentrations 1 μM
Incubation Time 48 h
Results combined treatment of breast cancer cell lines with a suboptimal concentration (that is, 8 μM GSIXII and 1 μM ABT-737) strongly synergized to induce cell death (Figure A). The GSIXII and ABT-737 combination led to inhibition of mammosphere formation in both MCF7 and BT549 cell lines (Figure B ). The SAHM1 a nd ABT-737 combinational so decreased mammosphere formation (Figure C).

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Rating
Source Dr. Arnim Weber of Medizinische Mikrobiologie und Hygiene Universitatsklinikum Freiburg. ABT-737 purchased from Selleck
Method
Cell Lines
Concentrations 1 μM
Incubation Time 24 h
Results

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Rating
Source , Dr. Zhang of Tianjin Medical University. ABT-737 purchased from Selleck
Method Hoechst staining
Cell Lines MDB-MA-231 cells
Concentrations 100 nM
Incubation Time
Results

文献中の引用 (86)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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