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)

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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  MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGXNfYkzPTBibl5CpC=> M3LvT|czKGh? MnvCSG1UVw>? NEX1[XFk[XW|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>? NWDm[Y1kOjZ4NUeyPFg>
KG1a NHjaSINE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{XzUlAuOTBizszN NX72cHB2OjRiaB?= MUDEUXNQ NGr4fVJKSzVyPUeuOlgh|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnrrNlY2PTJ5MUK=
Kasumi-1 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1m2ZVAuOTBizszN NHP2NZkzPCCq NFzUcW9FVVOR NGDjUIVKSzVyPUSuPFch|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYfXNWVIOjZ3NUK3NVI>
KG1a M2DpeGFxd3C2b4Ppd{BCe3OjeR?= Mn;HNE0yOCEQvF2= NIXRfYgzPCCq NFvFSnhFVVOR M4foR4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M13u[FI3PTV{N{Gy
Kasumi-1 M1G2UWFxd3C2b4Ppd{BCe3OjeR?= MlPGNE0yOCEQvF2= MV:yOEBp M1q2N2ROW09? NVPzS2hWcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVqyOlU2OjdzMh?=
MC-3  M2nYXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nUUVUwOTBxMkCg{txO NHL3e3gzPCCq MX;EUXNQ M1\mXYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVHSOodUOjZ2NEe2NVU>
HN22  Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[yMlUwPy53L{KyMlUh|ryP NEDPdWQzPCCq MmjhSG1UVw>? NWDFR4FrcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NUTFSHZLOjZ2NEe2NVU>
MC-3  NYf2VWNrSXCxcITvd4l{KEG|c3H5 NYm2XJRiPS9zMD:yNEDPxE1? M{jhelI1KGh? MYDEUXNQ NF3wR29qdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz NV;rcYlROjZ2NEe2NVU>
HN22  Mkm2RZBweHSxc3nzJGF{e2G7 NIW1SWQzNjVxNz61M|IzNjVizszN NEPGO|UzPCCq MV3EUXNQ MlO2bY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= MVqyOlQ1PzZzNR?=
MOLT-4 NUHOb|BDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNE02ODByIH7N MonmO|IhcA>? NHruXo1FVVOR MorHTWM2OD1yLkG5PEDPxE1? MnGwNlY{QTJ|M{K=
RS4;11 NU\ielJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrtSXlFOTBvNUCwNEBvVQ>? MYW3NkBp MnXkSG1UVw>? M{DCVGlEPTB;MD6wNFIh|ryP M3LMZ|I3Ozl{M{Oy
JURKAT M3vBUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K4WVExNTVyMECgcm0> MVe3NkBp M{DybWROW09? NEnXXXhKSzVyPU[2JO69VQ>? NIm2T28zPjN7MkOzNi=>
CEM R NVHhc4NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v0S|ExNTVyMECgcm0> M3\RO|czKGh? NEPqb5lFVVOR NILDTlVKSzVyPUWuOEDPxE1? NF7PSlEzPjN7MkOzNi=>
CEM S M{jtNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HKNlExNTVyMECgcm0> NYnWOnVrPzJiaB?= MUDEUXNQ M4nreWlEPTB;MUKuNUDPxE1? M2XiUVI3Ozl{M{Oy
MOLT-4 NIrhVVBCeG:ydH;zbZMhSXO|YYm= Mkj2NVAuOTByMDDuUS=> NXrpSYI5OjRiaB?= MmTySG1UVw>? M3zCVYNifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x NHzHbJczPjN7MkOzNi=>
CEM S NWO4UmVrSXCxcITvd4l{KEG|c3H5 NHPySFUyOC1zMECwJI5O M1[1Z|I1KGh? NVL1eJMyTE2VTx?= NV7JTHZF[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> M3H6U|I3Ozl{M{Oy
JURKAT Mn7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LySlExOC1zMECwJI5O MkK4OFghcA>? NXHWXphZTE2VTx?= NYPjPWM1UUN3ME25OVXDuTlwMzDuUS=> NV\MSXVYOjZzN{KyOlk>
LOUCY Mlf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULWZVQ3OTByLUGwNFAhdk1? MWe0PEBp M3\TZmROW09? NGDRbHNKSzVyPUOyMljDuTFyLkmgcm0> MWWyOlE4OjJ4OR?=
WM-115 NEH6XWRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHPoWHQyODEEoH7N MmjFO|IhcA>? MYTlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? MX2yOlEyPjd5Nh?=
B16 MkXuR4VtdCCYaXHibYxqfHliQYPzZZk> M1q1cFExOMLibl2= MXu3NkBp NYPYW2o2\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= M{mwVVI3OTF4N{e2
HL-60  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;2RYdFPzJiaB?= MYnJR|UxyqB;IEGwMlchdk1? NHTDcpkzPjB2NU[wPS=>
MOLM-13  NW\nOmJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjMSIdjPzJiaB?= MYHJR|UxyqB;IEK3Mlkhdk1? M2XkXlI3ODR3NkC5
OCI-AML3 M3PqdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33OPFczKGh? NEm0XmpKSzVywrC9JFE6PTBibl2= NFy2NnQzPjB2NU[wPS=>
BCWM.1 NFTNbGFCeG:ydH;zbZMhSXO|YYm= MoDoNE0yNjZizszN MmTCNlQhcA>? MWPpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MmHRNlU5QTN{OUC=
MWCL-1 MmXYRZBweHSxc3nzJGF{e2G7 MUCwMVEvPiEQvF2= M1XuOlI1KGh? MnTMbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M{XMS|I2QDl|Mkmw
MM.1s NXf5T2JGSXCxcITvd4l{KEG|c3H5 MVywMVEvPiEQvF2= MYeyOEBp NI\1OHZqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M1XvVVI2QDl|Mkmw
HCT116 MnPoSpVv[3Srb36gRZN{[Xl? MlH4N{8yOCEQvF2= M2jUNlEzyqCqwrC= MVXEUXNQ M4LNTolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= MUWyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO M{e2dmZ2dmO2aX;uJGF{e2G7 NV\1[2JxOy9zMDFOwG0> MVyxNuKhcMLi Mlr2SG1UVw>? M1vCTolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= NXjYcW9vOjV5MUWwNlg>
HCT116 NGXvUYZHfW6ldHnvckBCe3OjeR?= M3O2RlExKM7:TR?= MYmxNuKhcMLi NYHCWXZPTE2VTx?= NInWVYZqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th MnLWNlU4OTVyMki=
HCT116 BAX BAK1 DKO NYnDT2xxTnWwY4Tpc44hSXO|YYm= NVrKcGh{OTBizszN MWGxNuKhcMLi Mn25SG1UVw>? M1vRNIlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= MVqyOVcyPTB{OB?=
HCT116 MWnBeZRweGijZ4mgRZN{[Xl? NIHobVQyOCEQvF2= NFvDNm8yOsLiaNMg M2DxNGROW09? M1fEc4lv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm M4jC[lI2PzF3MEK4
HCT116 BAX BAK1 DKO MnfURZV1d3CqYXf5JGF{e2G7 MX6xNEDPxE1? NGXQdHQyOsLiaNMg M2XmfWROW09? MoS1bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> NEjXTpAzPTdzNUCyPC=>
U937 NIPqRmNCeG:ydH;zbZMhSXO|YYm= NWPSe3c6OC5zMkWtNkDPxE1? MnLFNlQhcA>? MWTlcohidmOnczDETGEwYC1zMT3pcoR2[2WmIHHwc5B1d3Orcx?= MXGyOVcyPDB{NB?=
U937  NULkTXRUSXCxcITvd4l{KEG|c3H5 M4m5XlAvPSEQvF2= NH;ERYYzPCCq MWHlcohidmOnczDjcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlMVMh[XNid3XscEBieyCQb4jhJIxmfmWu NYHPdIx1OjV5MUSwNlQ>
HL-60 AAA-Bcl-2 Mm\pRZBweHSxc3nzJGF{e2G7 M2SzWlAuPSEQvF2= NGrEbVI1QCCq MkLYTWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mnu3NlU4OTF2NkC=
HL-60 EEE-Bcl-2 NIf2NXVCeG:ydH;zbZMhSXO|YYm= NV\Zd4dSOC13IN88US=> MVm0PEBp NVL6N5FQUUN3ME21JO69de,:jDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NF65NnAzPTdzMUS2NC=>
U87 NUXHcXNITnWwY4Tpc44hSXO|YYm= NFjicXo2OCEQvF2= NVvHV4VEOjRiaB?= MnrQdoVlfWOnczD0bIUhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?= NYrCNVNbOjV4Nke2OlM>
K562 NWnrOlFMS2WubDDWbYFjcWyrdImgRZN{[Xl? MYGxMVExKM7:TR?= MWq0PEBp M170R2ROW09? NX3odIx3UUN3ME2yOk44KM7:TR?= MlXvNlU2QTZ3NkG=
K562/Mcl -1-IRESBim M{PMPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPMUVBLUUN3ME25MlMh|ryP NF;OS4EzPTV|NUmwNC=>
K562/Bcl- 2-IRESBim NIq3ZmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHsOnJKSzVyPUCuN|Uh|ryP MXWyOVU{PTlyMB?=
Jurkat Ml3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX3TWM2OD1yLk[2JO69VQ>? MmLJNlU2OzV7MEC=
JurkatΔBak MnL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[3dXBKSzVyPkWwJO69VQ>? M3z6VFI2PTN3OUCw
HL60/VCR MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRjFyMDFOwG0> NEjjW3ozPTV|NUmwNC=>
Kasumi-1 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1THSmlEPTB;MD6wNUDPxE1? M{HLUVI2PTN3OUCw
Kasumi-1/ABT MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\q[WlEPTB;MD61NUDPxE1? M4LFXlI2PTN3OUCw
THP-1 NGT4blFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrsPXVrUUN3ME2xMlI4KM7:TR?= M3TqflI2PTN3OUCw
U937 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofETWM2OD13LkK5JO69VQ>? NEC3[|YzPTV|NUmwNC=>
C1498 NYPVUZlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L5bWlEPTB;Nj6xN{DPxE1? MmjGNlU2OzV7MEC=
RPMI 8226 M3vWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\GWHRKSzVyPUCuNlUh|ryP MnvVNlU2OzV7MEC=
MM.1S NV3uN3lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTsTWM2OD1yLkSwJO69VQ>? NULLUHFtOjV3M{W5NFA>
NCI-H929 NFfGR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTF3LkKxJO69VQ>? NET1TYMzPTV|NUmwNC=>
U266 M1\nU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwNkig{txO MnfsNlU2OzV7MEC=
MCF-7 M2jGSWNmdGxiVnnhZoltcXS7IFHzd4F6 MUe1JO69VQ>? Ml\zOFghcA>? M{T1NmROW09? NX;kfFhS\W6qYX7j[ZMhfGinIIPlcpNqfGm4aYT5JJRwKG:{IILh[IlifGmxbh?= NFPuVJIzPTRyOUGyOC=>
MCF-7 MmX5RZBweHSxc3nzJGF{e2G7 M{nqNVUh|ryP M2LVXVQwOjRxNEigbC=> NVrsUXJiTE2VTx?= M4LBdolv[3KnYYPld{B1cGViY3zlZZZm\CCSQWLQ MWeyOVQxQTF{NB?=
MCF-7 M2n3[mZ2dmO2aX;uJGF{e2G7 MlPyOUDPxE1? NUHPb2RGOjRiaB?= NGjkV4pFVVOR M{XkSIVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NVHwT2FFOjV2MEmxNlQ>
MDA-MB 231  NHzFfIlHfW6ldHnvckBCe3OjeR?= MnuxOUDPxE1? NU\xWVM2OjRiaB?= NHLOOGJFVVOR MmTC[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh M1rZelI2PDB7MUK0
ZR-75-1  NFrhcnJHfW6ldHnvckBCe3OjeR?= MnPJOUDPxE1? NUPkWHNQOjRiaB?= M{XPZ2ROW09? M3LZV4VvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? MmDYNlU1ODlzMkS=
A549 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWewMVIxKM7:TR?= M2rmflczKGh? MWXEUXNQ NYnoSmxE\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NYSwSmp5OjV|OEi3OlI>
H1299 M1j4XmNmdGxiVnnhZoltcXS7IFHzd4F6 MXKwMVIxKM7:TR?= MnTXO|IhcA>? MYjEUXNQ M{DqVIRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M1vncFI2Ozh6N{[y
HO-8910 MVPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWGyUFdxOC1{MDFOwG0> M3XiZ|czKGh? NUjxbXd7TE2VTx?= M136S4Rm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? NYfmVFR4OjV|OEi3OlI>
HT-29 M1TXTmNmdGxiVnnhZoltcXS7IFHzd4F6 NILDZoIxNTJyIN88US=> M2TVfFczKGh? M3u1dWROW09? M{fhdoRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M3u0NVI2Ozh6N{[y
HCT-116 NYW4PItqS2WubDDWbYFjcWyrdImgRZN{[Xl? NXn3fZRJOC1{MDFOwG0> MmfnO|IhcA>? NY[2VYRSTE2VTx?= MkDy[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? MXeyOVM5QDd4Mh?=
A549 MkHmRZBweHSxc3nzJGF{e2G7 MkL1NlAh|ryP MUe0PEBp M4jXR2ROW09? NFfwcWxqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIgh[XOyaYLpci=> MUmyOVM5QDd4Mh?=
H1299 MnPyRZBweHSxc3nzJGF{e2G7 MWiyNEDPxE1? MofnOFghcA>? MYPEUXNQ NFzpVJpqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIgh[XOyaYLpci=> NGiweYUzPTN6OEe2Ni=>
Sc-1 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnTxNE4xODBzLUGg{txO M3TLTVk3KGh? MmjZ[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkPsNlU{PzN3MEi=
OcI-LY18 M1q5W2NmdGxiVnnhZoltcXS7IFHzd4F6 NEHHbZAxNjByMEGtNUDPxE1? MnjmPVYhcA>? MUjk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MUKyOVM4OzVyOB?=
RL  MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MorTNE4xODBzLUGg{txO MUO5OkBp MWfk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M173OFI2Ozd|NUC4
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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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