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)

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  NGfrbmJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUTodnU6OjVyIH7NxsA> MlTvO|IhcA>? MYrEUXNQ M2DKdYNifXOnZDC5O{UhdG:|czDv[kB3cWGkaXzpeJkhcW5iY3XscJMhfHKjboPm[YN1\WRid3n0bEBDS0x4IIPpVm5C M3TzNlI3PjV5Mki4
KG1a NV\NeoJCS2WubDDWbYFjcWyrdImgRZN{[Xl? M3;YdlAuOTBizszN MojONlQhcA>? MmfSSG1UVw>? MWjJR|UxRTdwNkig{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXf0eoR1OjZ3NUK3NVI>
Kasumi-1 NVPIdXFsS2WubDDWbYFjcWyrdImgRZN{[Xl? MYewMVExKM7:TR?= MUWyOEBp NIXHfGtFVVOR M1zj[mlEPTB;ND64O{DPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NITaT48zPjV3MkexNi=>
KG1a NHnCWGNCeG:ydH;zbZMhSXO|YYm= MnzBNE0yOCEQvF2= NGjyfWEzPCCq MX7EUXNQ NFWxd3NqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NYrp[IFsOjZ3NUK3NVI>
Kasumi-1 M4DGNGFxd3C2b4Ppd{BCe3OjeR?= NXLYZVRxOC1zMDFOwG0> NXLJTFF4OjRiaB?= MkjCSG1UVw>? MVrpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmnnNlY2PTJ5MUK=
MC-3  MkK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUC1M|ExNzJyIN88US=> MmTPNlQhcA>? NYfwclFUTE2VTx?= MojlbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFewd|AzPjR2N{[xOS=>
HN22  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH2d2U2Oi53L{euOU8zOi53IN88US=> MlHGNlQhcA>? MWLEUXNQ NYrPSpNZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2W4clI3PDR5NkG1
MC-3  M1:1SmFxd3C2b4Ppd{BCe3OjeR?= MX21M|ExNzJyIN88US=> MX[yOEBp M2rhOWROW09? MmjObY5lfWOnczDjZZNx[XOnLX3l[IlifGWmIHHwc5B1d3Orcx?= MXuyOlQ1PzZzNR?=
HN22  MVXBdI9xfG:|aYOgRZN{[Xl? NIXMVFMzNjVxNz61M|IzNjVizszN MmKxNlQhcA>? M2jKU2ROW09? MWHpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| M1HaN|I3PDR5NkG1
MOLT-4 NILVTIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWxNE02ODByIH7N NHPYXJc4OiCq MlS3SG1UVw>? NUnKS2N4UUN3ME2wMlE6QCEQvF2= NHTxNmUzPjN7MkOzNi=>
RS4;11 NHPUZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmxNE02ODByIH7N NUTQdI1kPzJiaB?= MX\EUXNQ NGPy[XZKSzVyPUCuNFAzKM7:TR?= M1LpZlI3Ozl{M{Oy
JURKAT MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWxNE02ODByIH7N M3KwSVczKGh? M{S0emROW09? NIL1XFBKSzVyPU[2JO69VQ>? M1XlPFI3Ozl{M{Oy
CEM R NIfPeYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zQTlExNTVyMECgcm0> MYq3NkBp M4TxRWROW09? NVnmZmQyUUN3ME21MlQh|ryP NH\CSI0zPjN7MkOzNi=>
CEM S NYrBXmRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuxNE02ODByIH7N NUjKNZhlPzJiaB?= NHPYWoJFVVOR M4\PXGlEPTB;MUKuNUDPxE1? NHLUdZczPjN7MkOzNi=>
MOLT-4 Mkn5RZBweHSxc3nzJGF{e2G7 NITNbYkyOC1zMECwJI5O NV;1S3JqOjRiaB?= MYHEUXNQ MVPjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= MmjBNlY{QTJ|M{K=
CEM S NVzDXnJNSXCxcITvd4l{KEG|c3H5 MWqxNE0yODByIH7N NGX0UpkzPCCq M3ixOGROW09? NGfyVpRk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> NVT3bVNbOjZ|OUKzN|I>
JURKAT MoDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj3NVAxNTFyMECgcm0> NIWyUFQ1QCCq NHj2dVZFVVOR M4n6PGlEPTB;OUW1xtE6NjNibl2= NHvo[4QzPjF5MkK2PS=>
LOUCY MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fNdFExOC1zMECwJI5O M2LTZ|Q5KGh? MnLPSG1UVw>? M3LVOmlEPTB;M{KuPOKyOTBwOTDuUS=> M4LMbFI3OTd{Mk[5
WM-115 MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MU[xNFDDqG6P NWHUb|czPzJiaB?= NV[1bIRz\W6qYX7j[ZMh[3W{Y4XtbY4ucW6mdXPl[EBidnSrLYP1dpZqfmGuwrC= NX3YSYM3OjZzMU[3O|Y>
B16 NFnPZ2JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGi4SHgyODEEoH7N NH\ZWHo4OiCq MYjlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NVjFS2ozOjZzMU[3O|Y>
HL-60  MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX23NkBp NHHldVBKSzVywrC9JFExNjdibl2= M3HKT|I3ODR3NkC5
MOLM-13  MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\pXG44OiCq NXz1XpFQUUN3MNMgQUAzPy57IH7N NXPWTI1DOjZyNEW2NFk>
OCI-AML3 NWnC[W9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHoVIk3PzJiaB?= M2TOXWlEPTEEoE2gNVk2OCCwTR?= M{e3OlI3ODR3NkC5
BCWM.1 NYDjbo5ZSXCxcITvd4l{KEG|c3H5 NEjQVWQxNTFwNjFOwG0> NYrJfHltOjRiaB?= NWHr[Xl6cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NXHINop5OjV6OUOyPVA>
MWCL-1 MmXNRZBweHSxc3nzJGF{e2G7 NGnkdIIxNTFwNjFOwG0> MkXCNlQhcA>? MlL4bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MW[yOVg6OzJ7MB?=
MM.1s M4\VN2Fxd3C2b4Ppd{BCe3OjeR?= NYDVZlBoOC1zLk[g{txO NYn0OHhYOjRiaB?= MXLpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NWrNS2NuOjV6OUOyPVA>
HCT116 NV[zdYhHTnWwY4Tpc44hSXO|YYm= MonBN{8yOCEQvF2= MmjRNVLDqGkEoB?= NE\6PJdFVVOR MmDWbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w M1mzcFI2PzF3MEK4
HCT116 BAX BAK1 DKO M2HZNGZ2dmO2aX;uJGF{e2G7 NGnBdVM{NzFyIN88US=> NXzWT2FPOTMEoHlCpC=> MXjEUXNQ NUjGW5UzcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u Mn;sNlU4OTVyMki=
HCT116 M1XY[mZ2dmO2aX;uJGF{e2G7 M{LzUVExKM7:TR?= NXTUUnl3OTMEoHlCpC=> MV7EUXNQ MWLpcoNz\WG|ZYOgS2ZRNUyFM1KgdJVv[3Sj M1rYWFI2PzF3MEK4
HCT116 BAX BAK1 DKO NWHYR2c5TnWwY4Tpc44hSXO|YYm= M4Ho[FExKM7:TR?= NGTsR4cyOsLiaNMg NFnrU|ZFVVOR NXrPNmE3cW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> MmHnNlU4OTVyMki=
HCT116 MVfBeZRweGijZ4mgRZN{[Xl? NE\GbGcyOCEQvF2= M17OOlEzyqCqwrC= M37YfmROW09? M2riVIlv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm NU[0O|I{OjV5MUWwNlg>
HCT116 BAX BAK1 DKO MYfBeZRweGijZ4mgRZN{[Xl? M2\0VVExKM7:TR?= MUWxNuKhcMLi NYPWPYdiTE2VTx?= NFPxSmNqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? MmTWNlU4OTVyMki=
U937 NXjJdJFFSXCxcITvd4l{KEG|c3H5 MViwMlEzPS1{IN88US=> NITuSGkzPCCq MmLi[Y5p[W6lZYOgSGhCN1hvMUGtbY5lfWOnZDDhdI9xfG:|aYO= MnXSNlU4OTRyMkS=
U937  NXv3UlROSXCxcITvd4l{KEG|c3H5 NViwUW5POC53IN88US=> NXOxdXZ{OjRiaB?= M{D0fYVvcGGwY3XzJINt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UuOyCjczD3[YxtKGG|IF7vfIEhdGW4ZXy= M2HBXVI2PzF2MEK0
HL-60 AAA-Bcl-2 MWLBdI9xfG:|aYOgRZN{[Xl? MWKwMVUh|ryP M1\1UFQ5KGh? NU\qdZBpUUN3ME2wMlg4KM7:bf-8kIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MoDTNlU4OTF2NkC=
HL-60 EEE-Bcl-2 NH7CSZFCeG:ydH;zbZMhSXO|YYm= M1POTlAuPSEQvF2= M4WyXFQ5KGh? M2fIeWlEPTB;NTFOwI3wxIxiaX7keYNmeyClZXzsJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVmyOVcyOTR4MB?=
U87 NE\ROmNHfW6ldHnvckBCe3OjeR?= MYS1NEDPxE1? MUeyOEBp NHzM[Hlz\WS3Y3XzJJRp\SCvUl7BJIV5eHKnc4Ppc44hdGW4ZXzzJI9nKE2PUD2yMEBOVVBvMUSgZY5lKEKlbD2y M2\sVlI2PjZ5Nk[z
K562 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NX23U|I{OS1zMDFOwG0> MUG0PEBp MY\EUXNQ M2\Jc2lEPTB;Mk[uO{DPxE1? MlXkNlU2QTZ3NkG=
K562/Mcl -1-IRESBim NWjaXXZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5[IRiUUN3ME25MlMh|ryP M4DRNFI2PTN3OUCw
K562/Bcl- 2-IRESBim MlLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rn[GlEPTB;MD6zOUDPxE1? NH7SSFczPTV|NUmwNC=>
Jurkat MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPFOm9KSzVyPUCuOlYh|ryP M4fse|I2PTN3OUCw
JurkatΔBak MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnCZ4k3UUN3ME61NEDPxE1? M1fIfFI2PTN3OUCw
HL60/VCR MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7nS3p2UUN3ME6xNFAh|ryP NVPlTW5mOjV3M{W5NFA>
Kasumi-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TacWlEPTB;MD6wNUDPxE1? M{LtVFI2PTN3OUCw
Kasumi-1/ABT NYHjU|JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPqTWM2OD1yLkWxJO69VQ>? NYPCV4FoOjV3M{W5NFA>
THP-1 M3e0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnOU41KSzVyPUGuNlch|ryP NUju[JVjOjV3M{W5NFA>
U937 M{\4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXJTWM2OD13LkK5JO69VQ>? MVGyOVU{PTlyMB?=
C1498 M1zFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXoTWM2OD14LkGzJO69VQ>? MnHENlU2OzV7MEC=
RPMI 8226 M1rQd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j1d2lEPTB;MD6yOUDPxE1? MWCyOVU{PTlyMB?=
MM.1S NHrDbmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX4SWVKSzVyPUCuOFAh|ryP MnvoNlU2OzV7MEC=
NCI-H929 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TacmlEPTB;MUWuNlEh|ryP MnO1NlU2OzV7MEC=
U266 MkKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwNkig{txO MWeyOVU{PTlyMB?=
MCF-7 M4DSS2NmdGxiVnnhZoltcXS7IFHzd4F6 MW[1JO69VQ>? M2rPUlQ5KGh? M4PY[2ROW09? MWXlcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v NF72ZYIzPTRyOUGyOC=>
MCF-7 NVjkXWpqSXCxcITvd4l{KEG|c3H5 MWi1JO69VQ>? MWq0M|I1NzR6IHi= NGjQWlFFVVOR NHXSbI9qdmO{ZXHz[ZMhfGinIHPs[YF3\WRiUFHSVC=> MYWyOVQxQTF{NB?=
MCF-7 MnzXSpVv[3Srb36gRZN{[Xl? Mlm4OUDPxE1? M1XmW|I1KGh? MWHEUXNQ MYPlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> NWfZXZl3OjV2MEmxNlQ>
MDA-MB 231  NGTHN3lHfW6ldHnvckBCe3OjeR?= M1TkdlUh|ryP NUnGVW9GOjRiaB?= MoTaSG1UVw>? NID1clFmdmijbnPld{B1cGWuZY\lcEBw\iCPY3ytNUBmgHC{ZYPzbY9vyqB? M1fxUVI2PDB7MUK0
ZR-75-1  NUfyfmg1TnWwY4Tpc44hSXO|YYm= M2jyNVUh|ryP NXj1e|lrOjRiaB?= Mnj1SG1UVw>? NWTsT4tP\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi M4rrcFI2PDB7MUK0
A549 NHHrUZNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3[zXFAuOjBizszN NHT3TXA4OiCq NIDpdmdFVVOR MkHt[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? NFjNdY0zPTN6OEe2Ni=>
H1299 Ml60R4VtdCCYaXHibYxqfHliQYPzZZk> MVqwMVIxKM7:TR?= MUO3NkBp NITPZodFVVOR NHzpZ4Vl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw MlHaNlU{QDh5NkK=
HO-8910 M1rLNGNmdGxiVnnhZoltcXS7IFHzd4F6 NFjaVocxNTJyIN88US=> MVy3NkBp M2rVZmROW09? MWrk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv MYOyOVM5QDd4Mh?=
HT-29 M3HRUWNmdGxiVnnhZoltcXS7IFHzd4F6 MnrINE0zOCEQvF2= NFW0SGI4OiCq MnfESG1UVw>? NUnzflBY\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NYTRb|FIOjV|OEi3OlI>
HCT-116 M1LWTWNmdGxiVnnhZoltcXS7IFHzd4F6 MXmwMVIxKM7:TR?= M3;vV|czKGh? NF7YUndFVVOR MkPY[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? NHe1PHgzPTN6OEe2Ni=>
A549 MmK5RZBweHSxc3nzJGF{e2G7 MlrjNlAh|ryP M1HGdFQ5KGh? MY\EUXNQ NIDkbmVqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIgh[XOyaYLpci=> Moq3NlU{QDh5NkK=
H1299 NHyxWmlCeG:ydH;zbZMhSXO|YYm= NFy4PFUzOCEQvF2= NW[wS3M5PDhiaB?= M4DUUGROW09? NV7YeFdkcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> NHPjOnAzPTN6OEe2Ni=>
Sc-1 NIPQTm1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWGwMlAxODFvMTFOwG0> NHLXV5Q6PiCq NWTwWmJ3\GWlcnXhd4V{KHSqZTDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIPzU4QzPTN5M{WwPC=>
OcI-LY18 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoTTNE4xODBzLUGg{txO M4T0XFk3KGh? NIXkc29l\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnTnNlU{PzN3MEi=
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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]-

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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