ABT-737

製品コードS1002

ABT-737化学構造

分子量(MW):813.43

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

サイズ 価格(税別)  
JPY 65700
JPY 21900
JPY 35200
JPY 96600
JPY 163000
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バルク問合せ

文献中Selleckの製品使用例(114)

製品安全説明書

Bcl-2阻害剤の選択性比較

生物活性

製品説明 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
特性 First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
ターゲット
Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
Bcl-B [1]
(Cell-free assay)
30.3 nM(EC50) 78.7 nM(EC50) 197.8 nM(EC50) 1.82 μM(EC50)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OCI-Ly1  NFjOdY5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MoS1NlUxKG6PwrC= NHnPV|I4OiCq MV\EUXNQ MmH5Z4F2e2WmIEm3KUBtd3O|IH;mJJZq[WKrbHn0fUBqdiClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJGJEVDZic3nSUmE> NGLLN2EzPjZ3N{K4PC=>
KG1a MnTYR4VtdCCYaXHibYxqfHliQYPzZZk> MXOwMVExKM7:TR?= MUiyOEBp MWPEUXNQ NUHuXY1mUUN3ME23MlY5KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MX6yOlU2OjdzMh?=
Kasumi-1 NXLGT2R3S2WubDDWbYFjcWyrdImgRZN{[Xl? MkK3NE0yOCEQvF2= MV6yOEBp NHT4OVVFVVOR NYDuZXhiUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXixXHkxOjZ3NUK3NVI>
KG1a NUXs[pd6SXCxcITvd4l{KEG|c3H5 NF7UbI0xNTFyIN88US=> MWKyOEBp NWPUUWxpTE2VTx?= NH\kNnlqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M1u5XFI3PTV{N{Gy
Kasumi-1 MXHBdI9xfG:|aYOgRZN{[Xl? NHPIO5IxNTFyIN88US=> M2Xm[FI1KGh? NV7ERWI1TE2VTx?= M3;RW4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIP6PJczPjV3MkexNi=>
MC-3  M13t[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1M|ExNzJyIN88US=> M3vOS|I1KGh? MUfEUXNQ MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4f0PVI3PDR5NkG1
HN22  Mn\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f5[VIvPS95LkWvNlIvPSEQvF2= M4DlTFI1KGh? NUe1doRDTE2VTx?= MlzFbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVuyOlQ1PzZzNR?=
MC-3  MlLuRZBweHSxc3nzJGF{e2G7 NHjGR2o2NzFyL{KwJO69VQ>? MlPjNlQhcA>? NIe2SINFVVOR MWLpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| MkfVNlY1PDd4MUW=
HN22  MlLURZBweHSxc3nzJGF{e2G7 NVO4bZJ{Oi53L{euOU8zOi53IN88US=> MknrNlQhcA>? NXvOW3dOTE2VTx?= NGHGb4FqdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz M17Mb|I3PDR5NkG1
MOLT-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO4PIUyOC13MECwJI5O MVW3NkBp NULLe4JUTE2VTx?= MmjzTWM2OD1yLkG5PEDPxE1? MnLSNlY{QTJ|M{K=
RS4;11 NVGxUJFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\PNm8yOC13MECwJI5O MWi3NkBp M4TnO2ROW09? NUj6b4Q2UUN3ME2wMlAxOiEQvF2= M4LWPVI3Ozl{M{Oy
JURKAT M3zNd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHDS2syOC13MECwJI5O NESyOW44OiCq MYTEUXNQ M3ixcGlEPTB;Nk[g{txO MXiyOlM6OjN|Mh?=
CEM R MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\GNVAuPTByMDDuUS=> NXy0c5U2PzJiaB?= NXfReWdTTE2VTx?= MkXwTWM2OD13LkSg{txO NVvBSXBOOjZ|OUKzN|I>
CEM S NVztUHVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jiSVExNTVyMECgcm0> NU[2emJpPzJiaB?= NUDrRZZoTE2VTx?= MUDJR|UxRTF{LkGg{txO NVi1WpRnOjZ|OUKzN|I>
MOLT-4 MmH1RZBweHSxc3nzJGF{e2G7 NEPzZVYyOC1zMECwJI5O NWjBNJJFOjRiaB?= M{jzcmROW09? NFPaNIhk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> NEDBbGozPjN7MkOzNi=>
CEM S NFLQNGRCeG:ydH;zbZMhSXO|YYm= M2nifVExNTFyMECgcm0> NWLZ[GkxOjRiaB?= MXvEUXNQ M17o[4NifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x NGG1bVMzPjN7MkOzNi=>
JURKAT NVPqdHN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULCSoZrOTByLUGwNFAhdk1? MXy0PEBp M3PPWWROW09? M2HMfWlEPTB;OUW1xtE6NjNibl2= NV34cpZKOjZzN{KyOlk>
LOUCY M1nSSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XZbVExOC1zMECwJI5O NFPMVXM1QCCq M3W3ZWROW09? MlvTTWM2OD1|Mj64xtEyOC57IH7N MnO5NlYyPzJ{Nkm=
WM-115 MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NILORVUyODEEoH7N NGj6OGk4OiCq Mojl[Y5p[W6lZYOgZ5Vz[3WvaX6tbY5lfWOnZDDhcpRqNXO3co\peoFtyqB? MYSyOlEyPjd5Nh?=
B16 NGDOSYRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGn6SngyODEEoH7N Mkf3O|IhcA>? M4jKbYVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi NFW3WmozPjFzNke3Oi=>
HL-60  NX\UbI4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\yO|IhcA>? NH\jPYtKSzVywrC9JFExNjdibl2= NH;YWXQzPjB2NU[wPS=>
MOLM-13  Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7Hemt[PzJiaB?= NUfPRnRIUUN3MNMgQUAzPy57IH7N M2K5NFI3ODR3NkC5
OCI-AML3 M325Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojWO|IhcA>? M1zEZmlEPTEEoE2gNVk2OCCwTR?= M1jlUVI3ODR3NkC5
BCWM.1 NWDWRYlPSXCxcITvd4l{KEG|c3H5 NGX3ZlYxNTFwNjFOwG0> Mne2NlQhcA>? MWnpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M3PQ[FI2QDl|Mkmw
MWCL-1 NELLV4dCeG:ydH;zbZMhSXO|YYm= NIjBXHExNTFwNjFOwG0> M3roV|I1KGh? M1nkdIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MkjUNlU5QTN{OUC=
MM.1s Mn70RZBweHSxc3nzJGF{e2G7 MnLyNE0yNjZizszN NEHXWo4zPCCq NEHwTnFqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MmDuNlU5QTN{OUC=
HCT116 MXnGeY5kfGmxbjDBd5NigQ>? NXHqPZdbOy9zMDFOwG0> MoS0NVLDqGkEoB?= MoDJSG1UVw>? M33RTolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= NHvQZpozPTdzNUCyPC=>
HCT116 BAX BAK1 DKO NVPHNWFNTnWwY4Tpc44hSXO|YYm= MoXtN{8yOCEQvF2= MWWxNuKhcMLi MUjEUXNQ MYPpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? MVuyOVcyPTB{OB?=
HCT116 MlvGSpVv[3Srb36gRZN{[Xl? NUXJPXhyOTBizszN NFTDdYYyOsLiaNMg MnvzSG1UVw>? M{m3WIlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= MkTwNlU4OTVyMki=
HCT116 BAX BAK1 DKO NX\hS5A3TnWwY4Tpc44hSXO|YYm= NEDjbIkyOCEQvF2= M2PTOVEzyqCqwrC= MVLEUXNQ NXPZTId6cW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> NWfqTG0{OjV5MUWwNlg>
HCT116 NVvFTWVGSXW2b4DoZYd6KEG|c3H5 NWHn[ZdJOTBizszN MnLxNVLDqGkEoB?= MYnEUXNQ MXHpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> NXnSbGZIOjV5MUWwNlg>
HCT116 BAX BAK1 DKO MWTBeZRweGijZ4mgRZN{[Xl? MnznNVAh|ryP MoL6NVLDqGkEoB?= MV\EUXNQ NIK5W5JqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? M1TIblI2PzF3MEK4
U937 MVvBdI9xfG:|aYOgRZN{[Xl? NF\6fXIxNjF{NT2yJO69VQ>? MYGyOEBp NX:zXWZD\W6qYX7j[ZMhTEiDL2itNVEucW6mdXPl[EBieG:ydH;zbZM> MWOyOVcyPDB{NB?=
U937  Mo\mRZBweHSxc3nzJGF{e2G7 MW[wMlUh|ryP NIHpNIMzPCCq M3HTWoVvcGGwY3XzJINt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UuOyCjczD3[YxtKGG|IF7vfIEhdGW4ZXy= MVWyOVcyPDB{NB?=
HL-60 AAA-Bcl-2 MVjBdI9xfG:|aYOgRZN{[Xl? NXXueJRZOC13IN88US=> NH:0Zos1QCCq M2XCc2lEPTB;MD64O{DPxG4xvJzpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NETZNnkzPTdzMUS2NC=>
HL-60 EEE-Bcl-2 M3TBdmFxd3C2b4Ppd{BCe3OjeR?= MVOwMVUh|ryP NF7TTWk1QCCq NEfJSI5KSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYSwdYlNOjV5MUG0OlA>
U87 MWHGeY5kfGmxbjDBd5NigQ>? M{jqd|UxKM7:TR?= M2\M[lI1KGh? MUDy[YR2[2W|IITo[UBuWk6DIHX4dJJme3Orb36gcIV3\Wy|IH;mJG1OWC1{LDDNUXAuOTRiYX7kJGJkdC1{ MVOyOVY3PzZ4Mx?=
K562 NEf4VplE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX7UTY1GOS1zMDFOwG0> NH7DcHk1QCCq MVjEUXNQ NFnvN2xKSzVyPUK2Mlch|ryP MUOyOVU6PjV4MR?=
K562/Mcl -1-IRESBim Ml;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y0VWlEPTB;OT6zJO69VQ>? M1\IflI2PTN3OUCw
K562/Bcl- 2-IRESBim M2XDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHS3blBKSzVyPUCuN|Uh|ryP M4TGZ|I2PTN3OUCw
Jurkat MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGmybWtKSzVyPUCuOlYh|ryP MkTuNlU2OzV7MEC=
JurkatΔBak M2ryO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRjVyIN88US=> M4TwV|I2PTN3OUCw
HL60/VCR NYrwboRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrOOJlzUUN3ME6xNFAh|ryP M2LGOlI2PTN3OUCw
Kasumi-1 M13RW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzMTWM2OD1yLkCxJO69VQ>? MUWyOVU{PTlyMB?=
Kasumi-1/ABT NWXMTGNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjR[4xvUUN3ME2wMlUyKM7:TR?= MWOyOVU{PTlyMB?=
THP-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFwMkeg{txO M2fIW|I2PTN3OUCw
U937 NIX2[25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X4bWlEPTB;NT6yPUDPxE1? NInDR5AzPTV|NUmwNC=>
C1498 NWrxVlI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq4TWM2OD14LkGzJO69VQ>? MWGyOVU{PTlyMB?=
RPMI 8226 NXraRYM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT6XWRtUUN3ME2wMlI2KM7:TR?= MoLxNlU2OzV7MEC=
MM.1S MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPSTWM2OD1yLkSwJO69VQ>? Mlz5NlU2OzV7MEC=
NCI-H929 MonrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLLRWVKSzVyPUG1MlIyKM7:TR?= Mn:yNlU2OzV7MEC=
U266 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwNkig{txO MYCyOVU{PTlyMB?=
MCF-7 MkXYR4VtdCCYaXHibYxqfHliQYPzZZk> M1fNcFUh|ryP MUO0PEBp MULEUXNQ MWflcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v MVuyOVQxQTF{NB?=
MCF-7 NXXNNIJQSXCxcITvd4l{KEG|c3H5 M{nCflUh|ryP NEe0XI81NzJ2L{S4JIg> M3zuUmROW09? M{\zRolv[3KnYYPld{B1cGViY3zlZZZm\CCSQWLQ MV2yOVQxQTF{NB?=
MCF-7 MX3GeY5kfGmxbjDBd5NigQ>? NXPSO2xzPSEQvF2= MYCyOEBp NX71bYcxTE2VTx?= M4fzW4VvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NFjCbGozPTRyOUGyOC=>
MDA-MB 231  MmnlSpVv[3Srb36gRZN{[Xl? MXG1JO69VQ>? M17CT|I1KGh? NFm3d|JFVVOR MmTL[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh MmnkNlU1ODlzMkS=
ZR-75-1  M2nE[2Z2dmO2aX;uJGF{e2G7 NWDJRVVrPSEQvF2= NILncHMzPCCq M4PjdmROW09? M{PuNoVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NYi4OWxSOjV2MEmxNlQ>
A549 MmjiR4VtdCCYaXHibYxqfHliQYPzZZk> NV7ke5VKOC1{MDFOwG0> MYm3NkBp M1PObWROW09? M1vFNYRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? M1O5V|I2Ozh6N{[y
H1299 NHX0XpdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEXwZ2ExNTJyIN88US=> MkeyO|IhcA>? NXHod2twTE2VTx?= M1rUeYRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? MnHqNlU{QDh5NkK=
HO-8910 MmH5R4VtdCCYaXHibYxqfHliQYPzZZk> MV6wMVIxKM7:TR?= NXrCT2ZVPzJiaB?= MV\EUXNQ NXv3V|NO\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NFHp[5EzPTN6OEe2Ni=>
HT-29 MYTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFnjWYsxNTJyIN88US=> NFy5TG44OiCq MWDEUXNQ MX3k[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv M3j3flI2Ozh6N{[y
HCT-116 NGKwTIhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkLnNE0zOCEQvF2= MX:3NkBp M3Lnb2ROW09? MYjk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NITa[WozPTN6OEe2Ni=>
A549 NWnNR3E1SXCxcITvd4l{KEG|c3H5 M2XE[VIxKM7:TR?= NV70V4ZkPDhiaB?= NGLUclhFVVOR NGnrXotqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIgh[XOyaYLpci=> M2jO[FI2Ozh6N{[y
H1299 NGPDNoFCeG:ydH;zbZMhSXO|YYm= NE\Hc2MzOCEQvF2= NIjZcoo1QCCq NFvoVpRFVVOR NYfv[4dQcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> NVn2UmsxOjV|OEi3OlI>
Sc-1 NYLrT3FIS2WubDDWbYFjcWyrdImgRZN{[Xl? MYKwMlAxODFvMTFOwG0> NYT6R3ozQTZiaB?= NFKyTGZl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIXyeIszPTN5M{WwPC=>
OcI-LY18 M3fxfGNmdGxiVnnhZoltcXS7IFHzd4F6 NXT2d4xmOC5yMECxMVEh|ryP NUL0[2tqQTZiaB?= MWXk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4DsWFI2Ozd|NUC4
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
PARP / c-PARP / cleaved caspase 3 ; 

PubMed: 21393866     


H146 cells were preincubated in normoxia or hypoxia (1% O2) for 18 hours prior to treatment with ABT-737 (89.1 nM ), after which cells were harvested for protein analysis by Western blot. 

Hif-1a; 

PubMed: 22006676     


Representative western blots for HIF-1α, PARP and cleaved caspase 3 in response to 24-72 hr exposure to ABT-737 in varying concentration in normoxia and hypoxia in 4 neuroblastoma cell lines. Actin is shown as a loading control. Blots are representative of 3 independent experiments.

γ-H2AX / p-ATM; 

PubMed: 21084274     


Induction of γ-H2AX and p-ATM by ABT-737. Cells were treated with 10 µmol/L ABT-737 for 24 hours and then maintained in fresh media for 1 or 2 more days prior to Western blot analysis.

21393866 22006676 21084274
Immunofluorescence
cytochrome C; 

PubMed: 26447615     


Immunocytochemistry revealed the release of mitochondrial cytochrome c (green) into the cytoplasm after ABT-737 exposure (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field.

Bax; 

PubMed: 26447615     


Immunocytochemistry revealed the mitochondrial translocation of Bax from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field C. To assess whether ABT-737 treatment has an effect on the dimerization of Bax, the levels of dimeric Bax were measured with or without ABT-737 treatment in MC-3 and HN22 cells.

Bim; 

PubMed: 26447615     


Immunocytochemistry revealed the mitochondrial translocation of Bim from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field.

AIF; 

PubMed: 25034785     


localization of apoptosis inducing factor (AIF) in LCSC pre-stained with Mitotracker Red and untreated or treated with 500 nM ABT-737 for 48 h. Magnification × 60, zoom × 3, bar 20 μm. 

p65 ; 

PubMed: 28846096     


BCL-xL dependent SVEC cells were treated with ABT-737 (10 μM) +/- Q-VD-Oph (30 μM) for 1 h, immunostained for p65 and analysed by confocal microscopy. TNF (20 ng/ml) was used as positive control for p65 nuclear translocation. Scale bar represents 30μM. Representative images from three independent experiments.

26447615 25034785 28846096
Growth inhibition assay
Cell viability; 

PubMed: 22311987     


Stably transfected K562 cells were treated with increasing concentrations of ABT-737, obatoclax, or maritoclax for 24 h. Cell viability was determined by measuring intracellular ATP levels with the CellTiter Glo assay.

22311987
ELISA
IL-6 / IL-8; 

PubMed: 21084274     


The secretion of IL-6 and IL-8 in PV-10 cells treated with DMSO, ABT-737 or enantiomer for 24 hours was determined by ELISA.

21084274
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[4]

+ 展開
  • 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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (122.93 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% Propylene glycol, 5% Tween 80, 65% D5W
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 813.43
化学式

C42H45ClN6O5S2

CAS No. 852808-04-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What’s the recommended method about reconstitution of the compound for in vivo animal study?

  • 回答:

    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.

Bcl-2シグナル伝達経路

Bcl-2 Inhibitors with Unique Features

相関Bcl-2製品

Tags: ABT-737を買う | ABT-737 ic50 | ABT-737供給者 | ABT-737を購入する | ABT-737費用 | ABT-737生産者 | オーダーABT-737 | ABT-737化学構造 | ABT-737分子量 | ABT-737代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID