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  NWOwNlVZS2WubDDWbYFjcWyrdImgRZN{[Xl? MXiyOVAhdk4EoB?= M{Hzb|czKGh? NITSNWhFVVOR MX7jZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRmNNPiC|aWLORS=> NILwUmwzPjZ3N{K4PC=>
KG1a NV63O4Q1S2WubDDWbYFjcWyrdImgRZN{[Xl? NVu3WmF2OC1zMDFOwG0> NF\VbJYzPCCq MWjEUXNQ MljZTWM2OD15Lk[4JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFK4eZczPjV3MkexNi=>
Kasumi-1 M1LWfGNmdGxiVnnhZoltcXS7IFHzd4F6 NXXsW5VJOC1zMDFOwG0> MnzsNlQhcA>? MoG0SG1UVw>? NV:2ZZVUUUN3ME20Mlg4KM7:TTyg[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NG\mWZAzPjV3MkexNi=>
KG1a M2HD[2Fxd3C2b4Ppd{BCe3OjeR?= MmPhNE0yOCEQvF2= MmHHNlQhcA>? MXfEUXNQ M1vwSYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWeyOlU2OjdzMh?=
Kasumi-1 Mnr6RZBweHSxc3nzJGF{e2G7 Mlv6NE0yOCEQvF2= NXW1Smc4OjRiaB?= MnzKSG1UVw>? Ml:0bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYOwSItwOjZ3NUK3NVI>
MC-3  M3jNc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUO1M|ExNzJyIN88US=> NW\uNlRFOjRiaB?= MVLEUXNQ MojmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFXHXGMzPjR2N{[xOS=>
HN22  MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nROFIvPS95LkWvNlIvPSEQvF2= M37UV|I1KGh? M1ntNmROW09? M1nL[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVXMWZNTOjZ2NEe2NVU>
MC-3  NWHQSnZ3SXCxcITvd4l{KEG|c3H5 MVi1M|ExNzJyIN88US=> MYCyOEBp M4LKNGROW09? NXL4UJp[cW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> MnywNlY1PDd4MUW=
HN22  MXjBdI9xfG:|aYOgRZN{[Xl? MnvBNk42NzdwNT:yNk42KM7:TR?= NHjpNIwzPCCq M2m3bmROW09? NGnNTo9qdmS3Y3XzJINie3Cjc3WtcYVlcWG2ZXSgZZBweHSxc3nz MnS5NlY1PDd4MUW=
MOLT-4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPmZ5BFOTBvNUCwNEBvVQ>? NFizT5U4OiCq NET6ZmtFVVOR M{TQN2lEPTB;MD6xPVgh|ryP NFTJO4czPjN7MkOzNi=>
RS4;11 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn2ZYh1OTBvNUCwNEBvVQ>? NXT0W4hKPzJiaB?= MmfaSG1UVw>? MYTJR|UxRTBwMECyJO69VQ>? MYGyOlM6OjN|Mh?=
JURKAT NHHFXphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxNE02ODByIH7N Mo\vO|IhcA>? M1nkOmROW09? NVXHcFFvUUN3ME22OkDPxE1? M3LwblI3Ozl{M{Oy
CEM R M1P4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\5SYFHOTBvNUCwNEBvVQ>? M{nr[|czKGh? MYjEUXNQ NEHUNotKSzVyPUWuOEDPxE1? MV6yOlM6OjN|Mh?=
CEM S NGSxeGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmxNE02ODByIH7N NUXpdHlNPzJiaB?= M{\aZmROW09? NHnaXpdKSzVyPUGyMlEh|ryP NUTrelJEOjZ|OUKzN|I>
MOLT-4 MX7BdI9xfG:|aYOgRZN{[Xl? NHX3PIwyOC1zMECwJI5O M3nRfVI1KGh? MYHEUXNQ M2m0VYNifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x NH;lbpUzPjN7MkOzNi=>
CEM S M4X6bWFxd3C2b4Ppd{BCe3OjeR?= MYmxNE0yODByIH7N MYWyOEBp NU\jXGJ7TE2VTx?= NVHL[m9v[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> MViyOlM6OjN|Mh?=
JURKAT MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjnRpIyODBvMUCwNEBvVQ>? NGnTXHo1QCCq NGPocHdFVVOR MUPJR|UxRTl3NdMxPU4{KG6P NETj[HYzPjF5MkK2PS=>
LOUCY MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2xNFAuOTByMDDuUS=> MnzZOFghcA>? M3vEVmROW09? NF3JVnFKSzVyPUOyMljDuTFyLkmgcm0> MVOyOlE4OjJ4OR?=
WM-115 NVvufJYyS2WubDDWbYFjcWyrdImgRZN{[Xl? NFz4OnMyODEEoH7N NU\RZ4UzPzJiaB?= NGL1XYlmdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= MorSNlYyOTZ5N{[=
B16 NIjyc5FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFn2fIgyODEEoH7N MVO3NkBp MXnlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? M4nrfFI3OTF4N{e2
HL-60  NEGwZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT1eZBbPzJiaB?= MkKwTWM2OMLiPTCxNE44KG6P M1fOeVI3ODR3NkC5
MOLM-13  NHLRNYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWq3NkBp NULBW3RTUUN3MNMgQUAzPy57IH7N MUKyOlA1PTZyOR?=
OCI-AML3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\4T2w4OiCq MY\JR|UxyqB;IEG5OVAhdk1? M{XTWFI3ODR3NkC5
BCWM.1 Mo[4RZBweHSxc3nzJGF{e2G7 MWiwMVEvPiEQvF2= MY[yOEBp M{TQ[olv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NI\WPZkzPTh7M{K5NC=>
MWCL-1 MXXBdI9xfG:|aYOgRZN{[Xl? MmDLNE0yNjZizszN NVy2[I12OjRiaB?= NFTWS5VqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MlfGNlU5QTN{OUC=
MM.1s NGTseJdCeG:ydH;zbZMhSXO|YYm= MX6wMVEvPiEQvF2= NHTL[WUzPCCq NHrucXdqdmS3Y3XzJINmdGxiYYDvdJRwe2m| Mn7CNlU5QTN{OUC=
HCT116 NHLPZ4dHfW6ldHnvckBCe3OjeR?= Mn\lN{8yOCEQvF2= MYqxNuKhcMLi MUjEUXNQ MmrjbY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w NHzMZWMzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO NIXHOmVHfW6ldHnvckBCe3OjeR?= NH:2NIo{NzFyIN88US=> NFnTOZcyOsLiaNMg NUjGVVNpTE2VTx?= M1rOWolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= NHrXTo4zPTdzNUCyPC=>
HCT116 M3;iW2Z2dmO2aX;uJGF{e2G7 MYGxNEDPxE1? NUTCboFVOTMEoHlCpC=> MVvEUXNQ MUDpcoNz\WG|ZYOgS2ZRNUyFM1KgdJVv[3Sj NXP4WmNwOjV5MUWwNlg>
HCT116 BAX BAK1 DKO NEfvUXVHfW6ldHnvckBCe3OjeR?= MmWxNVAh|ryP NF\P[FAyOsLiaNMg NIHLdItFVVOR NFznb|NqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th NX\Xc412OjV5MUWwNlg>
HCT116 M1HpOGF2fG:yaHHnfUBCe3OjeR?= NVrDVJE4OTBizszN NVzQTnJiOTMEoHlCpC=> M3vCZWROW09? MV;pcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> MWCyOVcyPTB{OB?=
HCT116 BAX BAK1 DKO NHXXfoVCfXSxcHjh[5khSXO|YYm= MUexNEDPxE1? NIey[24yOsLiaNMg M3fvcGROW09? NXu0dGhDcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? MnrvNlU4OTVyMki=
U937 M1jnfmFxd3C2b4Ppd{BCe3OjeR?= NYfoOVJwOC5zMkWtNkDPxE1? M3;yZVI1KGh? M2HuTIVvcGGwY3XzJGRJSS:[LUGxMYlv\HWlZXSgZZBweHSxc3nz MkDRNlU4OTRyMkS=
U937  M1;2OGFxd3C2b4Ppd{BCe3OjeR?= M2KwU|AvPSEQvF2= MlPBNlQhcA>? NF\Yd2ZmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs M4j5T|I2PzF2MEK0
HL-60 AAA-Bcl-2 NF7OeJNCeG:ydH;zbZMhSXO|YYm= MkD4NE02KM7:TR?= M3TEelQ5KGh? M{njTGlEPTB;MD64O{DPxG4xvJzpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVLNbWNyOjV5MUG0OlA>
HL-60 EEE-Bcl-2 NHu5fWdCeG:ydH;zbZMhSXO|YYm= MX[wMVUh|ryP M2X5flQ5KGh? NGDRW5dKSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUiyOVcyOTR4MB?=
U87 MlzQSpVv[3Srb36gRZN{[Xl? MV:1NEDPxE1? NF\LbZkzPCCq M{TpPJJm\HWlZYOgeIhmKG2UTlGg[ZhxemW|c3nvckBt\X[nbIOgc4YhVU2SLUKsJG1OWC1zNDDhcoQhSmOuLUK= M3TuSFI2PjZ5Nk[z
K562 M1P2WWNmdGxiVnnhZoltcXS7IFHzd4F6 NIDreooyNTFyIN88US=> M4P6cVQ5KGh? MU\EUXNQ NInWSWpKSzVyPUK2Mlch|ryP NXm1UXVZOjV3OU[1OlE>
K562/Mcl -1-IRESBim MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTlwMzFOwG0> MlvQNlU2OzV7MEC=
K562/Bcl- 2-IRESBim NGPkTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\VNYtjUUN3ME2wMlM2KM7:TR?= M4rPclI2PTN3OUCw
Jurkat NYTPeVBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPXTWM2OD1yLk[2JO69VQ>? Mmi2NlU2OzV7MEC=
JurkatΔBak NYTu[3lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzmZWhYUUN3ME61NEDPxE1? Mlm2NlU2OzV7MEC=
HL60/VCR NYLYR|Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTrXYdpUUN3ME6xNFAh|ryP MVmyOVU{PTlyMB?=
Kasumi-1 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrYSoFpUUN3ME2wMlAyKM7:TR?= MUGyOVU{PTlyMB?=
Kasumi-1/ABT NGK5VpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHO4S45KSzVyPUCuOVEh|ryP NEjpelUzPTV|NUmwNC=>
THP-1 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moi2TWM2OD1zLkK3JO69VQ>? M2\idFI2PTN3OUCw
U937 NELJRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HIV2lEPTB;NT6yPUDPxE1? NH62SJQzPTV|NUmwNC=>
C1498 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf0Z5lKSzVyPU[uNVMh|ryP M2PNdlI2PTN3OUCw
RPMI 8226 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMkWg{txO MWWyOVU{PTlyMB?=
MM.1S MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HQWGlEPTB;MD60NEDPxE1? MnixNlU2OzV7MEC=
NCI-H929 M2rsO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITpdZRKSzVyPUG1MlIyKM7:TR?= NHjTWnMzPTV|NUmwNC=>
U266 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjLTWM2OD1yLk[4JO69VQ>? NVvt[JE6OjV3M{W5NFA>
MCF-7 NHvnUVlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFvxS5Q2KM7:TR?= NHrFflE1QCCq NHPVT21FVVOR MV7lcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v Ml[wNlU1ODlzMkS=
MCF-7 NUjae3Q3SXCxcITvd4l{KEG|c3H5 MmLVOUDPxE1? NEDpTpk1NzJ2L{S4JIg> MWTEUXNQ MkjobY5kemWjc3XzJJRp\SClbHXheoVlKFCDUmC= NIXBOG4zPTRyOUGyOC=>
MCF-7 NVTzWY9oTnWwY4Tpc44hSXO|YYm= MUe1JO69VQ>? Ml3SNlQhcA>? MYDEUXNQ MkPi[Y5p[W6lZYOgeIhmdGW4ZXygc4YhVWOuLUGg[ZhxemW|c3nvcuKh M{nBSVI2PDB7MUK0
MDA-MB 231  MoXMSpVv[3Srb36gRZN{[Xl? MkK1OUDPxE1? MVmyOEBp MmXjSG1UVw>? M1fQZoVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NWjQN3p6OjV2MEmxNlQ>
ZR-75-1  MUXGeY5kfGmxbjDBd5NigQ>? NYLBe2NNPSEQvF2= MoKzNlQhcA>? MX\EUXNQ M2XROIVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NVfDdYxjOjV2MEmxNlQ>
A549 NWT2R4F3S2WubDDWbYFjcWyrdImgRZN{[Xl? NFjuT|kxNTJyIN88US=> NEHmT2w4OiCq M160SGROW09? MoXi[IVkemWjc3XzJJRp\SClZXzsJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyJINwdWKrbnXkJJdqfGhiYYPwbZJqdg>? MlLLNlU{QDh5NkK=
H1299 M1[yRmNmdGxiVnnhZoltcXS7IFHzd4F6 M2LLbFAuOjBizszN NF;xV2I4OiCq MYrEUXNQ NHTVXGpl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NUK1TZp5OjV|OEi3OlI>
HO-8910 NFqwb3ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFrHcJUxNTJyIN88US=> M1XDO|czKGh? NFnxTIVFVVOR NGrkfmll\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw M2jzTVI2Ozh6N{[y
HT-29 M{XtT2NmdGxiVnnhZoltcXS7IFHzd4F6 MnrlNE0zOCEQvF2= MmHRO|IhcA>? MV7EUXNQ M1jHN4Rm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? NW[2TGNZOjV|OEi3OlI>
HCT-116 NV3TfYY2S2WubDDWbYFjcWyrdImgRZN{[Xl? NV3H[I1KOC1{MDFOwG0> Ml3DO|IhcA>? MVHEUXNQ NHHXRpVl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[2:vYnnu[YQhf2m2aDDhd5Bqemmw NFzzU4MzPTN6OEe2Ni=>
A549 NVTRc2dGSXCxcITvd4l{KEG|c3H5 NY\NN2JVOjBizszN NYH0R4ppPDhiaB?= M13PTmROW09? M{\zdYlv\HWlZYOgZZBweHSxc3nzJJNq\26rZnnjZY51dHliY3;tZolv\WRid3n0bEBie3Crcnnu NXHVTVNrOjV|OEi3OlI>
H1299 NXTaToJ5SXCxcITvd4l{KEG|c3H5 MXGyNEDPxE1? NITPTXI1QCCq MVLEUXNQ NUXOPGtOcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKGG|cHnybY4> MorjNlU{QDh5NkK=
Sc-1 M2DlZ2NmdGxiVnnhZoltcXS7IFHzd4F6 NWTje292OC5yMECxMVEh|ryP NH7DSW46PiCq NHzTW|Fl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEDXRpAzPTN5M{WwPC=>
OcI-LY18 MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnXONE4xODBzLUGg{txO NH;uPVA6PiCq NXXQUXBC\GWlcnXhd4V{KHSqZTDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXOyOVM4OzVyOB?=
RL  NHnqW4xE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV\MPVRNOC5yMECxMVEh|ryP NYX2TnJqQTZiaB?= MXzk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4LYN|I2Ozd|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 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。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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