ABT-737

Catalog No.S1002

For research use only.

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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

ABT-737 Chemical Structure

CAS No. 852808-04-9

Selleck's ABT-737 has been cited by 334 publications

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Other Bcl-2 Products

Biological Activity

Description 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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
Features First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
Targets
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)
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OCI-Ly1  MmjVR4VtdCCYaXHibYxqfHliQYPzZZk> MYGyOVAhdk4EoB?= MoSzO|IhcA>? M1LhPGROW09? NWDOT21Z[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? MorYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUeyPFgoRjJ4NkW3Nlg5RC:jPh?=
KG1a M4W3[GNmdGxiVnnhZoltcXS7IFHzd4F6 NXHQOHlSOC1zMDFOwG0> NUKxTJY{OjRiaB?= MUXEUXNQ M1fiNmlEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NH31VXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW1NlcyOid-Mk[1OVI4OTJ:L3G+
Kasumi-1 NV:4[JZoS2WubDDWbYFjcWyrdImgRZN{[Xl? NHu1U3YxNTFyIN88US=> MmK2NlQhcA>? NUPUNoZoTE2VTx?= MXTJR|UxRTRwOEeg{txONCCmZXPy[YF{\XNiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkjqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NUK3NVIoRjJ4NUWyO|EzRC:jPh?=
KG1a Mm\QRZBweHSxc3nzJGF{e2G7 M1PMU|AuOTBizszN MXqyOEBp MX3EUXNQ MV;pcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIXoWHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW1NlcyOid-Mk[1OVI4OTJ:L3G+
Kasumi-1 NVfwfI84SXCxcITvd4l{KEG|c3H5 NFzNXYcxNTFyIN88US=> MVKyOEBp Mn;USG1UVw>? NETEXYJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M33V[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO|EzLz5{NkW1NlcyOjxxYU6=
MC-3  M2PNb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLr[Zc2NzFyL{KwJO69VQ>? MX:yOEBp MWnEUXNQ Mn\SbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
HN22  Mlm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLhclkzNjVxNz61M|IzNjVizszN M4fCc|I1KGh? MY\EUXNQ MlWzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{XrSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O|YyPTxxYU6=
MC-3  NYjubIF1SXCxcITvd4l{KEG|c3H5 NX7sZ5RyPS9zMD:yNEDPxE1? NYq4b3JjOjRiaB?= NFnQR29FVVOR MX\pcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| NGTFNIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS0O|YyPSd-Mk[0OFc3OTV:L3G+
HN22  NFzWcZZCeG:ydH;zbZMhSXO|YYm= MVWyMlUwPy53L{KyMlUh|ryP NFKzS2MzPCCq NUjEUlFFTE2VTx?= NX\kWWNGcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> NGjmbGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS0O|YyPSd-Mk[0OFc3OTV:L3G+
MOLT-4 NFXyeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofiNVAuPTByMDDuUS=> M3;H[|czKGh? NGDRcHhFVVOR M4HqNGlEPTB;MD6xPVgh|ryP NUew[VN{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVI{OzJpPkK2N|kzOzN{PD;hQi=>
RS4;11 NWL1dINCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxNE02ODByIH7N M{fJVVczKGh? NVKzPGhNTE2VTx?= M3zqbWlEPTB;MD6wNFIh|ryP M{\zXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
JURKAT NE\RTHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTBclBmOTBvNUCwNEBvVQ>? MYS3NkBp MWXEUXNQ MWLJR|UxRTZ4IN88US=> NELyc4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM R NETWfYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\VfmViOTBvNUCwNEBvVQ>? MV:3NkBp NGX3S5NFVVOR NFLJOm5KSzVyPUWuOEDPxE1? M1PCdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
CEM S MkTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TGelExNTVyMECgcm0> MkPFO|IhcA>? NVjGN2xSTE2VTx?= NVPqTGRMUUN3ME2xNk4yKM7:TR?= M1jXblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
MOLT-4 MXLBdI9xfG:|aYOgRZN{[Xl? M2f5c|ExNTFyMECgcm0> MmrlNlQhcA>? M2K4[WROW09? MVrjZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= NF7Kc3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM S NIDsbZZCeG:ydH;zbZMhSXO|YYm= MkfsNVAuOTByMDDuUS=> MWWyOEBp MlLFSG1UVw>? NF3IZVJk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
JURKAT NWLad|RUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELaPHMyODBvMUCwNEBvVQ>? NXe0NJAzPDhiaB?= MY\EUXNQ NFr5d3pKSzVyPUm1OeKyQS5|IH7N MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF5MkK2PUc,OjZzN{KyOlk9N2F-
LOUCY NInuS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XTd|ExOC1zMECwJI5O M{PIVVQ5KGh? M{G4dGROW09? NIC3dY1KSzVyPUOyMljDuTFyLkmgcm0> M4jzelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUeyNlY6Lz5{NkG3NlI3QTxxYU6=
WM-115 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlnBNVAxyqCwTR?= MWm3NkBp MUXlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NEXEWo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlc4Pid-Mk[xNVY4PzZ:L3G+
B16 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXL3WVJ[OTBywrDuUS=> MWG3NkBp MXvlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NFzmXZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlc4Pid-Mk[xNVY4PzZ:L3G+
HL-60  MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:0fFczKGh? MUHJR|UxyqB;IEGwMlchdk1? M1mzfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES1OlA6Lz5{NkC0OVYxQTxxYU6=
MOLM-13  NYTRfmVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHiO|IhcA>? MYnJR|UxyqB;IEK3Mlkhdk1? MknDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNEW2NFkoRjJ4MES1OlA6RC:jPh?=
OCI-AML3 MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H4VFczKGh? M3fvNGlEPTEEoE2gNVk2OCCwTR?= NV;KbHFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOFU3ODlpPkK2NFQ2PjB7PD;hQi=>
BCWM.1 MYnBdI9xfG:|aYOgRZN{[Xl? MnLONE0yNjZizszN MUiyOEBp M1\tU4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M1L0eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N|I6ODxxYU6=
MWCL-1 MUTBdI9xfG:|aYOgRZN{[Xl? MXSwMVEvPiEQvF2= NXKweGdtOjRiaB?= MlTqbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NXfxVoNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4PVMzQTBpPkK1PFk{OjlyPD;hQi=>
MM.1s M2fwXGFxd3C2b4Ppd{BCe3OjeR?= Mom1NE0yNjZizszN MVuyOEBp MlX6bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M2foV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N|I6ODxxYU6=
HCT116 NWrCXWlpTnWwY4Tpc44hSXO|YYm= M2\RZlMwOTBizszN NGC3eVAyOsLiaNMg Mki2SG1UVw>? NF\ud3RqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hVEN|Qj3JTUBkd264ZYLzbY9vKGGwZDDTVXNVVTFiZHXndoFl[XSrb36= NYTiVXp6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
HCT116 BAX BAK1 DKO MYPGeY5kfGmxbjDBd5NigQ>? NFTEcHo{NzFyIN88US=> NUTLT3p7OTMEoHlCpC=> NFS5SlFFVVOR M36wZYlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= NFHx[2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 MWTGeY5kfGmxbjDBd5NigQ>? M{C4dVExKM7:TR?= NUTyVoxJOTMEoHlCpC=> MmX3SG1UVw>? NWG3cFk5cW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> NIfDTmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 BAX BAK1 DKO NFTUU|FHfW6ldHnvckBCe3OjeR?= NITSOpQyOCEQvF2= M2jDUVEzyqCqwrC= NEHjbnBFVVOR NV3mcXZ2cW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> NEDHPJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 MVXBeZRweGijZ4mgRZN{[Xl? M4jUZ|ExKM7:TR?= NFf4dFEyOsLiaNMg MU\EUXNQ Mm\EbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> M3fXeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116 BAX BAK1 DKO MUHBeZRweGijZ4mgRZN{[Xl? M{LWd|ExKM7:TR?= MlnpNVLDqGkEoB?= MV\EUXNQ NVGwTVk2cW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNicnXzdI9ve2V? NWjic3FPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
U937 NVewb4xrSXCxcITvd4l{KEG|c3H5 NXXjTWZPOC5zMkWtNkDPxE1? MmXvNlQhcA>? M4njRoVvcGGwY3XzJGRJSS:[LUGxMYlv\HWlZXSgZZBweHSxc3nz M3niRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G0NFI1Lz5{NUexOFAzPDxxYU6=
U937  NFPQR4tCeG:ydH;zbZMhSXO|YYm= M1rHPVAvPSEQvF2= M{LZOVI1KGh? NIPW[lRmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs MoTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUSwNlQoRjJ3N{G0NFI1RC:jPh?=
HL-60 AAA-Bcl-2 M2Dw[mFxd3C2b4Ppd{BCe3OjeR?= Ml71NE02KM7:TR?= NXrVTGxHPDhiaB?= NIjkNG1KSzVyPUCuPFch|ryv78{MbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWi2dIRoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVE1PjBpPkK1O|EyPDZyPD;hQi=>
HL-60 EEE-Bcl-2 MofvRZBweHSxc3nzJGF{e2G7 MVWwMVUh|ryP M3vKXlQ5KGh? NGrvfZRKSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NULkV|BqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVE1PjBpPkK1O|EyPDZyPD;hQi=>
U87 MVPGeY5kfGmxbjDBd5NigQ>? MVu1NEDPxE1? NFvUZWkzPCCq MlzmdoVlfWOnczD0bIUhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?= MlPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4Nke2OlMoRjJ3Nk[3OlY{RC:jPh?=
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NB1643 MlPzdWhVWyCjc4PhfS=> NV\3ZXd5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| M{i0N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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Assay
Methods Test Index PMID
Western blot PARP / c-PARP / cleaved caspase 3 ; Hif-1a ; γ-H2AX / p-ATM 21393866 22006676 21084274
Immunofluorescence cytochrome C ; Bax ; Bim ; AIF ; p65 26447615 25034785 28846096
Growth inhibition assay Cell viability 22311987
ELISA IL-6 / IL-8 21084274
In vivo 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]

Protocol (from reference)

Kinase Assay:

[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.

Cell Research:

[4]

  • Cell lines: SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
  • Concentrations: 0.001-10 μM
  • Incubation Time: 48 hours
  • Method:

    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.

Animal Research:

[1]

  • Animal Models: Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
  • Dosages: 20 and 30 mg/kg
  • Administration: For intraperitoneal (i.p.) every day

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2%DMSO+40%PEG300+5%Tween80+53%ddH2O
For best results, use promptly after mixing.

2mg/mL

Chemical Information

Molecular Weight 813.43
Formula

C42H45ClN6O5S2

CAS No. 852808-04-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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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.

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