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 322 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  NGWwd41E\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn3KNlUxKG6PwrC= MkezO|IhcA>? MVvEUXNQ MVHjZZV{\WRiOUelJIxwe3Nib3[geoli[mmuaYT5JIlvKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRmNNPiC|aWLORS=> NF70clY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1O|I5QCd-Mk[2OVczQDh:L3G+
KG1a NWTz[4N4S2WubDDWbYFjcWyrdImgRZN{[Xl? MnzvNE0yOCEQvF2= MYWyOEBp NXXOTZg1TE2VTx?= NFfLNoNKSzVyPUeuOlgh|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEPt[nE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW1NlcyOid-Mk[1OVI4OTJ:L3G+
Kasumi-1 NXjIe3ZnS2WubDDWbYFjcWyrdImgRZN{[Xl? MV6wMVExKM7:TR?= M2TyN|I1KGh? NXzEWXV7TE2VTx?= MonnTWM2OD12Lki3JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M17LfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO|EzLz5{NkW1NlcyOjxxYU6=
KG1a MmTKRZBweHSxc3nzJGF{e2G7 NGf4dIgxNTFyIN88US=> NFXYdI8zPCCq MYPEUXNQ NV3o[JBJcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4XNNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO|EzLz5{NkW1NlcyOjxxYU6=
Kasumi-1 MYHBdI9xfG:|aYOgRZN{[Xl? NVn1[3NQOC1zMDFOwG0> MYiyOEBp NGX3d|ZFVVOR MlzEbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn;UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NUK3NVIoRjJ4NUWyO|EzRC:jPh?=
MC-3  NY\0cmpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWm1M|ExNzJyIN88US=> NXLk[pF6OjRiaB?= MlPvSG1UVw>? M2r0bolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
HN22  M2TBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\QNk42NzdwNT:yNk42KM7:TR?= NXfqRmx2OjRiaB?= NGPCRYZFVVOR MXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1LhVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O|YyPTxxYU6=
MC-3  NICyNYRCeG:ydH;zbZMhSXO|YYm= Mm\UOU8yOC9{MDFOwG0> MYWyOEBp M2LHbGROW09? MW\pcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| M1Hkb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NES3OlE2Lz5{NkS0O|YyPTxxYU6=
HN22  M4PKdWFxd3C2b4Ppd{BCe3OjeR?= MnLYNk42NzdwNT:yNk42KM7:TR?= NI\4U3czPCCq NFPIfWNFVVOR NYrTNVkzcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> MoLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEe2NVUoRjJ4NES3OlE2RC:jPh?=
MOLT-4 M17He2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3CT|VYOTBvNUCwNEBvVQ>? M4jYRlczKGh? MVzEUXNQ Moi0TWM2OD1yLkG5PEDPxE1? MkfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
RS4;11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHlNVAuPTByMDDuUS=> MkHiO|IhcA>? MofFSG1UVw>? MUHJR|UxRTBwMECyJO69VQ>? MnfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
JURKAT Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzpOosyOC13MECwJI5O M4HES|czKGh? NYnDfYFKTE2VTx?= MUPJR|UxRTZ4IN88US=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
CEM R M{fFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES3UHoyOC13MECwJI5O NWnhZ5F{PzJiaB?= M1[4WWROW09? NVTNN4lwUUN3ME21MlQh|ryP NF\0Sng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM S MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorzNVAuPTByMDDuUS=> MWK3NkBp NXr6T3R3TE2VTx?= MYTJR|UxRTF{LkGg{txO MmXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
MOLT-4 NVu0UGlWSXCxcITvd4l{KEG|c3H5 M1;yclExNTFyMECgcm0> MmqyNlQhcA>? NWK3PWN6TE2VTx?= NIrHOpVk[XW|ZYOgeIhmKGOuZXH2ZYdmKG:oIFLjcE0zKGGwZDD0bIUh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIFv\CCPY3ytNS=> NHLCcWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM S MlzrRZBweHSxc3nzJGF{e2G7 NI\Z[W8yOC1zMECwJI5O NHLmVZQzPCCq MXvEUXNQ NXvOPHBK[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> M{nhVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
JURKAT NHrMXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHjN4oyODBvMUCwNEBvVQ>? M1vJdlQ5KGh? M3nQS2ROW09? MnHjTWM2OD17NUZCtVkvOyCwTR?= NWnFbpNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xO|IzPjlpPkK2NVczOjZ7PD;hQi=>
LOUCY MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3O0OFExOC1zMECwJI5O MmrROFghcA>? MV7EUXNQ MWHJR|UxRTN{LklCtVExNjlibl2= M4ewZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUeyNlY6Lz5{NkG3NlI3QTxxYU6=
WM-115 M4e1T2NmdGxiVnnhZoltcXS7IFHzd4F6 MljDNVAxyqCwTR?= NY\0c49rPzJiaB?= MVzlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NWnJUoFFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVY4PzZpPkK2NVE3Pzd4PD;hQi=>
B16 NVjFPZR5S2WubDDWbYFjcWyrdImgRZN{[Xl? NXLj[GRGOTBywrDuUS=> NYXlcoY1PzJiaB?= MVPlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNke3Okc,OjZzMU[3O|Y9N2F-
HL-60  MnXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fQeVczKGh? MVfJR|UxyqB;IEGwMlchdk1? NIeyS3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OVYxQSd-Mk[wOFU3ODl:L3G+
MOLM-13  NGD5S5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLuO|IhcA>? M3u5RmlEPTEEoE2gNlcvQSCwTR?= M1TScVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES1OlA6Lz5{NkC0OVYxQTxxYU6=
OCI-AML3 NGfTW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWG3NkBp MYnJR|UxyqB;IEG5OVAhdk1? M{PNUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES1OlA6Lz5{NkC0OVYxQTxxYU6=
BCWM.1 M3izeGFxd3C2b4Ppd{BCe3OjeR?= MUmwMVEvPiEQvF2= M1X4eFI1KGh? MmjZbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NX\DdGRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4PVMzQTBpPkK1PFk{OjlyPD;hQi=>
MWCL-1 M3vRe2Fxd3C2b4Ppd{BCe3OjeR?= NVfNXHV[OC1zLk[g{txO NUDabJhDOjRiaB?= NHHQOHdqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M{PEW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N|I6ODxxYU6=
MM.1s M3jQO2Fxd3C2b4Ppd{BCe3OjeR?= MnfSNE0yNjZizszN NE[1NYczPCCq MXHpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh7M{K5NEc,OjV6OUOyPVA9N2F-
HCT116 NHzXN2xHfW6ldHnvckBCe3OjeR?= MWCzM|ExKM7:TR?= MYOxNuKhcMLi MoC0SG1UVw>? M4n6VIlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= M1LLR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116 BAX BAK1 DKO M2G2cGZ2dmO2aX;uJGF{e2G7 NWjTS4FIOy9zMDFOwG0> NHzQSGsyOsLiaNMg MXPEUXNQ MV;pcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? MlPNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116 MlTHSpVv[3Srb36gRZN{[Xl? NF65VIYyOCEQvF2= MmTnNVLDqGkEoB?= NHf6TnJFVVOR MlvVbY5kemWjc3XzJGdHWC2OQ{PCJJB2dmO2YR?= M4LyOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116 BAX BAK1 DKO NUPqXGd4TnWwY4Tpc44hSXO|YYm= MYKxNEDPxE1? NFrTWoUyOsLiaNMg NEi3dppFVVOR MVPpcoNz\WG|ZYOgS2ZRNUyFM1KgdJVv[3Sj MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNUCyPEc,OjV5MUWwNlg9N2F-
HCT116 NXf5[JNPSXW2b4DoZYd6KEG|c3H5 MX6xNEDPxE1? NWjYPHdrOTMEoHlCpC=> M4HmV2ROW09? NGfxN4NqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yC{ZYPwc45{\Q>? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNUCyPEc,OjV5MUWwNlg9N2F-
HCT116 BAX BAK1 DKO MYDBeZRweGijZ4mgRZN{[Xl? M1SyW|ExKM7:TR?= MXOxNuKhcMLi NIX0fW5FVVOR M4HsTolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKHKnc4DvcpNm NV\1Um9oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
U937 NHjafVhCeG:ydH;zbZMhSXO|YYm= NFrYVIkxNjF{NT2yJO69VQ>? NF32T2YzPCCq MYflcohidmOnczDETGEwYC1zMT3pcoR2[2WmIHHwc5B1d3Orcx?= M4jybVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G0NFI1Lz5{NUexOFAzPDxxYU6=
U937  NUXoTlBlSXCxcITvd4l{KEG|c3H5 MknvNE42KM7:TR?= NX\5Uo1FOjRiaB?= NInTdpVmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzNECyOEc,OjV5MUSwNlQ9N2F-
HL-60 AAA-Bcl-2 NXzCfVRkSXCxcITvd4l{KEG|c3H5 MWSwMVUh|ryP MoDZOFghcA>? MlTETWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzMUS2NEc,OjV5MUG0OlA9N2F-
HL-60 EEE-Bcl-2 NV7KSmlRSXCxcITvd4l{KEG|c3H5 Mn\uNE02KM7:TR?= MWm0PEBp NFHqfYpKSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTdzMUS2NEc,OjV5MUG0OlA9N2F-
U87 M3i2U2Z2dmO2aX;uJGF{e2G7 NWG5bo45PTBizszN MVeyOEBp MlTadoVlfWOnczD0bIUhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDv[kBOVVBvMjygUW1RNTF2IHHu[EBD[2xvMh?= NXPkcHJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2Olc3PjNpPkK1OlY4PjZ|PD;hQi=>
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Rh18 MX\xTHRUKGG|c3H5 MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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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.

  • (Only for Reference)
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
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(122.93 mM)
Water Insoluble
Ethanol Insoluble

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

* 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.

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
If you have any other enquiries, please leave a message.

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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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