TW-37

Catalog No.S1121

TW-37 Chemical Structure

Molecular Weight(MW): 573.7

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.

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In DMSO USD 146 In stock
USD 160 In stock
USD 680 In stock
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Cited by 17 Publications

9 Customer Reviews

  • (a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.

    Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.

    (b) Whole-cell lysates of H23 cells exposed for 0–24 h to TW-37 (10 uM) were probed with antibodies against PARP and caspase-9. The appearance of both the p89 processed form of PARP and the p35 form of caspase-9 were characteristic of the intrinsic pathway of apoptosis.

    Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.

  • (c) Whole-cell lysates of BAK-reconstituted and -deficient Jurkat cells exposed for 0–24 h to TW-37 (10 uM ) were probed as in B. % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.

    Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.

    (d) Electron micrographs of control and TW-37 (10 uM for 24 h); treated BAK-reconstituted and -deficient Jurkat cells reveal a dependence on BAK for TW-37- mediated apoptosis (scale bar, 5 um)

    Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.

  • MCL-1 is a key anti-apoptotic BCL-2 family member that regulates ER membrane reorganisation. (a) Pan-BCL-2 family inhibitors induce ER membrane reorganisation more potently than BCL-2 and BCL-XL-specific inhibitors. Apogossypol (10 μM) and TW37 (20 μM) induced extensive membrane reorganisation, assessed by BAP31 staining in HeLa cells, within 4 h of exposure, whereas ABT-737 (20 μM) induced modest reorganisation after 8 h and the inactive enantiomer ABT-737E (20 μM) failed to induce reorganisation (scale bar, 20 μm).

    Cell Death Differ 2012 19, 1896-907. TW-37 purchased from Selleck.

    Cytotoxicity of TW-37 monotherapy. TTC549 cells and KP-MRTRY cells were seeded in 96-well plates, incubated for 24 h, treated with TW-37 (0-1,000 nM), and then analyzed. TW-37 IC50 values for the TTC549 and KP-MRT-RY cell lines were 554 and 588 nM, respectively.

    J Cell Physiol, 2016, 231(9):1932-40. TW-37 purchased from Selleck.

  • Sensitivity to ABT-199 and TW-37 in AML cell lines. Using ABT-199 and TW-37 to antagonise BCL-2 and MCL-1 respectively. The IC50s shown were obtained from alamar blue assays after treating 11 AML cell lines at a starting cell concentration of 2.5x105 /ml for 48 hours. Each cell line thawed is tested around the time of its final passage to authenticate its provenance using the Powerplex 16 kit to amplify short tandem repeats.

    PLoS One, 2018, 13(1): e0190682. TW-37 purchased from Selleck.

    MEF cells were treated for  24 hours with the Bcl-2 antagonists  TW-37at the indicated doses.Acute survival was monitored by propidium iodide uptake assays(red lines).Long term survival(red line) was measured by replacing the drug-containing media with normal media and incubating the cells until visible colonies formed.Clonogenic survival is expressed relative to the numbers of colonies formed following 24 hours incubation in normal media(lacking drugs).

    Dr. Christine Hawkins of La Trobe University. TW-37 purchased from Selleck.

  • MDB-MA-231 cells were exposed to 30 um cisplatin in the absence or in thepresence of 100 nm TW-37.The cell were stained with Hoechst 33342,MitoTracker Red and Yo-pro-1.

     

     

    Dr. Zhang of Tianjin Medical University. TW-37 purchased from Selleck.

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Biological Activity

Description TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.
Targets
Mcl-1 [1]
(Cell-free assay)
Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
0.26 μM(Ki) 0.29 μM(Ki) 1.11 μM(Ki)
In vitro

TW-37 targets the BH3-binding groove in Bcl-2 where proapoptotic Bcl-2 proteins bind, and shows higher affinity and selectivity for Bcl-2 and Mcl-1 over Bcl-xL with Ki values of 0.29 μM, 0.26 μM and 1.11 μM, respectively. [1] In vitro, TW-37 shows significant anti-proliferative and pro-apoptotic effect in a de novo chemo-resistant WSU-DLCL2 lymphoma cell line and primary cells obtained from a lymphoma patient without effects on normal peripheral blood lymphocytes. [1] TW-37 exhibits the inhibitory effect on both cell growth and cell death in endothelial cell with IC50 of approximately 1.8 μM without effect on the fibroblasts exposed to the same concentration range as the endothelial cells. In addition, TW37 also shows the anti-proliferation effects in MCF-7, LNCaP, and SLK tumor cell lines with the same or lower concentration range than those required to inhibit endothelial cell growth. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human JAR cell NVSwRWR6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvkTY5pcWKrdHnvckBw\iCqdX3hckBLSVJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Lk[gcm0> MoPCV2FPT0WU
human Ca9-22 cell NWOydnhTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1TLNmlvcGmkaYTpc44hd2ZiaIXtZY4hS2F7LUKyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= NWWzU|Q5W0GQR1XS
human CHL-1 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkLqTY5pcWKrdHnvckBw\iCqdX3hckBEUExvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlkhdk1? NHTnT|BUSU6JRWK=
human A549 cell NX7BVm4yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnFfmVKdmirYnn0bY9vKG:oIHj1cYFvKEF3NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4xQSCwTR?= NGHOWJFUSU6JRWK=
human RKO cell M2\DPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3LkG3JI5O NYnmWHlmW0GQR1XS
human GCIY cell NHL4T2tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mor4TY5pcWKrdHnvckBw\iCqdX3hckBIS0m\IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkCuPFMhdk1? M37q[HNCVkeHUh?=
human BHT-101 cell M1rSeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGnMfZdKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS56MzDuUS=> MV;TRW5ITVJ?
human Hs-578-T cell M2fRemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJGh{NTV5OD3UJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvPTlibl2= NHrrcIhUSU6JRWK=
human SK-UT-1 cell M3nNVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHjPfFdKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC54ODDuUS=> MWjTRW5ITVJ?
human NB7 cell NHfCXIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5DPyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7LkK4JI5O NHX5S3dUSU6JRWK=
human YKG-1 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnH1TY5pcWKrdHnvckBw\iCqdX3hckB[U0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5Mlc3KG6P NFP4VXdUSU6JRWK=
human HuH-7 cell MmLLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3LzVGlvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNk45OiCwTR?= NFnoT|VUSU6JRWK=
human SAS cell NIHQUnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnOTY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Mz6xPEBvVQ>? MUTTRW5ITVJ?
human UACC-62 cell M2jPVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVe1[3dmUW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVYzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwM{Wgcm0> NWDLVWZyW0GQR1XS
human AGS cell NI[4fXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF\Y[VZKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO3MlU{KG6P MULTRW5ITVJ?
human SK-MEL-30 cell NH;Xbm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XKTmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzdwOUegcm0> NUTmXZhLW0GQR1XS
human A427 cell NWfy[|UxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI\GVllKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OE43QSCwTR?= NFH4PJpUSU6JRWK=
human DU-145 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NI\pdGNKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUzNjF|IH7N MoLFV2FPT0WU
human HCT-116 cell M{[3dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Nk43PiCwTR?= NVS2OYxvW0GQR1XS
human A673 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2\1fWlvcGmkaYTpc44hd2ZiaIXtZY4hSTZ5MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWzMlg2KG6P M2S5R3NCVkeHUh?=
human SF126 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWnJcohq[mm2aX;uJI9nKGi3bXHuJHNHOTJ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuNFchdk1? NUfzWY9SW0GQR1XS
human SW872 cell NGXiU49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnq0TY5pcWKrdHnvckBw\iCqdX3hckBUXzh5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW4Mlkhdk1? MYHTRW5ITVJ?
human NCI-H1581 cell NFX5SHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2G2emlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOVgyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjdwNkSgcm0> NIXWbZFUSU6JRWK=
human SK-MEL-5 cell M1PWXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHiTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVY6NjJ3IH7N NGjsRmtUSU6JRWK=
human CP50-MEL-B cell NW\w[oxyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFL5O3VKdmirYnn0bY9vKG:oIHj1cYFvKEOSNUCtUWVNNUJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14OT61PUBvVQ>? MVHTRW5ITVJ?
human YH-13 cell NVvZRZlET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYTSe3U6UW6qaXLpeIlwdiCxZjDoeY1idiC\SD2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcxNjV7IH7N NWfBbJpNW0GQR1XS
human LXF-289 cell M2rSeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUP0fmplUW6qaXLpeIlwdiCxZjDoeY1idiCOWF[tNlg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PzJwOEWgcm0> M{H6NXNCVkeHUh?=
human MC-IXC cell NUj0SFFFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NE\lcI1KdmirYnn0bY9vKG:oIHj1cYFvKE2FLVnYR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc2NjN|IH7N M{mwUnNCVkeHUh?=
human NB14 cell NH3vXodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvIS3lTUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|YvPDVibl2= NY\SOHVYW0GQR1XS
human HEC-1 cell NYfZb5pCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGhGSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OEGuN|chdk1? MkTxV2FPT0WU
human U-87-MG cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mof2TY5pcWKrdHnvckBw\iCqdX3hckBWNTh5LV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFIvOjRibl2= MUPTRW5ITVJ?
human HOS cell M2CyNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjQNVZDUW6qaXLpeIlwdiCxZjDoeY1idiCKT2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OE44OSCwTR?= MYTTRW5ITVJ?
human HUTU-80 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7zdHBKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05Py5yMTDuUS=> NH;Ob2pUSU6JRWK=
human A375 cell Mn3IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVLic4lRUW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFgvQDNibl2= MWHTRW5ITVJ?
human A204 cell M3TWfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3jQNWlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3Mlg1KG6P NITnOYdUSU6JRWK=
human GB-1 cell NGnTNXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2K5NmlvcGmkaYTpc44hd2ZiaIXtZY4hT0JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlY6KG6P M4HkdXNCVkeHUh?=
human MDA-MB-231 cell NYm2UlBYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXlfXBUUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOjNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNFgxPyEQvF2= MlzHV2FPT0WU
human SW982 cell NEPxd3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2TPOGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyODdizszN MXXTRW5ITVJ?
human SW756 cell M1X5cGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlz1TY5pcWKrdHnvckBw\iCqdX3hckBUXzd3NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVEzOzZizszN MWHTRW5ITVJ?
human MG-63 cell M2[zemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUTJcohq[mm2aX;uJI9nKGi3bXHuJG1INTZ|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVI1QCEQvF2= M4ftSHNCVkeHUh?=
human Daoy cell NHjnVnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH\pVWJKdmirYnn0bY9vKG:oIHj1cYFvKESjb4mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE1ODd|IN88US=> MVjTRW5ITVJ?
human MDA-MB-453 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUPwTYxtUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuPDV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOVE5QCEQvF2= MUTTRW5ITVJ?
human HT-144 cell NGjqcllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml;ETY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OjBzIN88US=> MWfTRW5ITVJ?
human LoVo cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2Kx[GlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVYxQTNizszN NWDURXk2W0GQR1XS
human NY cell NF7LTWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLTWHJKdmirYnn0bY9vKG:oIHj1cYFvKE6\IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xO|c3OiEQvF2= MljUV2FPT0WU
human SW1783 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrzS2xKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUe4N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjF|MEGg{txO MVvTRW5ITVJ?
human A2780 cell M{PUfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\kOFBMUW6qaXLpeIlwdiCxZjDoeY1idiCDMke4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjF6NE[g{txO Mn\zV2FPT0WU
human MDA-MB-361 cell MkDOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mkf3TY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtN|YyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{Mk[0JO69VQ>? MnS3V2FPT0WU
human RPMI-2650 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvMk[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN6M{Gg{txO M4\HZnNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo TW-37 shows a maximum tolerated dose (MTD) of 40 mg/kg for three i.v. injections in severe combined immunodeficient (SCID) mice when given alone, and enhances tumor inhibitory effect of cyclophosphamide-doxorubicin-vincristine-prednisone (CHOP) regimen. [1] TW-37, administrated by i.v. produces the antiangiogenic effect by decreasing the density of functional human microvessels in the severe combined immunodeficient mouse model of human angiogenesis. [2] The combination of TW-37 and MEK inhibitors synergistically block melanoma cell growth in mice by a significant reduction in tumor volume and tumor mass. [3]

Protocol

Kinase Assay:[1]
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Fluorescence polarization-based binding assay for recombinant Bcl-2, Bcl-XL, and Mcl-1 protein :

For this assay, the 21-residue BH3 peptide QEDIIRNIARHLAQVGDSMDR derived from Bid labeled with 6-carboxyfluorescein succinimidyl ester (FAM-Bid) and recombinant proteins derived from human Bcl-2,Bcl-X L,and Mcl-1 are employed. It is determined that FAM-Bid has a Ki of 11 nM to Bcl-2 protein,25 nM to Bcl-XL protein,and 5.7 nM to Mcl-1 protein. The competitive binding assay for Bcl-XL is same as that for Bcl-2 with the following exceptions: 30 nM Bcl-XL protein and 2.5 nM FAM-Bid peptide in the following assay buffer [50 mM Tris-Bis (pH 7.4) and 0.01% bovine gamma-globulin].
Cell Research:[2]
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  • Cell lines: HDMECs
  • Concentrations: 0 - 100 μM
  • Incubation Time: 96 hours
  • Method: The sulforhodamine B (SRB) cytotoxicity assay is used as described. Briefly, optimal cell density for cytotoxicity assay is determined by growth curve analysis. HDMECs are seeded in a 96-well plate and allowed to adhere overnight. Drug or control is diluted in EGM2-MV and layered onto cells, which are allowed to incubate for times as indicated in the figures. Alternatively, HDMECs are coincubated with TW37 and 0 to 100 ng/mL recombinant human VEGF (rhVEGF)165 or 0 to 100 ng/mL recombinant human CXCL8. Cells are fixed on the plates by addition of cold trichloroacetic acid (10% final concentration) and incubation for 1 hour at 4 °C. Cellular protein is stained by addition of 0.4% SRB in 1% acetic acid and incubation at room temperature for 30 minutes. Unbound SRB is removed by washing with 1% acetic acid and the plates are air dried. Bound SRB is resolubilized in 10 mM unbuffered Tris-base and absorbance is determined on a microplate reader at 560 nm. Test results are normalized against initial plating density and drug-free controls. Data are obtained from triplicate wells per condition and are representative of at least three independent experiments
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Athymic NCr-nu/nu mice bearing SK-Mel-147 melanoma xenografts
  • Formulation: TW-37 is resuspended in 1:1 Tween 80/ethanol (diluted 10-fold in 0.9% saline before use).
  • Dosages: ~40 mg/kg
  • Administration: Administered via i.v. or i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 115 mg/mL (200.45 mM)
Ethanol 4 mg/mL (6.97 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/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 573.7
Formula

C33H35NO6S

CAS No. 877877-35-5
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID