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.

Size Price Stock Quantity  
In DMSO USD 146 In stock
USD 160 In stock
USD 680 In stock
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  • (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.

  • 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 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHXydHJKdmirYnn0bY9vKG:oIHj1cYFvKEqDUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuOkBvVQ>? M2fjT3NCVkeHUh?=
human Ca9-22 cell MkPiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH\oSIhKdmirYnn0bY9vKG:oIHj1cYFvKEOjOT2yNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDJibl2= M3zmcXNCVkeHUh?=
human CHL-1 cell NHPtbllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYLhPWhDUW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjlibl2= NFvCbpBUSU6JRWK=
human A549 cell NHvlc4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3vKSGlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlA6KG6P MWHTRW5ITVJ?
human RKO cell M2jJNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3LkG3JI5O M{nnbHNCVkeHUh?=
human GCIY cell M4nVV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJGdEUVliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MD64N{BvVQ>? NV;4cI9tW0GQR1XS
human BHT-101 cell NUi5SHlCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4qwUGlvcGmkaYTpc44hd2ZiaIXtZY4hSkiWLUGwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjh|IH7N MYXTRW5ITVJ?
human Hs-578-T cell NWjVOZNDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvjTY5pcWKrdHnvckBw\iCqdX3hckBJey13N{itWEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjV7IH7N NGfYNmFUSU6JRWK=
human SK-UT-1 cell NEjNbZJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV\pN4t7UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3VWE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjhwNkigcm0> NIXQWVRUSU6JRWK=
human NB7 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NE\FT|NKdmirYnn0bY9vKG:oIHj1cYFvKE6ENzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5MlI5KG6P NV\lO|ByW0GQR1XS
human YKG-1 cell M4fXPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKGi3bXHuJHlMTy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkmuO|Yhdk1? M4K5N3NCVkeHUh?=
human HuH-7 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfOTY5pcWKrdHnvckBw\iCqdX3hckBJfUhvNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOyMlgzKG6P MUXTRW5ITVJ?
human SAS cell NED4UWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3f0[GlvcGmkaYTpc44hd2ZiaIXtZY4hW0GVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{OuNVghdk1? MnzxV2FPT0WU
human UACC-62 cell NHjiS|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH7RPW9KdmirYnn0bY9vKG:oIHj1cYFvKFWDQ1OtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC5|NTDuUS=> MlWxV2FPT0WU
human AGS cell Mmn3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3v2SWlvcGmkaYTpc44hd2ZiaIXtZY4hSUeVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{euOVMhdk1? MYPTRW5ITVJ?
human SK-MEL-30 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM4Njl5IH7N NHLwNZdUSU6JRWK=
human A427 cell NHnPWplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlrJTY5pcWKrdHnvckBw\iCqdX3hckBCPDJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NESuOlkhdk1? NHzMXHBUSU6JRWK=
human DU-145 cell M2XFTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFKy[GxKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUzNjF|IH7N MVXTRW5ITVJ?
human HCT-116 cell NIfCV3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4izNGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUzNjZ4IH7N M1rLN3NCVkeHUh?=
human A673 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLHc|RxUW6qaXLpeIlwdiCxZjDoeY1idiCDNkezJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVMvQDVibl2= M4HKcHNCVkeHUh?=
human SF126 cell NGnDOXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfrXlJqUW6qaXLpeIlwdiCxZjDoeY1idiCVRkGyOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU4NjB5IH7N MoPKV2FPT0WU
human SW872 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4DRXWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d6N{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PE46KG6P NEXmVVBUSU6JRWK=
human NCI-H1581 cell M4nSSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MofTTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG1PFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03Py54NDDuUS=> M4GzbHNCVkeHUh?=
human SK-MEL-5 cell NXi4UYtjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1jUNGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS5{NTDuUS=> MoPEV2FPT0WU
human CP50-MEL-B cell Ml3LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1z3fGlvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ7LkW5JI5O Mne2V2FPT0WU
human YH-13 cell NE\qO2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mm\ZTY5pcWKrdHnvckBw\iCqdX3hckB[UC1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUewMlU6KG6P NUTwfWIzW0GQR1XS
human LXF-289 cell M3LGNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIjvXJNKdmirYnn0bY9vKG:oIHj1cYFvKEy[Rj2yPFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04Oi56NTDuUS=> MoKxV2FPT0WU
human MC-IXC cell M3PncGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlf4TY5pcWKrdHnvckBw\iCqdX3hckBOSy2LWFOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23OU4{OyCwTR?= NYX5PXlSW0GQR1XS
human NB14 cell M3n3RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2LBOGlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUe2MlQ2KG6P NHjBdJhUSU6JRWK=
human HEC-1 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NE\QW3FKdmirYnn0bY9vKG:oIHj1cYFvKEiHQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFEvOzdibl2= MmntV2FPT0WU
human U-87-MG cell M1PNUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn31TY5pcWKrdHnvckBw\iCqdX3hckBWNTh5LV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFIvOjRibl2= NWDOboR1W0GQR1XS
human HOS cell NWLRVZlrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFPlfGxKdmirYnn0bY9vKG:oIHj1cYFvKEiRUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUi0MlcyKG6P NH3oU|lUSU6JRWK=
human HUTU-80 cell NXXYeWt1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTw[4pKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05Py5yMTDuUS=> NFHib5hUSU6JRWK=
human A375 cell NV7UUGl[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{e2PWlvcGmkaYTpc44hd2ZiaIXtZY4hSTN5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUi4Mlg{KG6P M3\TVHNCVkeHUh?=
human A204 cell NE\adnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGEzODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17Nz64OEBvVQ>? M3HrZXNCVkeHUh?=
human GB-1 cell MmHES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI\xWVZKdmirYnn0bY9vKG:oIHj1cYFvKEeELUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25PE43QSCwTR?= NIfINVVUSU6JRWK=
human MDA-MB-231 cell NEDyPG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkH2TY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zMEiwO{DPxE1? NULTN3I6W0GQR1XS
human SW982 cell M4W3W2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVvYTYd7UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTFyNzFOwG0> M4C1e3NCVkeHUh?=
human SW756 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkjUTY5pcWKrdHnvckBw\iCqdX3hckBUXzd3NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVEzOzZizszN MoHJV2FPT0WU
human MG-63 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkP4TY5pcWKrdHnvckBw\iCqdX3hckBOTy14MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVEzPDhizszN NVHEVIh[W0GQR1XS
human Daoy cell Mn:2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGRid3liY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG0NFc{KM7:TR?= NGnIUWpUSU6JRWK=
human MDA-MB-453 cell NH;hcIpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4jtNWlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ2OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUWxPFgh|ryP MnG5V2FPT0WU
human HT-144 cell NIPpTJhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlXVTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OjBzIN88US=> NWrFd|A4W0GQR1XS
human LoVo cell Mlf0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mlv2TY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlA6OyEQvF2= MX3TRW5ITVJ?
human NY cell NV7yeI55T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJG5[KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zN{e2NkDPxE1? M2T2XnNCVkeHUh?=
human SW1783 cell NGfvZ|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYTJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTd6MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlE{ODFizszN NU[zNWUyW0GQR1XS
human A2780 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUXJcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNVg1PiEQvF2= M3XlVnNCVkeHUh?=
human MDA-MB-361 cell M2LJbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHP6c4dKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk0{PjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKyOlQh|ryP MUTTRW5ITVJ?
human RPMI-2650 cell M{GzNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1rkSWlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST2yOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{M{izNUDPxE1? NVLRVplsW0GQR1XS

... 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]
+ Expand
  • 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 individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID