Alvespimycin (17-DMAG) HCl

For research use only.

Catalog No.S1142 Synonyms: NSC 707545,BMS 826476 HCl,KOS 1022

50 publications

Alvespimycin (17-DMAG) HCl Chemical Structure

CAS No. 467214-21-7

Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

Selleck's Alvespimycin (17-DMAG) HCl has been cited by 50 publications

Purity & Quality Control

Choose Selective HSP (HSP90) Inhibitors

Biological Activity

Description Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.
Features A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.
Targets
HSP90 [1]
(Cell-free assay)
62 nM
In vitro

17-DMAG displays ~2 times potency against human Hsp90 than 17-AAG, with IC50 of 62 nM versus 119 nM. In SKBR3 and SKOV3 cells which over-express Hsp90 client protein Her2, 17-DMAG causes down-regulation of Her2 with EC50 of 8 nM and 46 nM, respectively, as well as induction of Hsp70 with EC50 of 4 nM and 14 nM, respectively, leading to significant cytotoxicity with GI50 of 29 nM and 32 nM, respectively, consistent with Hsp90 inhibition. [1] 17-DMAG in combination with vorinostat synergistically induces apoptosis of the cultured MCL cells as well as primary MCL cells, more potently than either agent alone, by markedly attenuating the levels of cyclin D1 and CDK4, as well as of c-Myc, c-RAF and Akt. [3] In contrast to 17-AAG which is only active for IKKβ in chronic lymphocytic leukemia (CLL) cells, 17-DMAG treatment effectively leads to depletion of the Hsp90 client protein, resulting in diminished NF-κB p50/p65 DNA binding, decreased NF-κB target gene transcription, and caspase-dependent apoptosis. By targeting the NF-κB family, 17-DMAG selectively mediates dose- and time-dependent cytotoxicity against CLL cells, but not normal T cells or NK cells important for immune surveillance. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKBr3 NXHMcHU2S3m2b4TvfIlkcXS7IHHzd4F6 NIfCOFFEgXSxdH;4bYNqfHliYXfhbY5{fCCVS1LyN{Bk\WyuczygTWM2OD1yLkCyOO69VS5? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjF4NUO1OEc,OTZzNkWzOVQ9N2F-
SKBR3 NEHTeIdHfW6ldHnvckBie3OjeR?= NFTmV4hWeHKnZ4XsZZRqd25ib3[gTJNxPzBiaX6gV2tDWjNiY3XscJMtKEWFNUC9NE4xODUQvF2u MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKBR3 M3S5fGZ2dmO2aX;uJIF{e2G7 MXrE[Ydz[WSjdHnvckBw\iCKZYKyJIlvKFONQmKzJINmdGy|LDDFR|UxRTBwMEC4{txONg>? NID2OpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNki1OFA3Pid-MU[4OVQxPjZ:L3G+
SKOV3 NXz6bGVRTnWwY4Tpc44h[XO|YYm= MYjVdJJm\3WuYYTpc44hd2ZiSIPwO|AhcW5iU1vPWlMh[2WubIOsJGVEPTB;MD6wNVTPxE1w M3nLSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY3Lz5zNki1OFA3PjxxYU6=
SKOV3 M1i2SGZ2dmO2aX;uJIF{e2G7 MWTE[Ydz[WSjdHnvckBw\iCKZYKyJIlvKFONT2[zJINmdGy|LDDFR|UxRTBwMES2{txONg>? M17JT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY3Lz5zNki1OFA3PjxxYU6=
AGS NWO4NIxjTnWwY4Tpc44h[XO|YYm= MVexOkBpenN? MlzwTY5pcWKrdHnvckBw\iCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hSUeVIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmyb4jpZU1qdmS3Y3XkJIx2[2moZYLhd4Uh\XiycnXzd4lwdiCjZoTldkAyPiCqcoOgZpkhemWyb4L0[ZIh[XO|YYmsJGlEPTB;MD6wN|bPxE1w M1rQO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
Hep3B MnrCSpVv[3Srb36gZZN{[Xl? M3PNUlE3KGi{cx?= NIi2[2hKdmirYnn0bY9vKG:oIFjJSlEh[WO2aY\heIlwdiCrbjDoeY1idiCKZYCzRkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCudXPp[oVz[XOnIHX4dJJme3Orb36gZYZ1\XJiMU[gbJJ{KGK7IILldI9zfGW{IHHzd4F6NCCLQ{WwQVAvODZzzszNMi=> NYj2Uow{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1PFM6PTBpPkG3OVg{QTVyPD;hQi=>
AGS NH\JfGFHfW6ldHnvckBie3OjeR?= M{PX[VI1KGi{cx?= MnzqWoli[mmuaYT5JI9nKGi3bXHuJGFIWyClZXzsd{B2dmSncjDuc5Jud3irYzDjc45lcXSrb37zJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUdOwG0v MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV6M{m1NEc,OTd3OEO5OVA9N2F-
NCI-H526 NXzhVFBtTnWwY4Tpc44h[XO|YYm= MYOxJJVO MoToNlQhcHK| NULRb2hbSmmwZHnu[{Bi\m[rbnn0fUB1dyCKU2C5NEBqdiCqdX3hckBPS0lvSEWyOkBk\WyuczDheEAyKHWPIHHmeIVzKDJ2IHjyd{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5 MljKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4MEO1OFAoRjF5NkCzOVQxRC:jPh?=
NCI-H526 M{C3NGZ2dmO2aX;uJIF{e2G7 NF20N3QyKHWP NVvXTIo4QTZiaILz NITUeIdKdmirYnn0bY9vKG:oIFjTVFkxNW2nZHnheIVlKHC{b3zp[oVz[XSrb36gc4YhcHWvYX6gUmNKNUh3Mk[gZ4VtdHNiYYSgNUB2VSCjZoTldkA6PiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeR?= NGH1[I09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[wN|U1OCd-MUe2NFM2PDB:L3G+
AGS MUXGeY5kfGmxbjDhd5NigQ>? MU\Jcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzIHHjeIl3[XSrb36gbY4hcHWvYX6gRWdUKGOnbHzzJIJ6KHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OC5yMEO2{txONg>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN3OU[zNUc,OTh|NUm2N|E9N2F-
HeLa Moq2SpVv[3Srb36gZZN{[Xl? NG\qeWJKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIF7GMYtieHCjQjDhZ5RqfmG2aX;uJIlvKGi3bXHuJGhmVGFiY3XscJMtKEmFNUC9NE4yPc7:TT6= M2TiTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{W5OlMyLz5zOEO1PVY{OTxxYU6=
HeLa MWnDfZRwfG:6aXPpeJkh[XO|YYm= MmL3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi5yNt88UU4> MlrhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|NUm2N|EoRjF6M{W5OlMyRC:jPh?=
AGS NGrpe5VEgXSxdH;4bYNqfHliYYPzZZk> NGfJXJJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCT1NiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTF4zszNMi=> NIX2RWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
A2058 NXXjU|NKS3m2b4TvfIlkcXS7IHHzd4F6 NF7kPHVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjB3ODDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNFIy|ryPLh?= MkfxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
MDA-MB-231 MYHGeY5kfGmxbjDhd5NigQ>? MkGxTY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGinckKg[IVoemGmYYTpc44tKEmFNUC9NE4xODR3zszNMi=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl{OUS4Okc,OTh7Mkm0PFY9N2F-
MDA-MB-231 NEexTpFEgXSxdH;4bYNqfHliYYPzZZk> M4jtZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODB3ON88UU4> NF\Ue5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
A2058 M2jKd2Z2dmO2aX;uJIF{e2G7 NVTDVpFzUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCDMkC1PEBk\WyuczygSWM2OD1yLkCwO|nPxE1w M2TrPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
MDA-MB-231 NVrwNGZlTnWwY4Tpc44h[XO|YYm= M3;3T2lvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCDa4Sg[IVoemGmYYTpc44tKEmFNUC9NE4xOTd4zszNMi=> Mk\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
A2058 M{PRNmZ2dmO2aX;uJIF{e2G7 NVfwRlZMUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCDMkC1PEBk\WyuczDhd5Nme3OnZDDhd{BCc3RiZHXndoFl[XSrb36sJGlEPTB;MD6wNlQ{|ryPLh?= NIrDdXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
HuH7 MWfBcpRqfmm{YXygZZN{[Xl? MVqzJIRigXN? M1jlbmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJIdmdm:2eYDlJFFjKEOxbkGgbY5n\WO2ZXSgbY4hcHWvYX6gTJVJPyClZXzsd{Bie3Onc4Pl[EBieyCJQWDETEBTVkFib4KgNVhUKHKUTlGgcIV3\WxiYX\0[ZIhOyCmYYnzJIJ6KHGUVD3QR3Ih[W6jbInzbZMtKEWFNUC9NE4xODF{zszNMi=> NFWwcXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmzOlE6OSd-MUi5N|YyQTF:L3G+
HuH7 MWLBcpRqfmm{YXygZZN{[Xl? MXGzJIRigXN? NYe1SZo3SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KENidnnyeZMh\2Wwb4T5dIUhOWJiQ3;uNUBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IFfBVGRJKFKQQTDvdkAyQFNicmLORUBt\X[nbDDh[pRmeiB|IHThfZMhe2WuZXP0[YQhf2m2aDC0NEBvVSCKQ2[tO|k3KGGwZDC4NFAhdk1iYn;j[ZBz\X[rcjDifUByWlRvUFPSJIFv[Wy7c3nzMEBGSzVyPUCuNFA{Oc7:TT6= M3rJ[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUO2NVkyLz5zOEmzOlE6OTxxYU6=
SKBR3 NVzCSZlzTnWwY4Tpc44h[XO|YYm= MXPCbY5lcW6pIHHm[olvcXS7IITvJGh{eDlyIHnuJIh2dWGwIGPLRnI{KGOnbHzzMEBKSzVyPUCuNFI1|ryPLh?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTBzN{W2Nkc,OTlyMUe1OlI9N2F-
Hep3B MX3GeY5kfGmxbjDhd5NigQ>? MXOzNEBucW6| MWDJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzYXzwbIEheHKxdHXpckBi[2O3bYXsZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgeJJm[XSnZDDmc5IhOzBibXnud{Bu\WG|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVAvODV5Mt88UU4> M37pdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MEeyNlE1Lz5zOUC3NlIyPDxxYU6=
Hep3B MnjySpVv[3Srb36gZZN{[Xl? NFP6cZcyPiCqcoO= MoHmTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhXkWJRjDwdo91\WmwIIPlZ5JmfGmxbjDpckBpfW2jbjDI[ZA{SiClZXzsd{Bi\nSncjCxOkBpenNiYomgSWxKW0FuIFnDOVA:OC5yN{m1{txONg>? NGfGRYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUC3NlIyPCd-MUmwO|IzOTR:L3G+
HCT116 NWnqVlZvS3m2b4TvfIlkcXS7IHHzd4F6 NEXkdmk4OiCqcoO= MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEW3{txONg>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ|MUi2OEc,OTl{M{G4OlQ9N2F-
SKBR3 MlHUR5l1d3SxeHnjbZR6KGG|c3H5 NIOwO2k4OiCqcoO= NV3EUGVSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFU5|ryPLh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ|MUi2OEc,OTl{M{G4OlQ9N2F-
MCF7 M171XmN6fG:2b4jpZ4l1gSCjc4PhfS=> MoXJO|IhcHK| NV23b5NGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD6wO|HPxE1w MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ|MUi2OEc,OTl{M{G4OlQ9N2F-
SKOV3 M4O2XWN6fG:2b4jpZ4l1gSCjc4PhfS=> MVu3NkBpenN? MnPaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMUKy{txONg>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ|MUi2OEc,OTl{M{G4OlQ9N2F-
SKBR3 MnXwR5l1d3SxeHnjbZR6KGG|c3H5 M2CzVVczKGi{cx?= MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4YhVlGRMTDpcohq[mm2b4Kg[Ilkd3WvYYLvcEwhUUN3ME2wMlI{|ryPLh?= NWPaSHMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyN|E5PjRpPkG5NlMyQDZ2PD;hQi=>
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MDA468 NX;wPG9VS3m2b4TvfIlkcXS7IHHzd4F6 M4O2OVczKGi{cx?= NUjtZnFuS3m2b4TvfIlkcXS7IHHnZYlve3RiTmGwNU1l\W[rY3nlcpQhcHWvYX6gUWRCPDZ6IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1zLkdOwG0v NXHOd|ZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyN|E5PjRpPkG5NlMyQDZ2PD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
HSP90 / HSP70 ; 

PubMed: 28915605     


Western blot analysis showing dose-dependent elevation of Hsp70 and HSP90 levels in AGS cells by 17-DMAG.

p-Akt / Survivin / MMP2 ; 

PubMed: 28915605     


Western blot analysis showing the dose-dependent reduction of the expression of HSP90 client proteins, such as p-Akt, survivin, and MMP2 by 17-DMAG.

PARP / Cleaved caspase-3 / Cleaved caspase-8 / Cleaved caspase-9 / PUMA ; 

PubMed: 28915605     


(C-D) 17-DMAG effects on the expression of apoptotic proteins (PARP, c-caspase 3, c-caspase-8, c-caspase-9, and PUMA) in AGS cells. Western blot analyses indicate that 17-DMAG significantly increased the expression of apoptotic proteins in AGS cells in a dose- (C) and time- (D) dependent manner (P < 0.05).

p-ALK / ALK / p-Akt / Akt / p-ERK / ERK ; 

PubMed: 26219569     


Modulation of ALK signaling in parental and 17-DMAG-resistant cells. Cells were treated with the indicated concentrations of 17-DMAG or AUY922 for 6 h. The molecules of ALK-related signaling activity were detected by western blot analysis.

α-Tax / α-IKKα / α-IKKβ/ α-NEMO / α-TBK1 / α-p65 / α-p50 ; 

PubMed: 24109220     


C8166, MT-2, and MT-4 cells were treated with 17-DMAG as indicated, and cell lysates were subjected to immunoblotting with the indicated antibodies.

28915605 26219569 24109220
Growth inhibition assay
Cell proliferation ; 

PubMed: 28915605     


Proliferation assay of AGS cells treated with graded concentrations of 17-DMAG for 24 h or 48 h. 17-DMAG resulted in significant dose- and time-dependent reduction of AGS cell proliferation (P < 0.05)

28915605
In vivo 17-DMAG treatment at 5 mg/kg or 25 mg/kg thrice per week significantly reduces tumor growth of TMK-1 xenografts, by significantly reducing vessel area and numbers of proliferating tumor cells in sections. [2] Consistent the inhibition of FAK signaling in vivo, 17-DMAG treatment at 25 mg/kg three times a week significantly suppresses tumor growth, and metastasis of ME180 and SiHa xenografts in mice. [4] Administration of 17-DMAG at 10 mg/kg for 16 days significantly decreases the white blood cell count and prolongs the survival in a TCL1-SCID transplant mouse model. [5]

Protocol

Kinase Assay:[1]
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Fluorescence polarization (FP)-based competition binding assay:

This assay utilizes a boron difluoride dipyrromethene (BODIPY) labeled geldanamycin analogue (BODIPY-AG) as a probe and measured fluorescence polarization upon binding of the probe to a protein. Native human Hsp90 protein (α + β isoforms) is isolated from HeLa cells. BODIPY-AG solution is freshly prepared in FP assay buffer (20 mM HEPES-KOH, pH 7.3, 1.0 mM EDTA, 100 mM KCl, 5.0 mM MgCl2, 0.01% NP-40, 0.1 mg/mL fresh bovine γ-globulin (BGG), 1.0 mM fresh DTT, and protease inhibitor from stock solution in DMSO. Competition curves are obtained by mixing 10 μL each of a solution containing BODIPY-AG and Hsp90, and a serial dilution of 17-DMAG freshly prepared in FP assay buffer from stock solution in DMSO. Final concentrations are 10 nM BODIPY-AG, 40 or 60 nM Hsp90, varying concentration of 17-DMAG (0.10 nM-10 μM), and ≤0.25% DMSO in a 384-well microplate. After 3 hours incubation at 30 °C, fluorescence anisotropy (γEx = 485 nm, γEm = 535 nm) is measured on an EnVision 2100 multilabel plate reader. IC50 value of 17-DMAG is obtained from the competition curves.
Cell Research:[5]
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  • Cell lines: Chronic lymphocytic leukemia (CLL)
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 24, or 48 hours
  • Method: Cells are exposed to various concentrations of 17-DMAG for 24, or 48 hours. For the assessment of cytotoxicity, MTT reagent is then added, and plates are incubated for an additional 24 hours before spectrophotometric measurement. Apoptosis is determined by staining with annexin V-fluorescein isothiocyanate and propidium iodide (PI).
    (Only for Reference)
Animal Research:[5]
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  • Animal Models: SCID mice engrafted with TCL1 leukemia cells
  • Dosages: 10 mg/kg
  • Administration: Intraperitoneal injection 5 times per week
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 131 mg/mL (200.54 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
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 653.21
Formula

C32H48N4O8•HCl

CAS No. 467214-21-7
Storage powder
in solvent
Synonyms NSC 707545,BMS 826476 HCl,KOS 1022
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)C)OC)OC(=O)N)C)C)O)OC.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × 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 SDS / 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 SDS / 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

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00780000 Terminated Drug: Alvespimycin Breast Cancer Bristol-Myers Squibb April 2008 Phase 2
NCT00248521 Unknown status Drug: alvespimycin hydrochloride Unspecified Adult Solid Tumor Protocol Specific Institute of Cancer Research United Kingdom|National Cancer Institute (NCI) October 2005 Phase 1

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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HSP (HSP90) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID