Geldanamycin (NSC 122750)

Catalog No.S2713

For research use only.

Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.

Geldanamycin (NSC 122750) Chemical Structure

CAS No. 30562-34-6

Selleck's Geldanamycin (NSC 122750) has been cited by 27 publications

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
Targets
p185 [4]
(SKBr3 cells)
HSP90 (N-terminal domain) [1]
(Cell-free assay)
HSP90 [1]
(Cell-free assay)
70 nM 0.78 μM(Kd) 1.2 μM(Kd)
In vitro

Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. [1] Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. [2] Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 Ml7wR49ueG:3bnSge4F{KGW4YXz1ZZRm\CCob4KgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJIxqdmViQUK3PFAtKEmFNUC9N{41KM7:TR?= MmHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF3MUSxOFUoRjFzNUG0NVQ2RC:jPh?=
SW620 cell M{jR[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPHTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4h[2:ub4LlZ5RidCClYYLjbY5wdWFiU2e2NlAh[2WubDDsbY5meyxiSVO1NF03NjJibl2= NFjJWIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNU[1PFg4QSd-MUW2OVg5Pzl:L3G+
MCF-7 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3jDcGlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKGK{ZXHzeEBk[W6lZYKgUWNHNTdiY3XscEBtcW6nczygTWM2OD14LkWgcm0> M1fp[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3NkW4PFc6Lz5zNU[1PFg4QTxxYU6=
K562 cell M1nl[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnSyTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4hdGW3a3XtbYEhUzV4MjDj[YxtKGyrbnXzMEBKSzVyPUKyMlEhdk1? M{WxNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3NkW4PFc6Lz5zNU[1PFg4QTxxYU6=
HT-29 cell Mn\NS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX\zTnVpUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgbJVu[W5iY3;sc5Jm[3SjbDDjZZJkcW6xbXGgTHQuOjliY3XscEBtcW6nczygTWM2OD1{ND61JI5O NXjGZ5lsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW2OVg5PzlpPkG1OlU5QDd7PD;hQi=>
SK-BR-3 NFPuNndHfW6ldHnvckBie3OjeR?= MX61NEBu\y:tZx?= MUHJcohq[mm2aX;uJI9nKG:wY3;n[Y5mKHC{b3T1Z5QheDF6NTDldoJDNTJiZoLvcUBpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHzzLHNMNUKULUOgZ4VtdHNrIHH0JFUxKG2pL3vnJIRwe2VuIFnDOVA:OC5yN988US=> MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwPzV4MkmxNUc,PzV4MkmxNVww[T5?
SK-BR-3 MojCSpVv[3Srb36gZZN{[Xl? NWPCXmxvUW5idnn0do8hcW6qaXLpeIlwdiCxZjDwNVg2KGW{YlKtNkBwdmOxcILveIVqdiCrbjDoeY1idiCkcnXhd5Qh[2GwY3XyJHNMNUKULUOgZ4VtdHNuIFnDOVA:OC5yN988US=> NGKwUYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi95NU[yPVEzLz55NU[yPVEzRC:jPh?=
MCF-7 M2[0dGZ2dmO2aX;uJIF{e2G7 MkPqTY5pcWKrdHnvckBw\iC|dHXh[Jkue3SjdHWg[ZhxemW|c3nvckBw\iCKRWKyJIlvKE2FRj23JIJz\WG|dDDjZY5k\XJiY3XscJMtKEmFNUC9NE4xPc7:TR?= M2DRVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyM{SwOlA2Lz5zMEO0NFYxPTxxYU6=
MCF-7 MlXmSpVv[3Srb36gZZN{[Xl? Mnr4TY5pcWKrdHnvckBw\iC|dHXh[Jkue3SjdHWg[ZhxemW|c3nvckBw\iCHUjDpckBOS0ZvNzDidoVie3RiY3HuZ4VzKGOnbHzzMEBKSzVyPUCuNFbPxE1? NGPu[3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMEO0NFYxPSd-MUCzOFA3ODV:L3G+
MCF-7 M4H5NGZ2dmO2aX;uJIF{e2G7 NFjofJFKdmirYnn0bY9vKG:oIIP0[YFlgS2|dHH0[UBmgHC{ZYPzbY9vKG:oIGLh[k0yKGmwIF3DSk04KGK{ZXHzeEBk[W6lZYKgZ4VtdHNuIFnDOVA:OC5{zszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODN2ME[wOUc,OTB|NEC2NFU9N2F-
SKBR-3 MkfaSpVv[3Srb36gZZN{[Xl? NFLpT2pG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDmc5IhUGW{LUKg[IVoemGmYYTpc44hcW5iU1vCVk0{KGOnbHzzMEBEd26lZX70doF1cW:wPUZOwG0> MkfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV5MUO0NVAoRjF3N{GzOFExRC:jPh?=
HEK293 MX7GeY5kfGmxbjDhd5NigQ>? Ml\qTY5pcWKrdHnvckBw\iCKU2C5NEBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGWoZnXjeEBwdiCDa4SxPpAzPyCrboTldoFkfGmxbjDjc41xdGW6ZYOgZpkhTVmIUDDhcoQwd3JiWV\QJHZmdnW|IH\yZYdu\W62IHLhd4VlKHKncH;yeIVzKGenbnWgZZN{[Xl? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ6MEG1PUc,OTZ4OECxOVk9N2F-
LS174T MoTjR5l1d3SxeHnjbZR6KGG|c3H5 MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMV|E4PFRiY3XscJMh[nliTWTTJIF{e2G7LDDJR|UxRTBwNEZOwG0> NEPNUmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{CzOFE{PSd-MUewN|QyOzV:L3G+
rat neuronal cells MmW2R5l1d3SxeHnjbZR6KGG|c3H5 NYftTZF{OTBidV2= MV6yOEBpenN? NX[5[4E4S3m2b4TvfIlkcXS7IHHnZYlve3RicnH0JI5mfXKxbnHsJINmdGy|IHH0JFExKHWPIHHmeIVzKDJ2IHjydy=> NGn3VYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{K3OlY4QSd-MUeyO|Y3Pzl:L3G+
P19 M{e5bWN6fG:2b4jpZ4l1gSCjc4PhfS=> Mlz0NVghcHK| MnfsR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFE6KGOnbHzzJIFnfGW{IEG4JIhzeyxiSVO1NF0xNjIQvF2= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR2MkW2OUc,OTd2NEK1OlU9N2F-
MCF7 MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mk\6S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjDkZZl{KGK7IGPSRkBie3OjeTygS2k2OD1|NT62{txO NXXBN5hxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe4OlkxQThpPkG3PFY6ODl6PD;hQi=>
HCT116 NF7Ed3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnPuS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{NCCJSUWwQVAvODJzzszN M{\4V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkSzO|A{Lz5zOEK0N|cxOzxxYU6=
DLD1 MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDEUGQyKGOnbHzzMEBIUTVyPUCuNFM4|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ2M{ewN{c,OTh{NEO3NFM9N2F-
KPL4 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDLVGw1KGOnbHzzMEBIUTVyPUCuNFU6|ryP MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ2M{ewN{c,OTh{NEO3NFM9N2F-
A549 MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX\Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDBOVQ6KGOnbHzzMEBIUTVyPUCuNFY1|ryP MmXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{NEO3NFMoRjF6MkSzO|A{RC:jPh?=
KPL4 MUHGeY5kfGmxbjDhd5NigQ>? MX[0NEBpenN? M{\hOmlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hU1CONDDj[YxteyCjc4Pld5Nm\CCjczDk[ZBt\XSrb36gc4YhTXKkQkKgcIV3\WxiYX\0[ZIhPDBiaILzMEBOTUN;MD6xNe69VQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ2M{ewN{c,OTh{NEO3NFM9N2F-
KPL4 MnrESpVv[3Srb36gZZN{[Xl? NHjIW2U1OCCqcoO= NIDY[ppKdmirYnn0bY9vKG:oIFjzdFkxKGmwIHj1cYFvKEuSTESgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVxdGW2aX;uJI9nKFKjZj2xJIxmfmWuIHHmeIVzKDRyIHjyd{whVUWFPUCuN|PPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ2M{ewN{c,OTh{NEO3NFM9N2F-
Jurkat NU\OW4VKTnWwY4Tpc44h[XO|YYm= MW[xJJVO M1vpU2lvcGmkaYTpc44hd2ZidH:gTHNRQTBiaX6gSmFFTCCmZX\pZ4lmdnRiaIXtZY4hUnW{a3H0JINmdGy|IHHzd4V{e2WmIHHzJHJKWCCycn;0[YlvKGSnZ4Lh[IF1cW:wIHH0JFEhfU1iYomgW4V{fGW{bjDicI91 NWHL[pVLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0NFg4OTNpPkG4OFA5PzF|PD;hQi=>
HEK293T NUGwWGo4TnWwY4Tpc44h[XO|YYm= M{OxZ2lvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiTl[tb4FxeGGEIHHjeIl3[XSrb36g[ZhxemW|c3XkJIlvKEiHS{K5N3Qh[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 NEDwU2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOESwPFcyOyd-MUi0NFg4OTN:L3G+
Jurkat M2LwbWZ2dmO2aX;uJIF{e2G7 M4fpRWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiTl[tb4FxeGGEIHHjeIl3[XSrb36g[ZhxemW|c3XkJIlvKE[DRFSg[IVncWOrZX70JIh2dWGwIFr1dotifCClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDRyOEexN{c,OTh2MEi3NVM9N2F-
SKBR3 M{HabGZ2dmO2aX;uJIF{e2G7 NX7Fd4x7OjRiaILz NFHQVohKdmirYnn0bY9vKG:oIFjzdFkxNW2nZHnheIVlKEiHUkKg[IVoemGmYYTpc44hcW5iaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdB?= NIDwSoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEixOlEyOSd-MUi4NVYyOTF:L3G+
SKBR3 NWO3TFhZTnWwY4Tpc44h[XO|YYm= MWSyOEBpenN? MoDvTY5pcWKrdHnvckBw\iCKc4C5NE1u\WSrYYTl[EBT[WZiZHXndoFl[XSrb36gbY4hcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfA>? NHzJfpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEixOlEyOSd-MUi4NVYyOTF:L3G+
HuH7 MV3BcpRqfmm{YXygZZN{[Xl? NWfob2xqOyCmYYnz M4nz[WFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJIdmdm:2eYDlJFFjKEOxbkGgbY5n\WO2ZXSgbY4hcHWvYX6gTJVJPyClZXzsd{Bie3Onc4Pl[EBieyCJQWDETEBTVkFib4KgNVhUKHKUTlGgcIV3\WxiYX\0[ZIhOyCmYYnzJIJ6KHGUVD3QR3Ih[W6jbInzbZMtKEWFNUC9NE4xODB{Nd88US=> M4XnelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUO2NVkyLz5zOEmzOlE6OTxxYU6=
HuH7 MUPBcpRqfmm{YXygZZN{[Xl? NHLHPVI{KGSjeYO= M2Tq[WFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJIdmdm:2eYDlJFFjKEOxbkGgbY5n\WO2ZXSgbY4hcHWvYX6gTJVJPyClZXzsd{Bie3Onc4Pl[EBieyCJQWDETEBTVkFib4KgNVhUKHKUTlGgcIV3\WxiYX\0[ZIhOyCmYYnzJJNmdGWldHXkJJdqfGhiNECgcm0hUEOYLUe5OkBidmRiOECwJI5OKGKxY3XwdoV3cXJiYomgdXJVNVCFUjDhcoFtgXOrczygSWM2OD1yLkCwNVLPxE1? M{Lpd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUO2NVkyLz5zOEmzOlE6OTxxYU6=
SH-SY5Y MkS1UoV2em:ycn;0[YN1cW:wIHHzd4F6 NGX1XHBP\XW{b4Dyc5Rm[3Srb36gZYdicW6|dDDi[ZRiNWGveXzvbYQheGWydHnk[UAyNTR{LXnu[JVk\WRidH;4bYNqfHliaX6gbJVu[W5iU1itV3k2YSClZXzsd{Bie3Onc4Pl[EBieyCuYXP0ZZRmKGSnaInkdo9o\W6jc3WgdoVt\WG|ZTygSWM2OD1yLkC0NlY6|ryP MlfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzM{i4OVkoRjF7MUO4PFU6RC:jPh?=
SH-SY5Y NEHZW2dP\XW{b4Dyc5Rm[3Srb36gZZN{[Xl? MnHBNVAhdk1? MlPMUoV2em:ycn;0[YN1cW:wIHHnZYlve3RiYnX0ZU1idXmub3nkJJBmeHSrZHWgNU01Oi2rbnT1Z4VlKHSxeHnjbZR6KGmwIILleIlvd2mlIHHjbYQu\GmoZnXy[Y51cWG2ZXSgbJVu[W5iU1itV3k2YSClZXzsd{Bie3Onc4Pl[EBieyCuYXP0ZZRmKGSnaInkdo9o\W6jc3WgdoVt\WG|ZTDheEAyOCCwTR?= NV7Wd2VjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxN|g5PTlpPkG5NVM5QDV7PD;hQi=>
SKBR3 NHjjfXFEgXSxdH;4bYNqfHliYYPzZZk> MWS3NkBpenN? MnHPR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9iYYPzZZktKEmFNUC9NE4xPDIQvF2= M4\aU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NEC1OVI5Lz5zOUSwOVUzQDxxYU6=
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NCI-H1975 NGPXdJRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NH7wVHkyKHSxIEOg[IF6ew>? MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHfl[ol1cW6rYj3y[ZNqe3SjboSgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGGodHXyJFEhfG9iMzDkZZl{KGK7IF3UV{Bie3OjeTygS2k2OD1yLkW2{txO M4L0NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{izPVc4Lz5{N{e4N|k4PzxxYU6=
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A549 MWjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NFi0R3E4OiCqcoO= NHTvfYZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OD1yLkJOwG0> M3rYWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyNFg2Lz5{OUG3NlA5PTxxYU6=
NCI-H1975 MYXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVzTemNXPzJiaILz NWjBTW5oSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHygWIl1\XJiOU[gRZF2\W:3czDPcoUhW2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG|c3H5MEBIUTVyPUCuOVbPxE1? M4DWcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkCyOFAzLz5{OUKwNlQxOjxxYU6=
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In vivo Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6]

Protocol (from reference)

Kinase Assay:

[1]

  • Isothermal Titration Calorimetry (ITC) of Nucelotide Binding:

    The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.

Cell Research:

[2]

  • Cell lines: A2780 human ovarian cell line
  • Concentrations: 0.001-10 μM
  • Incubation Time: 3 hours
  • Method:

    Exponentially growing cells are treated with Geldanamycin and at various times DNA synthesis is assessed by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, cells are incubated with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Cells are stained for 30 minutes at room temperature with propidium iodide and analysed by flow cytometry using a Coulter EPICS Profile Analyzer.

  • (Only for Reference)
Animal Research:

[6]

  • Animal Models: FRE/erbB-2 tumors in nu/nu mice
  • Dosages: 50 mg/kg
  • Administration: Administered via i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 36 mg/mL warmed
(64.21 mM)
Water Insoluble
Ethanol Insoluble

* 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 560.64
Formula

C29H40N2O9

CAS No. 30562-34-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)C)OC)OC(=O)N)C)C)O)OC

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

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00003969 Completed Drug: tanespimycin Unspecified Adult Solid Tumor Protocol Specific Cancer Research UK|National Cancer Institute (NCI) August 1998 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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