Ganetespib (STA-9090) 化学構造
分子量: 364.4

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Quality Control & MSDS

製品説明

  • Compare HSP (e.g. HSP90) Inhibitors
    HSP (e.g. HSP90)製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 Ganetespib (STA-9090)は独特な triazolone-containing Hsp90阻害剤、 IC50 が4 nM となる.
ターゲット HSP90
IC50 4 nM [1]
In vitro試験 The 50% inhibitory concentrations (IC50) for Ganetespib against malignant mast cell lines are 10-50 times lower than that for 17-AAG, indicating that triazolone class of HSP90 inhibitors likely exhibits greater potency than geldanamycin based inhibitors. [1] Ganetespib inhibits MG63 cell lines with IC50 of 43 nM. [1] Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and serves as a potent Hsp90 inhibitor by causing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 and c-Met as well as Wilms' tumor 1. [2] Ganetespib, at low nanomolar concentrations, potently arrests cell proliferation and induces apoptosis in a wide variety of human cancer cell lines, including many receptor tyrosine kinase inhibitor- and tanespimycin-resistant cell lines. Ganetespib exhibits potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those that express mutated kinases that confer resistance to small-molecule tyrosine kinase inhibitors. [3] Ganetespib treatment rapidly caused the degradation of known Hsp90 client proteins, exhibits superior potency to the ansamycin inhibitor 17-AAG, and shows sustained activity even with short exposure times.[3] In anohter study, Ganetespib induces apoptosis of malignant canine mast cell lines. Ganetespib is active at significantly lower concentrations for C2 and BR canine malignant mast cells with IC50 of 19 and 4 nM, respectively, while 17-AAG inhibits C2 and BR canine malignant mast cells with IC50 of 958 and 44 nM, respectively. [4] Both the expression of WT and mutant Kit are downregulated by 100 nM Ganetespib after 24 hours in all lines treated including C2 and BMCMCs cells. However, no effects on PI3K or HSP90 expression are observed following treatment with Ganetespib.[4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HL60 M2fLOmFxd3C2b4Ppd{BCe3OjeR?= NYHpVIVNOzBxOECvNVUxNzJ3MDDuUS=> NIT1b2QzPC92OD:3NkBp MmDIbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz M4jpSFI2QDh{NUWw
MV411 MmfyRZBweHSxc3nzJGF{e2G7 NGDIUpE{OC96MD:xOVAwOjVyIH7N NEHDbVQzPC92OD:3NkBp M37nO4lv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> MUCyOVg5OjV3MB?=
MGC-803 Mnr3R4VtdCCYaXHibYxqfHliQYPzZZk> NWC2bZJWOC5zLUGwNFAhdk1? NHn3fms4OiCq Moe4bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NXr2W3ZYOjV3OUC4NFU>
SGC-7901 NGnkNGZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUKwMlEuOTByMDDuUS=> NHzzepg4OiCq MYXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NEfaZZQzPTV7MEiwOS=>
MKN-28 MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn\tNE4yNTFyMECgcm0> NWjQc|VnPzJiaB?= NXvhRnF[cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXXF[29JOjV3OUC4NFU>
MGC-803 MYfGeY5kfGmxbjDBd5NigQ>? M4r0R|AvOS1zMECwJI5O M2nwOFI1KGh? NHnxR|NqdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? MWOyOVU6ODhyNR?=
HCT-116 NF3BNIFHfW6ldHnvckBCe3OjeR?= NEDVWFU2OG6P MXuyOEBp NUnPVGNXTE2VTx?= MmDVbY5lfWOnZDDHNE9IOSCjcoLld5Q> MkjNNlUzOTB5OUS=
HT-29 NVPpO4JCTnWwY4Tpc44hSXO|YYm= NFTSOog2OG6P NHjnR3YzPCCq M3nCWGROW09? MlfKbY5lfWOnZDDHNE9IOSCjcoLld5Q> MoO1NlUzOTB5OUS=
SCC25 NH7mWmJEgXSxeHnjbZR6KEG|c3H5 M4PLdlExNzVyIH7N NYHLeVBYOjRiaB?= NYi5fXNV\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M4rJT|I2OjB3NEOw
FUDA M37yZ2N6fG:6aXPpeJkhSXO|YYm= NFTi[oYyOC93MDDuUS=> M2LUPVI1KGh? Mnq0[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NWTDSlA{OjV{MEW0N|A>
Detroit562 NFXF[HBEgXSxeHnjbZR6KEG|c3H5 M1[yd|ExNzVyIH7N NF7aUpQzPCCq NEHaVVNl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MYGyOVIxPTR|MB?=
CAL27 MlPQR5l1d3irY3n0fUBCe3OjeR?= Mm\JNVAwPTBibl2= MnP6NlQhcA>? NW\2OWJv\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NF7OdYMzPTJyNUSzNC=>
DSH1 M3rId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HWU2lEPTB;NjDuUS=> MUSyOFc5PDh|OR?=
SW-1710 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXLTWM2OD14IH7N MmDBNlQ4QDR6M{m=
T24 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTdibl2= M{TjXVI1Pzh2OEO5
RT112 NIrrXZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TyUmlEPTB;OTDuUS=> M36zXVI1Pzh2OEO5
639-V NHXwWWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HTSWlEPTB;MUCgcm0> NYD4dmI6OjR5OES4N|k>
SCaBER M3vaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTOTWM2OD1zMDDuUS=> MW[yOFc5PDh|OR?=
BFTC Mlj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHpdpd{UUN3ME2xO{BvVQ>? NI\kV2gzPDd6NEizPS=>
J82 MmLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[zcm1HUUN3ME2xPEBvVQ>? NWDBUG9oOjR5OES4N|k>
HT-1376 NVHkfXE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJzIH7N M1XpNFI1Pzh2OEO5
647-V M1\ZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDOOGxKSzVyPUK3JI5O Mon1NlQ4QDR6M{m=
UM-UC3 Moq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTN|IH7N NHXyPYMzPDd6NEizPS=>
LB831-BLC NETlO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XJOWlEPTB;M{Sgcm0> MYqyOFc5PDh|OR?=
KU-19-19 NF\l[GRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrJUpBiUUN3ME2zOkBvVQ>? MmLMNlQ4QDR6M{m=
35612 NXzUNGhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTN6IH7N NWC2fXo6OjR5OES4N|k>
5637 Mo[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LoOmlEPTB;NESgcm0> MmrqNlQ4QDR6M{m=
HT-1197 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\SbmlEPTB;NUOgcm0> MmfsNlQ4QDR6M{m=
MGH-U3 NW\KNpY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TyeWlEPTB;NUOgcm0> MUeyOFc5PDh|OR?=
TCCSUP M1zWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfmcVVzUUN3ME2xOFIhdk1? M2[5U|I1Pzh2OEO5
RT4 NFKxVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkS5TWM2OD1zN{OzJI5O NVPCWY1POjR5OES4N|k>
SW780 NGnhZ|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfvSFBKSzVyPUO0OVEhdk1? MVGyOFc5PDh|OR?=
RKO NH\We2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3m2UWlEPTB;NDDuUS=> M3G1TVI1Pjh{N{S3
LS-411 N NELVRmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPxTVJzUUN3ME21JI5O MYmyOFY5Ojd2Nx?=
SW620 MlvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnzTWM2OD16IH7N NW\MR3E3OjR4OEK3OFc>
HCT-15 M{\DOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XZfWlEPTB;ODDuUS=> MYKyOFY5Ojd2Nx?=
HuTu-80 NIXCU4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rMd2lEPTB;MUOgcm0> MkDjNlQ3QDJ5NEe=
HCT 116 M324TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PNeGlEPTB;MUSgcm0> NGLoT5kzPDZ6Mke0Oy=>
COLO-205 NYLmcnlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLHTWM2OD1zNDDuUS=> MkTSNlQ3QDJ5NEe=
NCI-H747 M3XVbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nzS2lEPTB;MUegcm0> MkK4NlQ3QDJ5NEe=
COLO-678 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOyNJVKSzVyPUKxJI5O MXmyOFY5Ojd2Nx?=
LoVo M4rCTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPsbodKSzVyPUKyJI5O M4ixZ|I1Pjh{N{S3
LS-1034 NXvr[YxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XpfGlEPTB;M{Ggcm0> MmDENlQ3QDJ5NEe=
SNU-C2B M4TZbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXjRllvUUN3ME20OUBvVQ>? NF;TTGIzPDZ6Mke0Oy=>
LS-123 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXsRo9xUUN3ME23N{BvVQ>? MnTSNlQ3QDJ5NEe=
SK-CO-1 NXHub2FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\uNpZKSzVyPUixJI5O MYqyOFY5Ojd2Nx?=
HCC2998 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Dob2lEPTB;MUK4JI5O MnO1NlQ3QDJ5NEe=
MDA-MB-231 NUCwe4R6TnWwY4Tpc44hSXO|YYm= MkHyNVAxKG6P MkTyN|AhdWmw NHexRmZqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NYKyTYU2OjR{NEiyOlU>
MDA-MB-435 NH70eVlHfW6ldHnvckBCe3OjeR?= M2HHS|ExOCCwTR?= MV:zNEBucW5? NX7PSYRPcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MXGyOFI1QDJ4NR?=
BT-20  MWPGeY5kfGmxbjDBd5NigQ>? NUfpe2Z1OTByL{K1NEBvVQ>? Mlv5NlQhcA>? M{HpPZJme3WudHXkJIlvKGFiZH;z[U1l\XCnbnTlcpQh\GW|dHHibYxqgmG2aX;uJI9nKEWJRmKsJGlITi2LUjygUWVVNCCjbnSgR3JCTg>? Mom4NlQyPzN3NEG=
MDA-MB-231 NV;iVotqTnWwY4Tpc44hSXO|YYm= MkOyNVAxKG6P NXzJbm9oOjRiaB?= MmfNbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> MWKyOFE4OzV2MR?=
H82 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXxe|c3UUN3ME2zNE4zPyCwTR?= NEPSNXMzPDF4NkWwOS=>
GLC4 M3PvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[4TWM2OD1{MD60O{BvVQ>? NU\ucXM{OjRzNk[1NFU>
H69 M1zwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLZbW81UUN3ME24N{4{PiCwTR?= NVnHbXR[OjRzNk[1NFU>
H128 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLwTWM2OD14OT61OUBvVQ>? NYKwb4VpOjRzNk[1NFU>
H146 MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ6LkWxJI5O NH\od2UzPDF4NkWwOS=>
H187 NHPL[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\kdmRKSzVyPUK0Mlk6KG6P M1HBVlI1OTZ4NUC1
H526 NX73fJp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfseJZbUUN3ME2yNU43PCCwTR?= NFTLPIYzPDF4NkWwOS=>
N592 NIDU[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\rTmlEPTB;MUSuNVIhdk1? NVrMbFlkOjRzNk[1NFU>
H620 M3LWVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHJfHFRUUN3ME2zNk43PyCwTR?= MkjlNlQyPjZ3MEW=
H792 NUKx[FF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTR3LkC3JI5O M{jMPVI1OTZ4NUC1
H1173 NY\oeWN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzHTWM2OD1zMj62NkBvVQ>? MYiyOFE3PjVyNR?=
AC3 Mlf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TP[mlEPTB;MkWuPUBvVQ>? MUmyOFE3PjVyNR?=
H82 MoL0SpVv[3Srb36gRZN{[Xl? M2fzO|MxKG6P MnHQO|IhcA>? MU\pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= Mor1NlQyPjZ3MEW=
GLC4 MXfGeY5kfGmxbjDBd5NigQ>? M3nHN|MxKG6P NInRcFA4OiCq NVm3OHFucW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NFHaUHUzPDF4NkWwOS=>
H146  MoT3SpVv[3Srb36gRZN{[Xl? NXnCR3p4OzBibl2= Mn[xO|IhcA>? MWTpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NV7WVnpHOjRzNk[1NFU>
OVCAR-5 NH\ESYZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{jiTFAuOTByMDDuUS=> NVvFfJk3PzJiaB?= NF\O[ZdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NF3vNYgzOzlyMEGzOi=>
OVCAR-8 M1zkOWNmdGxiVnnhZoltcXS7IFHzd4F6 M{DTXVAuOTByMDDuUS=> NWThSXNJPzJiaB?= MVzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NH\n[oszOzlyMEGzOi=>
A1847 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUPhZWpVOC1zMECwJI5O M3rHelczKGh? NIfXepZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2L3bVI{QTByMUO2
SKOV-3 NVLYS|J1S2WubDDWbYFjcWyrdImgRZN{[Xl? M4XCT|AuOTByMDDuUS=> M2jWUlczKGh? MVnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFXWcIczOzlyMEGzOi=>
OVCAR-5 MVvBdI9xfG:|aYOgRZN{[Xl? MVmxNE0yODBibl2= Mlv0NlQwPDhxN{KgbC=> MXLpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MlzsNlM6ODBzM{[=
OVCAR-8 NYTmR5YySXCxcITvd4l{KEG|c3H5 MVuxNE0yODBibl2= M{fPNVI1NzR6L{eyJIg> MVPpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 NVzycY9nOjN7MECxN|Y>
A1847 NEHmW5JCeG:ydH;zbZMhSXO|YYm= MXGxNE0yODBibl2= NFH2cnczPC92OD:3NkBp NIDqbYJqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NYfT[mJ[OjN7MECxN|Y>
H2228 MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGLtd5QxNTFyMECgcm0> M2[5W|czKGh? MnLOTWM2OD1zMzDuUS=> NYPEcXV5OjN3M{OyOlU>
H3122 MmPYR4VtdCCYaXHibYxqfHliQYPzZZk> M2\VeFAuOTByMDDuUS=> Mln3O|IhcA>? MVHJR|UxRTFyIH7N MWmyN|U{OzJ4NR?=
K008 MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mli4TWM2OD14MDDuUS=> MnP0NlM1OTh3MkO=
K028 MlvMR4VtdCCYaXHibYxqfHliQYPzZZk> Mle1TWM2OD16NDDuUS=> NGL6WnozOzRzOEWyNy=>
K029 NIfJZlVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NH3FcG5KSzVyPUS2JI5O MorHNlM1OTh3MkO=
M23 M1XHOWNmdGxiVnnhZoltcXS7IFHzd4F6 MY\JR|UxRTN5LkWgcm0> NGfseZMzOzRzOEWyNy=>
K033 NGHnOolE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnL3TWM2OD15NT61JI5O MUKyN|QyQDV{Mx?=
K008 NET2epFHfW6ldHnvckBCe3OjeR?= NWXGUphQOjVyIH7N MXyyOEBp MX3pcoR2[2W|IFeyJIFzemW|dB?= NWjQ[|NCOjN2MUi1NlM>
K028 NWjBTVZ2TnWwY4Tpc44hSXO|YYm= NGXxZlIzPTBibl2= M2DrclI1KGh? M2D1[Ylv\HWlZYOgS|Ih[XK{ZYP0 NXzROplIOjN2MUi1NlM>
K029 M1HGVWZ2dmO2aX;uJGF{e2G7 MXeyOVAhdk1? MUWyOEBp NV;JdlJrcW6mdXPld{BIOSCjcoLld5Q> NELkVFUzOzRzOEWyNy=>
M23 MnLpSpVv[3Srb36gRZN{[Xl? MXGyOVAhdk1? M37YVVI1KGh? M1f6XYlv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0 Mkm4NlM1OTh3MkO=
K033 M1;PdWZ2dmO2aX;uJGF{e2G7 MlHsNlUxKG6P NXjSN5dWOjRiaB?= M2X5Solv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= Mn;WNlM1OTh3MkO=
K008 NXvoSVVZSXCxcITvd4l{KEG|c3H5 NEDuNIUyODBibl2= MkexO|IhcA>? MUjzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MmDKNlM1OTh3MkO=
K028 Moi1RZBweHSxc3nzJGF{e2G7 NIrRSVMyODBibl2= MkX0O|IhcA>? MYXzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MVOyN|QyQDV{Mx?=
K029 M2H3V2Fxd3C2b4Ppd{BCe3OjeR?= M3nYPFExOCCwTR?= MVm3NkBp NFrSNWx{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NGfHUZAzOzRzOEWyNy=>
M23 NXvZ[Wd1SXCxcITvd4l{KEG|c3H5 Mon0NVAxKG6P MWW3NkBp NFPWdmN{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| M3;hS|I{PDF6NUKz
K033 M{jUe2Fxd3C2b4Ppd{BCe3OjeR?= MVWxNFAhdk1? Mk\BO|IhcA>? M3vHTJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M2XaeVI{PDF6NUKz
RD MnnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3McFdKUUN3ME24JI5O NYC1fIFGOjN|MEO3OFE>
Rh41 NVHWWFhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rGS2lEPTB;MUCuOEBvVQ>? NFXtXFMzOzNyM{e0NS=>
Rh18 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvrVIxKSzVyPU[uNkBvVQ>? MkfyNlM{ODN5NEG=
Rh30 NXnPcFJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXtc4xKSzVyPUWuOkBvVQ>? NIDYTIIzOzNyM{e0NS=>
BT-12 MnKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3RUI1KSzVyPUG0MlMhdk1? MlnBNlM{ODN5NEG=
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COR-L23 NELR[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\5VWdKSzVyPUKyJI5O MX[yN|AyOjJ2OB?=
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H1734 NEHGUGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTQZXg1UUN3ME2yPEBvVQ>? MnS0NlMxOTJ{NEi=
H358 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLTZ|gyUUN3ME2yPUBvVQ>? M2fmWVI{ODF{MkS4
A549 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTR|IH7N MXWyN|AyOjJ2OB?=
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Calu-1 M4rISWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFntb2tKSzVyPUW4JI5O MnrYNlMxOTJ{NEi=
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... Click to View More Cell Line Experimental Data

In vivo試験 Administration of Ganetespib leads to significant tumor shrinkage in several tumor xenograft models in mice and appears to be less toxic. Furthermore Ganetespib demonstrated better tumor penetration compared with tanespimycin.[2] Ganetespib inhibits in vivo tumor growth in both malignant mast cell and OSA xenograft models. Ganetespib significantly inhibits tumor growth when dosed with two repeating cycles of 25 mg/kg/day for 3 days, with a %T/C value of 18. Ganetespib is well-tolerated, with the vehicle and Ganetespib groups having average bodyweight changes relative to the start of the study of +0.3% and -8.1% on day 17, respectively.[4]
臨床試験 Ganetespib has entered in a phase II clinical trials in the treatment of non small cell lung cancer.
特集

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 OSA cells
濃度 0.001-1μM
反応時間 5 days
実験の流れ A total of 1.5 × 103 OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.

動物実験: [4]

動物モデル Female severe combined immune-deficient (SCID) mice
製剤 In DMSO and diluted 1:10 with 20% Cremophor RH 40
投薬量 25 mg/kg/day for 3 days
投与方法 Tail vein injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Ganetespib (STA-9090) SDF
分子量 364.4
化学式

C20H20N4O3

CAS No. 888216-25-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 40 mg/mL (109.76 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or 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.
化学名 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one

カスタマーフィードバック (2)


Click to enlarge
Rating
Source Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1017. Ganetespib (STA-9090) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231, SKM1, PaTu2, A549, HCT-116 cells
Concentrations 0-1.0 uM
Incubation Time 24 h
Results To investigate whether PRKD2 stability is affected after pharmacologic HSP90 inhibition, eight human cancer cell lines representing six different tumor types (breast cancer, pancreatic cancer, lung cancer, colon cancer, acutemyeloid leukemia, and glioblastoma) were incubated for 24 hours with increasing concentrations of two different compounds: PU-H71, an optimized water soluble member of the purine class of HSP90 inhibitors and STA-9090, a resor-cinol-containing triazole molecule with a novel chemical structure, both unrelated to the geldanamycin class of HSP90 inhibitors. Both inhibitors caused dose-dependent degradation of PRKD2 in all tumor cell lines. STA-9090 was associated with increased apoptosis as revealed by augmented PARP and caspase-9 cleavage in all tumor cell lines.

Click to enlarge
Rating
Source , , Hum Mol Genet, 2015, 10.1093/hmg/ddv136. Ganetespib (STA-9090) purchased from Selleck
Method Western Blot
Cell Lines Pkd1 null MEK cells、Pkd1 mutant PN24 cells
Concentrations 0-200 nM
Incubation Time 0-24 h
Results Treatment with STA9090, a second generation Hsp90 inhibitor that binds to ATP binding domain at the N-terminal of Hsp90, decreased the levels of Brd4 protein in Pkd1 mutant MEK cells and PN24 cells in a dose- and time-dependent manner.

文献中の引用 (5)

技術サポート&よくある質問(FAQ)

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Related HSP (e.g. HSP90) 阻害剤

  • PU-H71

    PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM.

  • KNK437

    KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

  • VER155008

    VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

  • FRAX597

    FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.

  • 17-AAG (Tanespimycin)

    17-AAG (Tanespimycin)は、5nMのIC50による強力な熱ショックタンパク質90(Hsp90)阻害剤です。

    Features:Displays very low toxicity toward normal cells.

  • Luminespib (AUY-922, NVP-AUY922)

    Luminespib (AUY-922, NVP-AUY922)は高度的に HSP90 を抑制、 HSP90α と HSP90β を作用すると、 IC50 がそれぞれ 13 nM 、 21 nM となる。

  • 17-DMAG (Alvespimycin) HCl

    17-DMAG (Alvespimycin) HClは、62nMのIC50による強力なHsp90阻害剤です。

    Features:A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.

  • Geldanamycin

    ノーカット二量体Hsp90またはN末端領域Hsp90と結合している間、Geldanamycinは1.2のμMまたは0.78のμMによるKdによる天然既存のHsp90阻害剤です。

  • HSP990 (NVP-HSP990)

    NVP-HSP990 (HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM.

    Features:NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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