Ganetespib (STA-9090) 化学構造
分子量: 364.4

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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 M3XkUmFxd3C2b4Ppd{BCe3OjeR?= NWe0OZJDOzBxOECvNVUxNzJ3MDDuUS=> NEjwTXgzPC92OD:3NkBp MnHGbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NIXR[5AzPTh6MkW1NC=>
MV411 MXjBdI9xfG:|aYOgRZN{[Xl? NEHE[Hc{OC96MD:xOVAwOjVyIH7N NWXSXnJZOjRxNEivO|IhcA>? MWDpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= M3i2OFI2QDh{NUWw
MGC-803 MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEDU[ocxNjFvMUCwNEBvVQ>? MUi3NkBp M2r0fYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWTKc2RsOjV3OUC4NFU>
SGC-7901 Mlr4R4VtdCCYaXHibYxqfHliQYPzZZk> NE\tOGUxNjFvMUCwNEBvVQ>? M4D1e|czKGh? NH\kb3FqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NXHpUYdGOjV3OUC4NFU>
MKN-28 MmKxR4VtdCCYaXHibYxqfHliQYPzZZk> MVGwMlEuOTByMDDuUS=> M4DhXVczKGh? MnrlbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MVyyOVU6ODhyNR?=
MGC-803 NUezUXp7TnWwY4Tpc44hSXO|YYm= MYSwMlEuOTByMDDuUS=> M2fPU|I1KGh? NULGXJhjcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NYrLbFFiOjV3OUC4NFU>
HCT-116 NIjSbHhHfW6ldHnvckBCe3OjeR?= MmTEOVBvVQ>? NWKyRVE3OjRiaB?= NGfPUJlFVVOR M2LvOolv\HWlZXSgS|AwTzFiYYLy[ZN1 NY\4SZlDOjV{MUC3PVQ>
HT-29 M{XuXmZ2dmO2aX;uJGF{e2G7 NXHw[XV4PTCwTR?= MnP6NlQhcA>? NEixUWhFVVOR MVjpcoR2[2WmIFewM2cyKGG{cnXzeC=> M{nGPVI2OjFyN{m0
SCC25 NFTmWYFEgXSxeHnjbZR6KEG|c3H5 NEfBRXoyOC93MDDuUS=> NW[1U5B{OjRiaB?= MVjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MWGyOVIxPTR|MB?=
FUDA M1zYS2N6fG:6aXPpeJkhSXO|YYm= NUfteVg3OTBxNUCgcm0> M4HKV|I1KGh? MUDk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M4rTNFI2OjB3NEOw
Detroit562 NVLF[FdqS3m2b4jpZ4l1gSCDc4PhfS=> M4XWNFExNzVyIH7N NXH1b2tyOjRiaB?= MUnk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NXf1[nZ[OjV{MEW0N|A>
CAL27 NUjB[IZ6S3m2b4jpZ4l1gSCDc4PhfS=> NHq0dWYyOC93MDDuUS=> NH[4XoQzPCCq NYnwN|JX\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MmjNNlUzODV2M{C=
DSH1 NYHtcotXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTZibl2= NVv3N|F{OjR5OES4N|k>
SW-1710 MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjXcFBKSzVyPU[gcm0> MWiyOFc5PDh|OR?=
T24 M2nsTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfaXGFYUUN3ME23JI5O NHH1cYMzPDd6NEizPS=>
RT112 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7xTmRKUUN3ME25JI5O NFPoWmIzPDd6NEizPS=>
639-V M{X3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7YcXNDUUN3ME2xNEBvVQ>? NH;PTFgzPDd6NEizPS=>
SCaBER NIfjOFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTDTWM2OD1zMDDuUS=> NFHXNWIzPDd6NEizPS=>
BFTC NHnMdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfYeHBKSzVyPUG3JI5O NEL0fFYzPDd6NEizPS=>
J82 MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPrSo9KSzVyPUG4JI5O MmftNlQ4QDR6M{m=
HT-1376 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\GbopKSzVyPUKxJI5O NYfjT4RpOjR5OES4N|k>
647-V MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVviXFVvUUN3ME2yO{BvVQ>? NFXTeXkzPDd6NEizPS=>
UM-UC3 MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DPPGlEPTB;M{Ogcm0> M4\r[lI1Pzh2OEO5
LB831-BLC M1vkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LIbGlEPTB;M{Sgcm0> Mk\QNlQ4QDR6M{m=
KU-19-19 MoTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\xTWM2OD1|NjDuUS=> NFfTW|IzPDd6NEizPS=>
35612 M4SzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrWb3NKSzVyPUO4JI5O MXOyOFc5PDh|OR?=
5637 NHzZcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vo[GlEPTB;NESgcm0> Mo\qNlQ4QDR6M{m=
HT-1197 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP5[mJKSzVyPUWzJI5O NWDEc4pJOjR5OES4N|k>
MGH-U3 M3;1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf1VXd[UUN3ME21N{BvVQ>? MU[yOFc5PDh|OR?=
TCCSUP M1:0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTF2MjDuUS=> NInzTXozPDd6NEizPS=>
RT4 NIDDVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT4dWxMUUN3ME2xO|M{KG6P MmXLNlQ4QDR6M{m=
SW780 Mki4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq2SopKSzVyPUO0OVEhdk1? NFHCRZMzPDd6NEizPS=>
RKO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlGzTWM2OD12IH7N M2LYcFI1Pjh{N{S3
LS-411 N MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3veXU4UUN3ME21JI5O Mk\KNlQ3QDJ5NEe=
SW620 M{fhW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPBflVKSzVyPUigcm0> M2fwOlI1Pjh{N{S3
HCT-15 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLYcW1KSzVyPUigcm0> NHfYSokzPDZ6Mke0Oy=>
HuTu-80 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF|IH7N NFzUU48zPDZ6Mke0Oy=>
HCT 116 NG\ufnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\ZcJJ{UUN3ME2xOEBvVQ>? M3nDclI1Pjh{N{S3
COLO-205 NIWzZWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDBcIJKSzVyPUG0JI5O NGTSZlQzPDZ6Mke0Oy=>
NCI-H747 NYTxcJc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoqwTWM2OD1zNzDuUS=> MoLoNlQ3QDJ5NEe=
COLO-678 M4jDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrTTWM2OD1{MTDuUS=> NGfhXmYzPDZ6Mke0Oy=>
LoVo NHGydpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW4TWM2OD1{MjDuUS=> NGD5fo8zPDZ6Mke0Oy=>
LS-1034 M1\OWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTNzIH7N MVOyOFY5Ojd2Nx?=
SNU-C2B MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTR3IH7N M{PuflI1Pjh{N{S3
LS-123 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\QcGlEPTB;N{Ogcm0> NW\TTlFkOjR4OEK3OFc>
SK-CO-1 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\te2lEPTB;OEGgcm0> MVqyOFY5Ojd2Nx?=
HCC2998 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEn6TIhKSzVyPUGyPEBvVQ>? NWXPdpN2OjR4OEK3OFc>
MDA-MB-231 MofRSpVv[3Srb36gRZN{[Xl? NGTwPXQyODBibl2= Mn3SN|AhdWmw M2jaWYlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MYKyOFI1QDJ4NR?=
MDA-MB-435 MVrGeY5kfGmxbjDBd5NigQ>? MWWxNFAhdk1? MWSzNEBucW5? NVr6bnp[cW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MmTaNlQzPDh{NkW=
BT-20  NXPKeW1LTnWwY4Tpc44hSXO|YYm= Mn;wNVAxNzJ3MDDuUS=> M3njOVI1KGh? Mmq3doV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH M{jPNFI1OTd|NUSx
MDA-MB-231 NIrjPZRHfW6ldHnvckBCe3OjeR?= MnnONVAxKG6P NG\xVVQzPCCq MkfLbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> MUCyOFE4OzV2MR?=
H82 Mmr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;3[3JjUUN3ME2zNE4zPyCwTR?= M1LablI1OTZ4NUC1
GLC4 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXYZ3BYUUN3ME2yNE41PyCwTR?= MlXpNlQyPjZ3MEW=
H69 M{SzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrqO2lmUUN3ME24N{4{PiCwTR?= NETvfVIzPDF4NkWwOS=>
H128 NW\iOJJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\2OGlEPTB;NkmuOVUhdk1? NX7oWVR[OjRzNk[1NFU>
H146 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjoNVNGUUN3ME2yPE42OSCwTR?= NH;5S4wzPDF4NkWwOS=>
H187 NX\wVnVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K2ZmlEPTB;MkSuPVkhdk1? MnjONlQyPjZ3MEW=
H526 NGXNOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\UVY5KSzVyPUKxMlY1KG6P M4fZe|I1OTZ4NUC1
N592 NE\ibG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTF2LkGyJI5O M4DlWFI1OTZ4NUC1
H620 NX7ufWlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHZbWhvUUN3ME2zNk43PyCwTR?= MnOzNlQyPjZ3MEW=
H792 M3n2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\GTWM2OD12NT6wO{BvVQ>? NULlXYd4OjRzNk[1NFU>
H1173 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITNeJhKSzVyPUGyMlYzKG6P MljWNlQyPjZ3MEW=
AC3 NWO5e4Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHC[|ZSUUN3ME2yOU46KG6P NWP2SHR[OjRzNk[1NFU>
H82 MWLGeY5kfGmxbjDBd5NigQ>? MVizNEBvVQ>? MUO3NkBp NFq0bZdqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MViyOFE3PjVyNR?=
GLC4 NVXjfHBuTnWwY4Tpc44hSXO|YYm= NWC3WWNbOzBibl2= MVW3NkBp MV;pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= MUWyOFE3PjVyNR?=
H146  NGrVdY1HfW6ldHnvckBCe3OjeR?= M4TnPFMxKG6P MlnXO|IhcA>? Mm[3bY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NWrKdmV2OjRzNk[1NFU>
OVCAR-5 MmnFR4VtdCCYaXHibYxqfHliQYPzZZk> M1LqO|AuOTByMDDuUS=> MYq3NkBp NX[zRWdQcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmPtNlM6ODBzM{[=
OVCAR-8 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUCwMVExODBibl2= M{m2XFczKGh? MVfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M1;mclI{QTByMUO2
A1847 NXm4WJg6S2WubDDWbYFjcWyrdImgRZN{[Xl? NGPnV|IxNTFyMECgcm0> MWe3NkBp M3y0RYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MlHkNlM6ODBzM{[=
SKOV-3 M4LTdGNmdGxiVnnhZoltcXS7IFHzd4F6 M2T5R|AuOTByMDDuUS=> NELkVWM4OiCq M{joRYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NHX5UFUzOzlyMEGzOi=>
OVCAR-5 NVzmcZNESXCxcITvd4l{KEG|c3H5 M2Hoc|ExNTFyMDDuUS=> M33Pd|I1NzR6L{eyJIg> M2DqT4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= M4jhNFI{QTByMUO2
OVCAR-8 NGXFOIJCeG:ydH;zbZMhSXO|YYm= MYSxNE0yODBibl2= MWmyOE81QC95MjDo Mo\tbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= M3r3W|I{QTByMUO2
A1847 MoXlRZBweHSxc3nzJGF{e2G7 MUCxNE0yODBibl2= M4jDVlI1NzR6L{eyJIg> NGXhUJBqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M3u3OlI{QTByMUO2
H2228 M{jDPWNmdGxiVnnhZoltcXS7IFHzd4F6 MkPHNE0yODByIH7N NHzBPIM4OiCq M3vLU2lEPTB;MUOgcm0> M4nmZ|I{PTN|Mk[1
H3122 NW\DbmF1S2WubDDWbYFjcWyrdImgRZN{[Xl? NYrrcIxQOC1zMECwJI5O MnW1O|IhcA>? NIW5colKSzVyPUGwJI5O MXOyN|U{OzJ4NR?=
K008 MXHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NULBS4lbUUN3ME22NEBvVQ>? MoDaNlM1OTh3MkO=
K028 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnnDTWM2OD16NDDuUS=> MmnWNlM1OTh3MkO=
K029 MmHTR4VtdCCYaXHibYxqfHliQYPzZZk> NUf4e3NsUUN3ME20OkBvVQ>? NF;0XVUzOzRzOEWyNy=>
M23 MkfxR4VtdCCYaXHibYxqfHliQYPzZZk> NFuwToFKSzVyPUO3MlUhdk1? MkHwNlM1OTh3MkO=
K033 NV3VNoo6S2WubDDWbYFjcWyrdImgRZN{[Xl? NV;sVHNbUUN3ME23OU42KG6P NHmxR5QzOzRzOEWyNy=>
K008 M2\DZ2Z2dmO2aX;uJGF{e2G7 MlfkNlUxKG6P M17sS|I1KGh? NIDnc4tqdmS3Y3XzJGczKGG{cnXzeC=> MnvKNlM1OTh3MkO=
K028 NYrZPWhRTnWwY4Tpc44hSXO|YYm= NFL3cpQzPTBibl2= NFHzdpozPCCq M{PqZYlv\HWlZYOgS|Ih[XK{ZYP0 NVLlZYNFOjN2MUi1NlM>
K029 M{XZc2Z2dmO2aX;uJGF{e2G7 M2f5TFI2OCCwTR?= MlG4NlQhcA>? NHnxZXlqdmS3Y3XzJGcyKGG{cnXzeC=> NIrodGgzOzRzOEWyNy=>
M23 MYHGeY5kfGmxbjDBd5NigQ>? MX:yOVAhdk1? M2GwcFI1KGh? Ml[2bY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= M2PpTlI{PDF6NUKz
K033 MXPGeY5kfGmxbjDBd5NigQ>? MmG0NlUxKG6P MX6yOEBp MX;pcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? Mmf6NlM1OTh3MkO=
K008 MljaRZBweHSxc3nzJGF{e2G7 NGTPN|YyODBibl2= NWO0UYN4PzJiaB?= MUXzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NXjEdWR6OjN2MUi1NlM>
K028 M1TjU2Fxd3C2b4Ppd{BCe3OjeR?= MmjINVAxKG6P NHnpUZg4OiCq MWTzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M1jmUlI{PDF6NUKz
K029 Ml2yRZBweHSxc3nzJGF{e2G7 NV7YeWc1OTByIH7N MXK3NkBp MnHNd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MVuyN|QyQDV{Mx?=
M23 Moj0RZBweHSxc3nzJGF{e2G7 MkX6NVAxKG6P MmDlO|IhcA>? NWjkOYJte2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MWCyN|QyQDV{Mx?=
K033 MYrBdI9xfG:|aYOgRZN{[Xl? NIi3[XcyODBibl2= NWHoXmNpPzJiaB?= NXHSOHNxe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MU[yN|QyQDV{Mx?=
RD NXzEO3B[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj5bJRWUUN3ME24JI5O NH\N[mIzOzNyM{e0NS=>
Rh41 M1W0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFyLkSgcm0> NIPlOnQzOzNyM{e0NS=>
Rh18 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PidGlEPTB;Nj6yJI5O MX2yN|MxOzd2MR?=
Rh30 M3f5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTVwNjDuUS=> MWqyN|MxOzd2MR?=
BT-12 Mnr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTF2LkOgcm0> M{HiSVI{OzB|N{Sx
CHLA-266 NUjXOIdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJ5LkGgcm0> NH7jc5AzOzNyM{e0NS=>
TC-71 Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnuTWM2OD12LkWgcm0> MYeyN|MxOzd2MR?=
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CHLA-258 MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G1[2lEPTB;Nj60JI5O MoKzNlM{ODN5NEG=
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NB-EBc1 NHfycGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF4Lkigcm0> MXOyN|MxOzd2MR?=
CHLA-90 Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfnSolrUUN3ME2yNk4{KG6P MUGyN|MxOzd2MR?=
CHLA-136 M3;rXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HLUGlEPTB;MkOuNkBvVQ>? MWiyN|MxOzd2MR?=
NALM-6 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG2So5vUUN3ME2xNU44KG6P M1XPVFI{OzB|N{Sx
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RS4;11 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPHZ3dIUUN3ME2xN{42KG6P M2TseFI{OzB|N{Sx
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CCRF-CEM (1) MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v5V2lEPTB;MUKuOUBvVQ>? NUXScYMxOjN|MEO3OFE>
CCRF-CEM (2) NVLnRmVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTdwMjDuUS=> NXf0O2o1OjN|MEO3OFE>
Kasumi-1 M4D5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zFXWlEPTB;NT64JI5O NF3rfWQzOzNyM{e0NS=>
Karpas-299 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmT6TWM2OD17Lk[gcm0> MWWyN|MxOzd2MR?=
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LNCaP MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TRPWlEPTB;ODDuUS=> MYqyN|E2OjByNB?=
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H1355 NH\2b3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTVibl2= M1nDXlI{ODF{MkS4
H157 MmHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXpXJRKSzVyPUegcm0> NF7sPZQzOzBzMkK0PC=>
H460 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13qfmlEPTB;ODDuUS=> M{D3[lI{ODF{MkS4
IA-LM M{PKdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFyIH7N MnfvNlMxOTJ{NEi=
HOP-62 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFzIH7N M2fBOlI{ODF{MkS4
H23 NXrwbmRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PTW2lEPTB;MUGgcm0> NVXMT3N2OjNyMUKyOFg>
H2030 NUDwOlVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrvSWlPUUN3ME2xNkBvVQ>? NFmy[4IzOzBzMkK0PC=>
H441 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[zTWM2OD1zNDDuUS=> NWrS[JJnOjNyMUKyOFg>
H2212 MoTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjuOoNKSzVyPUG3JI5O M{ThfFI{ODF{MkS4
SK-LU-1 M3jPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3sb4NKSzVyPUG4JI5O NIi4N4kzOzBzMkK0PC=>
H2009 MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF7IH7N NWnKT4hbOjNyMUKyOFg>
H1792 NWDNXnpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJyIH7N M1HoPVI{ODF{MkS4
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H727 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoH1TWM2OD1{ODDuUS=> MYqyN|AyOjJ2OB?=
H1734 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr5TWM2OD1{ODDuUS=> MlzvNlMxOTJ{NEi=
H358 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTPU3VKSzVyPUK5JI5O MlP5NlMxOTJ{NEi=
A549 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT6TW1KSzVyPUSzJI5O MlfzNlMxOTJ{NEi=
H2122 M{D2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPVU3hKSzVyPUWzJI5O MVeyN|AyOjJ2OB?=
Calu-1 NHLnRVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7MfJdKSzVyPUW4JI5O NVXnWpZOOjNyMUKyOFg>
Calu-6 M{LpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\RTWM2OD14NDDuUS=> NFqzU5IzOzBzMkK0PC=>
NCI-H1975 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;mbYE1QCCq M17z[GlEPTB;MU[gcm0> NHPhZnUzOjF2NE[2OS=>
NCI-H1975 M2DKdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHftXGM4OiCq NGDufnRKSzVyPUigcm0> M1\nUlIzOTR2Nk[1

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 40 mg/mL (109.76 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

文献中の引用 (5)

Frequently Asked Questions

  • Question 1
    Does this inhibitor inhibit both isoforms of HSP90?

    Answer: We don't have the information now and it is not very clear in the literature either. From following two references, it indicates that Ganetespib might be specific to the alpha form “Ganetespib binds to the ATP binding site of Hsp90 alpha with a Kd of 110 nM” http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3477583/

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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* 必須

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は1種のパン(pan)- HSP 阻害剤で、誘導HSPsの合成(HSP105、 HSP72,と HSP40を含める)を抑制します。

  • 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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