Ganetespib (STA-9090)

製品コードS1159

Ganetespib (STA-9090)化学構造

分子量(MW):364.4

Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.

サイズ 価格(税別)  
JPY 50132.00
JPY 44820.00
JPY 61420.00

カスタマーフィードバック(3)

  • Loss of viability (Z score) resulting from HSP90 inhibition (HSP90i; ganetespib, 5 nM) in FANCA null GM6914 cells transduced with retroviruses encoding FANCA wild-type (squares; WT) or empty vector control (circles; null) in the presence (black symbols) of MMC (31.6 nM) or DMSO control (gray symbols). Data from three independent experiments are presented as mean ± SEM.

    Cell, 2017, 168(5):856-866. Ganetespib (STA-9090) purchased from Selleck.

    Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.

    Cancer Res 2014 10.1158/0008-5472.CAN-14-1017. Ganetespib (STA-9090) purchased from Selleck.

  • Western blot analysis of the expression of Brd4 and Hsp90 from whole-cell lysates of Pkd1 null MEK cells and Pkd1 mutant PN24 cells treated with STA9090 at indicated concentrations for 24 h (B), and in Pkd1 null MEK cells and Pkd1 mutant PN24 cells treated with STA9090 (200 nM) at indicated time points (C).

    Hum Mol Genet, 2015, 10.1093/hmg/ddv136. Ganetespib (STA-9090) purchased from Selleck.

製品安全説明書

HSP (e.g. HSP90)阻害剤の選択性比較

生物活性

製品説明 Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
ターゲット
HSP90 [1]
(OSA 8 cells)
4 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 Ml7GRZBweHSxc3nzJGF{e2G7 MmD0N|AwQDBxMUWwM|I2OCCwTR?= M4TpdVI1NzR6L{eyJIg> Mm[4bY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz MmrxNlU5QDJ3NUC=
MV411 NEDhR2VCeG:ydH;zbZMhSXO|YYm= MUOzNE85OC9zNUCvNlUxKG6P NIG4bYIzPC92OD:3NkBp NXXzeIVLcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MlnqNlU5QDJ3NUC=
MGC-803 NYj5eJpuS2WubDDWbYFjcWyrdImgRZN{[Xl? MX:wMlEuOTByMDDuUS=> NX3RUGc1PzJiaB?= MXTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NVHOVppyOjV3OUC4NFU>
SGC-7901 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkDENE4yNTFyMECgcm0> NWKxfWhrPzJiaB?= NVz4bJRXcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M{nWSVI2PTlyOEC1
MKN-28 NWH3dI9HS2WubDDWbYFjcWyrdImgRZN{[Xl? M2jaTFAvOS1zMECwJI5O NYnHW28{PzJiaB?= M3nVZYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M2W1[|I2PTlyOEC1
MGC-803 M4HoOGZ2dmO2aX;uJGF{e2G7 MkO2NE4yNTFyMECgcm0> MnLENlQhcA>? NWnWfYtOcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 MlG2NlU2QTB6MEW=
HCT-116 Mn3JSpVv[3Srb36gRZN{[Xl? Mkf1OVBvVQ>? NGDHXoQzPCCq M1rhSmROW09? NUP3eJRRcW6mdXPl[EBIOC:JMTDhdpJme3R? MYiyOVIyODd7NB?=
HT-29 MlHWSpVv[3Srb36gRZN{[Xl? NFW5WYs2OG6P M3;aVVI1KGh? MknDSG1UVw>? M1\zfIlv\HWlZXSgS|AwTzFiYYLy[ZN1 NUHVR5JXOjV{MUC3PVQ>
SCC25 M1PHTGN6fG:6aXPpeJkhSXO|YYm= MXGxNE82OCCwTR?= MlfFNlQhcA>? M3[0[4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MU[yOVIxPTR|MB?=
FUDA M{XyOmN6fG:6aXPpeJkhSXO|YYm= NHW5NYsyOC93MDDuUS=> MV[yOEBp NVfYbIVp\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MVSyOVIxPTR|MB?=
Detroit562 Mn7MR5l1d3irY3n0fUBCe3OjeR?= NXjZdWp6OTBxNUCgcm0> NHnXO4kzPCCq NEjMWGNl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MkLaNlUzODV2M{C=
CAL27 M{Wyb2N6fG:6aXPpeJkhSXO|YYm= M1T3fFExNzVyIH7N NFnkTmYzPCCq NVOyWHRj\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NUG1S|VOOjV{MEW0N|A>
DSH1 M3fJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV76em0xUUN3ME22JI5O MVuyOFc5PDh|OR?=
SW-1710 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HlfGlEPTB;NjDuUS=> NWLZO|FXOjR5OES4N|k>
T24 MoDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nhNWlEPTB;NzDuUS=> NVzRR|M4OjR5OES4N|k>
RT112 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPXTWM2OD17IH7N NGmxdGYzPDd6NEizPS=>
639-V NX\kPZF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;sZodKSzVyPUGwJI5O M3TwTVI1Pzh2OEO5
SCaBER Mnr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2r4cWlEPTB;MUCgcm0> M33ublI1Pzh2OEO5
BFTC M1zCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3hOZlKSzVyPUG3JI5O MVKyOFc5PDh|OR?=
J82 Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTF6IH7N MXGyOFc5PDh|OR?=
HT-1376 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LzTGlEPTB;MkGgcm0> M3XkbFI1Pzh2OEO5
647-V M1\YR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTJ5IH7N NYX3OVJSOjR5OES4N|k>
UM-UC3 NWjD[I5LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYKxdFVNUUN3ME2zN{BvVQ>? MkHENlQ4QDR6M{m=
LB831-BLC MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnMd|hKSzVyPUO0JI5O NFPRbGEzPDd6NEizPS=>
KU-19-19 MmTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN4IH7N M{PzPVI1Pzh2OEO5
35612 M2OzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjoc2puUUN3ME2zPEBvVQ>? M3XJPFI1Pzh2OEO5
5637 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluwTWM2OD12NDDuUS=> M{TNd|I1Pzh2OEO5
HT-1197 NX;0dGxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTV|IH7N NXjGOmx5OjR5OES4N|k>
MGH-U3 NVLCeWc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzRUI5KSzVyPUWzJI5O M{HyT|I1Pzh2OEO5
TCCSUP MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfKZnFGUUN3ME2xOFIhdk1? M2C2bVI1Pzh2OEO5
RT4 NHfKOHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPUblZxUUN3ME2xO|M{KG6P NGHENYczPDd6NEizPS=>
SW780 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTN2NUGgcm0> NFL2ZXozPDd6NEizPS=>
RKO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTRibl2= M4rUc|I1Pjh{N{S3
LS-411 N MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPPTWM2OD13IH7N M1jpcFI1Pjh{N{S3
SW620 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T1WGlEPTB;ODDuUS=> MVSyOFY5Ojd2Nx?=
HCT-15 NF\rVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrrVpJOUUN3ME24JI5O MX2yOFY5Ojd2Nx?=
HuTu-80 NXmxOI9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTHTWM2OD1zMzDuUS=> NYDBNmw{OjR4OEK3OFc>
HCT 116 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfHbFZKSzVyPUG0JI5O MmH4NlQ3QDJ5NEe=
COLO-205 M1TNbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLUTWM2OD1zNDDuUS=> NGflfJIzPDZ6Mke0Oy=>
NCI-H747 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljnTWM2OD1zNzDuUS=> Mn3KNlQ3QDJ5NEe=
COLO-678 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3OcoZsUUN3ME2yNUBvVQ>? MXyyOFY5Ojd2Nx?=
LoVo MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ{IH7N NWDFbGlQOjR4OEK3OFc>
LS-1034 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m2S2lEPTB;M{Ggcm0> M3TWVVI1Pjh{N{S3
SNU-C2B NI\qZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR3IH7N M2DaTlI1Pjh{N{S3
LS-123 M33jV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTd|IH7N NYfaOnJ5OjR4OEK3OFc>
SK-CO-1 NYfRNpBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPWTWM2OD16MTDuUS=> NFn1PFkzPDZ6Mke0Oy=>
HCC2998 NVXMR45vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDkTWM2OD1zMkigcm0> NWHmflVMOjR4OEK3OFc>
MDA-MB-231 MmSwSpVv[3Srb36gRZN{[Xl? Mof6NVAxKG6P MoXFN|AhdWmw MVTpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? M2DmbFI1OjR6Mk[1
MDA-MB-435 NYPRd4VCTnWwY4Tpc44hSXO|YYm= NG\KSVcyODBibl2= M1fkb|MxKG2rbh?= M2PjRolvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MmPBNlQzPDh{NkW=
BT-20  Mkm2SpVv[3Srb36gRZN{[Xl? M2LUdlExOC9{NUCgcm0> MknINlQhcA>? M{D6OZJme3WudHXkJIlvKGFiZH;z[U1l\XCnbnTlcpQh\GW|dHHibYxqgmG2aX;uJI9nKEWJRmKsJGlITi2LUjygUWVVNCCjbnSgR3JCTg>? MXOyOFE4OzV2MR?=
MDA-MB-231 M2LRRWZ2dmO2aX;uJGF{e2G7 NVTBW2xXOTByIH7N M2HFWVI1KGh? MmrTbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> M3ryflI1OTd|NUSx
H82 NFTtOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETpd2xKSzVyPUOwMlI4KG6P NXe1cmh[OjRzNk[1NFU>
GLC4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;YdW1{UUN3ME2yNE41PyCwTR?= MojvNlQyPjZ3MEW=
H69 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1mySWlEPTB;OEOuN|Yhdk1? M{fySVI1OTZ4NUC1
H128 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITo[2FKSzVyPU[5MlU2KG6P MljVNlQyPjZ3MEW=
H146 NGDsWlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ6LkWxJI5O NGPyRZozPDF4NkWwOS=>
H187 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrJTWM2OD1{ND65PUBvVQ>? MV2yOFE3PjVyNR?=
H526 NHH5TXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe0cmJKSzVyPUKxMlY1KG6P M362[VI1OTZ4NUC1
N592 NYfDOoRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPEWWJKSzVyPUG0MlEzKG6P NFX0dFEzPDF4NkWwOS=>
H620 NEj0R25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3jTWM2OD1|Mj62O{BvVQ>? NFnCU|gzPDF4NkWwOS=>
H792 NVHROVQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR3LkC3JI5O MnK0NlQyPjZ3MEW=
H1173 MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrkSlE3UUN3ME2xNk43OiCwTR?= NEjUdoMzPDF4NkWwOS=>
AC3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJ3Lkmgcm0> M3;PT|I1OTZ4NUC1
H82 MmW4SpVv[3Srb36gRZN{[Xl? MXGzNEBvVQ>? MnjJO|IhcA>? NWHTNmhLcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NWPxe3RUOjRzNk[1NFU>
GLC4 Ml;pSpVv[3Srb36gRZN{[Xl? NIW5cWw{OCCwTR?= M{XyXVczKGh? NFXQN3NqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NHfXZ2szPDF4NkWwOS=>
H146  NVy4UoRoTnWwY4Tpc44hSXO|YYm= M{\MUlMxKG6P NHHRVJA4OiCq M3K4[Ylv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M3fqW|I1OTZ4NUC1
OVCAR-5 MlnuR4VtdCCYaXHibYxqfHliQYPzZZk> MVSwMVExODBibl2= M{OwXFczKGh? MoLVbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NELtcIszOzlyMEGzOi=>
OVCAR-8 MWLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2LCNVAuOTByMDDuUS=> M1vYRVczKGh? M3P2eYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{HnPVI{QTByMUO2
A1847 Mn[wR4VtdCCYaXHibYxqfHliQYPzZZk> MkfYNE0yODByIH7N NFL6bpM4OiCq NIPLXolqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NUjCepRJOjN7MECxN|Y>
SKOV-3 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFXPZpQxNTFyMECgcm0> NV;BcmFTPzJiaB?= M2TKW4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MoH0NlM6ODBzM{[=
OVCAR-5 NXnEWXhTSXCxcITvd4l{KEG|c3H5 NYDmXGY5OTBvMUCwJI5O MVWyOE81QC95MjDo NYLYbHZrcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MnK0NlM6ODBzM{[=
OVCAR-8 NFjhc4FCeG:ydH;zbZMhSXO|YYm= M2jYSVExNTFyMDDuUS=> NUHOTW9KOjRxNEivO|IhcA>? NXWxXVJlcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NFywfoozOzlyMEGzOi=>
A1847 MXTBdI9xfG:|aYOgRZN{[Xl? MlX5NVAuOTByIH7N MXSyOE81QC95MjDo NEPEWIZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 Mo\0NlM6ODBzM{[=
H2228 NInCOnlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlXyNE0yODByIH7N MmiyO|IhcA>? M4fCN2lEPTB;MUOgcm0> Mk\rNlM2OzN{NkW=
H3122 M3zDe2NmdGxiVnnhZoltcXS7IFHzd4F6 NEC1d2cxNTFyMECgcm0> NE\pPGI4OiCq NH6wbYZKSzVyPUGwJI5O MVeyN|U{OzJ4NR?=
K008 M1vSb2NmdGxiVnnhZoltcXS7IFHzd4F6 NXrvfoxuUUN3ME22NEBvVQ>? NIT4bJQzOzRzOEWyNy=>
K028 M33EXmNmdGxiVnnhZoltcXS7IFHzd4F6 NU\QW2w2UUN3ME24OEBvVQ>? M{LHUFI{PDF6NUKz
K029 NWLvU4Q4S2WubDDWbYFjcWyrdImgRZN{[Xl? M4\XcWlEPTB;NE[gcm0> MXmyN|QyQDV{Mx?=
M23 M{HHUGNmdGxiVnnhZoltcXS7IFHzd4F6 NF\MfVZKSzVyPUO3MlUhdk1? NUK5SlI{OjN2MUi1NlM>
K033 NWntOZF2S2WubDDWbYFjcWyrdImgRZN{[Xl? NIj3eIZKSzVyPUe1MlUhdk1? M3qyb|I{PDF6NUKz
K008 MljaSpVv[3Srb36gRZN{[Xl? M{CyT|I2OCCwTR?= M3vIW|I1KGh? NYrQUIJncW6mdXPld{BIOiCjcoLld5Q> NE\GS4gzOzRzOEWyNy=>
K028 M4TF[GZ2dmO2aX;uJGF{e2G7 NHPyfnEzPTBibl2= NVLlS4xvOjRiaB?= MnjqbY5lfWOnczDHNkBienKnc4S= NVz3eFc4OjN2MUi1NlM>
K029 NH3MNopHfW6ldHnvckBCe3OjeR?= MlXjNlUxKG6P NXrIRY9ROjRiaB?= NVq5cmM6cW6mdXPld{BIOSCjcoLld5Q> MknQNlM1OTh3MkO=
M23 MkXtSpVv[3Srb36gRZN{[Xl? MorUNlUxKG6P M4HONFI1KGh? NYj5N29LcW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> NWnmZllrOjN2MUi1NlM>
K033 Ml\2SpVv[3Srb36gRZN{[Xl? MXiyOVAhdk1? M{DvXFI1KGh? Mm\NbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w NYnZSXNJOjN2MUi1NlM>
K008 MYXBdI9xfG:|aYOgRZN{[Xl? MX[xNFAhdk1? M3\KWFczKGh? M133OJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M1\DWFI{PDF6NUKz
K028 M{fGdWFxd3C2b4Ppd{BCe3OjeR?= MkXKNVAxKG6P NWrMXHJbPzJiaB?= NGLFdGl{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MlHzNlM1OTh3MkO=
K029 MUfBdI9xfG:|aYOgRZN{[Xl? M{m2OFExOCCwTR?= MW[3NkBp NFrydnh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| M3T1OlI{PDF6NUKz
M23 Ml;VRZBweHSxc3nzJGF{e2G7 M2fTT|ExOCCwTR?= MoDlO|IhcA>? MlL0d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MlrUNlM1OTh3MkO=
K033 M3y2UWFxd3C2b4Ppd{BCe3OjeR?= MXuxNFAhdk1? MkjWO|IhcA>? NYDuSGh2e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NFfaWZYzOzRzOEWyNy=>
RD NHuxN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRThibl2= M4HYNVI{OzB|N{Sx
Rh41 NEK3b41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\ub3BKSzVyPUGwMlQhdk1? MnvhNlM{ODN5NEG=
Rh18 NXjsOG5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHzTWM2OD14LkKgcm0> MkP0NlM{ODN5NEG=
Rh30 NHrMO|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTVwNjDuUS=> M3jtUFI{OzB|N{Sx
BT-12 MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof2TWM2OD1zND6zJI5O Mn\5NlM{ODN5NEG=
CHLA-266 NHPJd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrkTWM2OD1{Nz6xJI5O NV;vWFVPOjN|MEO3OFE>
TC-71 Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ruW2lEPTB;ND61JI5O NWHYPZE4OjN|MEO3OFE>
CHLA-9 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zjOWlEPTB;ND62JI5O MnT1NlM{ODN5NEG=
CHLA-10 NWnSepJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrON2ZKSzVyPUWuO{BvVQ>? Ml\MNlM{ODN5NEG=
CHLA-258 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy0WZB1UUN3ME22MlQhdk1? NHHPdokzOzNyM{e0NS=>
SJ-GBM2 MlnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHYTWM2OD1zMj65JI5O NVfz[5ZCOjN|MEO3OFE>
NB-1643 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XJOGlEPTB;Nz60JI5O NXHpdpN3OjN|MEO3OFE>
NB-EBc1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjXV4hKSzVyPUG2Mlghdk1? NFnwOnYzOzNyM{e0NS=>
CHLA-90 NXjXVGlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXVTWM2OD1{Mj6zJI5O MYiyN|MxOzd2MR?=
CHLA-136 MnTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XNSmlEPTB;MkOuNkBvVQ>? MlLuNlM{ODN5NEG=
NALM-6 NXHSfXpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvITWM2OD1zMT63JI5O NEPVR|gzOzNyM{e0NS=>
COG-LL-317 NIiyWoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjiTWM2OD12LkSgcm0> MmX1NlM{ODN5NEG=
RS4;11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7pUHZNUUN3ME2xN{42KG6P NFXGbZMzOzNyM{e0NS=>
MOLT-4 NF;XPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFyLk[gcm0> M2\teVI{OzB|N{Sx
CCRF-CEM (1) MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv3ZpJKSzVyPUGyMlUhdk1? Mnz1NlM{ODN5NEG=
CCRF-CEM (2) MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLQTWM2OD15LkKgcm0> NGC4THQzOzNyM{e0NS=>
Kasumi-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPiOnZ[UUN3ME21Mlghdk1? MmDvNlM{ODN5NEG=
Karpas-299 NYLqbXh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW0OWl7UUN3ME25MlYhdk1? MkHQNlM{ODN5NEG=
Ramos-RA1 NGOxT3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTdwNDDuUS=> MVeyN|MxOzd2MR?=
LNCaP NH;aPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRThibl2= NFXnSWwzOzF3MkCwOC=>
VCaP NGLURZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1L0N2lEPTB;NzDuUS=> M2jyNlI{OTV{MEC0
H1355 M4jsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzCblhyUUN3ME21JI5O NHrFVIkzOzBzMkK0PC=>
H157 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLlTWM2OD15IH7N M1vVOFI{ODF{MkS4
H460 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK5TWM2OD16IH7N NXzt[oxCOjNyMUKyOFg>
IA-LM MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHLd3NGUUN3ME2xNEBvVQ>? NFXHTJEzOzBzMkK0PC=>
HOP-62 NWHpN415T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFzIH7N NInVbG4zOzBzMkK0PC=>
H23 NV25bIlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnQZ3VsUUN3ME2xNUBvVQ>? NXHwdWpnOjNyMUKyOFg>
H2030 NWTQXGE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\RZYNKSzVyPUGyJI5O M3zkc|I{ODF{MkS4
H441 M2nxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTF2IH7N Mni1NlMxOTJ{NEi=
H2212 NYXObnlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M375WWlEPTB;MUegcm0> M3jhXFI{ODF{MkS4
SK-LU-1 M{H6TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjYTWM2OD1zODDuUS=> MYOyN|AyOjJ2OB?=
H2009 M4DhNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LRSWlEPTB;MUmgcm0> NWn3O3pxOjNyMUKyOFg>
H1792 NIGyOGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDoTWM2OD1{MDDuUS=> MXmyN|AyOjJ2OB?=
COR-L23 M{\jUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O4NGlEPTB;MkKgcm0> MYOyN|AyOjJ2OB?=
H727 NEnoS|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ6IH7N NGru[40zOzBzMkK0PC=>
H1734 NYK4THV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi2SnRKSzVyPUK4JI5O MWmyN|AyOjJ2OB?=
H358 NEC0XVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmK5TWM2OD1{OTDuUS=> MVuyN|AyOjJ2OB?=
A549 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjCSZhnUUN3ME20N{BvVQ>? NYjqbmJpOjNyMUKyOFg>
H2122 M{DpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFm5c5FKSzVyPUWzJI5O MWiyN|AyOjJ2OB?=
Calu-1 NUfsXYVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmraTWM2OD13ODDuUS=> MUiyN|AyOjJ2OB?=
Calu-6 M4[5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTZ2IH7N MYOyN|AyOjJ2OB?=
NCI-H1975 NEnjS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLLRnpPPDhiaB?= NYLpW2N2UUN3ME2xOkBvVQ>? MmDnNlIyPDR4NkW=
NCI-H1975 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PyflczKGh? M1XBOGlEPTB;ODDuUS=> MV[yNlE1PDZ4NR?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[4]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 40 mg/mL (109.76 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+45% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
11mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 364.4
化学式

C20H20N4O3

CAS No. 888216-25-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1
NCT02334319 Terminated Stage I Hypopharyngeal Squamous Cell Carcinoma|Stage I Laryngeal Squamous Cell Carcinoma|Stage I Oral Cavity Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma|Stage II Hypopharyngeal Squamous Cell Carcinoma|Stage II Laryngeal Squamous Cell Carcinoma|Stage II Oral Cavity Squamous Cell Carcinoma|Stage II Oropharyngeal Squamous Cell Carcinoma|Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Hypopharyngeal Squamous Cell Carcinoma|Stage IVA Laryngeal Squamous Cell Carcinoma|Stage IVA Oral Cavity Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma Emory University|Synta Pharmaceuticals Corp. December 2014 Phase 1
NCT02192541 Terminated Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 2 2014 Phase 1
NCT02261805 Terminated Cancer|Small Cell Lung Cancer Georgetown University|Synta Pharmaceuticals Corp. October 2014 Phase 1|Phase 2
NCT02012192 Terminated Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Medical University Innsbruck|European Commission July 4 2014 Phase 1|Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    Does this inhibitor inhibit both isoforms of HSP90?

  • 回答:

    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/

HSP (e.g. HSP90)シグナル伝達経路

HSP (e.g. HSP90) Inhibitors with Unique Features

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Tags: Ganetespib (STA-9090)を買う | Ganetespib (STA-9090) ic50 | Ganetespib (STA-9090)供給者 | Ganetespib (STA-9090)を購入する | Ganetespib (STA-9090)費用 | Ganetespib (STA-9090)生産者 | オーダーGanetespib (STA-9090) | Ganetespib (STA-9090)化学構造 | Ganetespib (STA-9090)分子量 | Ganetespib (STA-9090)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID