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 MWjBdI9xfG:|aYOgRZN{[Xl? MkHrN|AwQDBxMUWwM|I2OCCwTR?= NXHBPZhnOjRxNEivO|IhcA>? M1nhRolv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> M{PYZ|I2QDh{NUWw
MV411 Mn:0RZBweHSxc3nzJGF{e2G7 NF3uc|E{OC96MD:xOVAwOjVyIH7N MnPoNlQwPDhxN{KgbC=> NUnCfHdYcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ M2n1W|I2QDh{NUWw
MGC-803 Mn3mR4VtdCCYaXHibYxqfHliQYPzZZk> M4PMWVAvOS1zMECwJI5O MkPiO|IhcA>? M3q0W4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NVrCZoRFOjV3OUC4NFU>
SGC-7901 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2f6elAvOS1zMECwJI5O NH\scmU4OiCq NH\CV4tqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGTNdGgzPTV7MEiwOS=>
MKN-28 NFzqT4lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX2wMlEuOTByMDDuUS=> MVq3NkBp Mm\0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NV;6eXdzOjV3OUC4NFU>
MGC-803 MkTDSpVv[3Srb36gRZN{[Xl? MWqwMlEuOTByMDDuUS=> M2PSXVI1KGh? M2ntSIlv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? MoTNNlU2QTB6MEW=
HCT-116 M17zUmZ2dmO2aX;uJGF{e2G7 M2\uNFUxdk1? MVGyOEBp MormSG1UVw>? NYrOSoFVcW6mdXPl[EBIOC:JMTDhdpJme3R? NGG3b|QzPTJzMEe5OC=>
HT-29 NXXrXWFuTnWwY4Tpc44hSXO|YYm= NUS4OG8zPTCwTR?= MYCyOEBp NXf0cJF3TE2VTx?= NUTi[29ucW6mdXPl[EBIOC:JMTDhdpJme3R? NYnMPWhMOjV{MUC3PVQ>
SCC25 NXfC[Jd4S3m2b4jpZ4l1gSCDc4PhfS=> MmLxNVAwPTBibl2= NVnRcINuOjRiaB?= M3G5WYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NIDnUIczPTJyNUSzNC=>
FUDA MmXpR5l1d3irY3n0fUBCe3OjeR?= M1zFOlExNzVyIH7N MXiyOEBp NFPIcWJl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M1zE[lI2OjB3NEOw
Detroit562 MmLoR5l1d3irY3n0fUBCe3OjeR?= MX2xNE82OCCwTR?= MYSyOEBp M2ruWoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M2\sb|I2OjB3NEOw
CAL27 NWDhUZNrS3m2b4jpZ4l1gSCDc4PhfS=> M1\5N|ExNzVyIH7N NWjER3dYOjRiaB?= NHnkc21l\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MlX3NlUzODV2M{C=
DSH1 M1vPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrEUnRKSzVyPU[gcm0> NHrwZW0zPDd6NEizPS=>
SW-1710 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTZibl2= NXq5epZXOjR5OES4N|k>
T24 M3fSU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETacGlKSzVyPUegcm0> NFHLXnMzPDd6NEizPS=>
RT112 NFjXbWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTlibl2= MUmyOFc5PDh|OR?=
639-V NUTUd|N5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrqTWM2OD1zMDDuUS=> MWWyOFc5PDh|OR?=
SCaBER M3\Wbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTFyIH7N NGPMSVczPDd6NEizPS=>
BFTC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPZNoF6UUN3ME2xO{BvVQ>? MmjZNlQ4QDR6M{m=
J82 NGPablJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF6IH7N MVuyOFc5PDh|OR?=
HT-1376 NW\3cnhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnroTWM2OD1{MTDuUS=> MnLINlQ4QDR6M{m=
647-V M2TL[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJ5IH7N NIf2R4QzPDd6NEizPS=>
UM-UC3 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTN|IH7N NGTnc2QzPDd6NEizPS=>
LB831-BLC MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTN2IH7N NG\BWI4zPDd6NEizPS=>
KU-19-19 NUDUSpRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTN4IH7N NWX4R2V3OjR5OES4N|k>
35612 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrafIZKSzVyPUO4JI5O NXG5S|BMOjR5OES4N|k>
5637 Ml7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLBSFFKSzVyPUS0JI5O Mn;nNlQ4QDR6M{m=
HT-1197 NGXSOJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvpVpZCUUN3ME21N{BvVQ>? M3zCTlI1Pzh2OEO5
MGH-U3 NWjFd4JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL1R2x5UUN3ME21N{BvVQ>? MXKyOFc5PDh|OR?=
TCCSUP MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDGW|JoUUN3ME2xOFIhdk1? MmnKNlQ4QDR6M{m=
RT4 M{fZdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTF5M{Ogcm0> NXv2UGw4OjR5OES4N|k>
SW780 MnrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWxWHFKSzVyPUO0OVEhdk1? NILpXGQzPDd6NEizPS=>
RKO NF:zXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTRibl2= MXmyOFY5Ojd2Nx?=
LS-411 N M3n0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrSTWM2OD13IH7N M1rmN|I1Pjh{N{S3
SW620 NHK2U|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzGVmlnUUN3ME24JI5O NEi4TJczPDZ6Mke0Oy=>
HCT-15 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTtVWRKSzVyPUigcm0> NELKfpEzPDZ6Mke0Oy=>
HuTu-80 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\FS2lEPTB;MUOgcm0> Mo\LNlQ3QDJ5NEe=
HCT 116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXqOmZKUUN3ME2xOEBvVQ>? MUmyOFY5Ojd2Nx?=
COLO-205 M{PqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3WwT2lEPTB;MUSgcm0> M2nXUVI1Pjh{N{S3
NCI-H747 M4\wRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHMeZM6UUN3ME2xO{BvVQ>? NFHCd2QzPDZ6Mke0Oy=>
COLO-678 MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTOTWM2OD1{MTDuUS=> M2r5T|I1Pjh{N{S3
LoVo MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnuTWM2OD1{MjDuUS=> NVr2W2xVOjR4OEK3OFc>
LS-1034 M1H0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOzcFE1UUN3ME2zNUBvVQ>? NXexT5JFOjR4OEK3OFc>
SNU-C2B MlLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTVWZc4UUN3ME20OUBvVQ>? NEmwToUzPDZ6Mke0Oy=>
LS-123 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXzdGlKSzVyPUezJI5O MUGyOFY5Ojd2Nx?=
SK-CO-1 NHzxZ3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXnbYtjUUN3ME24NUBvVQ>? MlfKNlQ3QDJ5NEe=
HCC2998 M371XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nyZmlEPTB;MUK4JI5O MYGyOFY5Ojd2Nx?=
MDA-MB-231 MVfGeY5kfGmxbjDBd5NigQ>? M3roOlExOCCwTR?= NGjC[VU{OCCvaX6= MmLVbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? MVWyOFI1QDJ4NR?=
MDA-MB-435 NWjx[nBYTnWwY4Tpc44hSXO|YYm= MWOxNFAhdk1? MYOzNEBucW5? NH3ocY1qdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NInQc2EzPDJ2OEK2OS=>
BT-20  MWfGeY5kfGmxbjDBd5NigQ>? MUexNFAwOjVyIH7N NHvpZZEzPCCq NGXXeHVz\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? M2mzdFI1OTd|NUSx
MDA-MB-231 MX7GeY5kfGmxbjDBd5NigQ>? NH3xUY8yODBibl2= NWrufW04OjRiaB?= MmrDbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> MXeyOFE4OzV2MR?=
H82 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jZPGlEPTB;M{CuNlchdk1? NGrCb2QzPDF4NkWwOS=>
GLC4 Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn4WItGUUN3ME2yNE41PyCwTR?= MYSyOFE3PjVyNR?=
H69 MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTGdY5bUUN3ME24N{4{PiCwTR?= NFy2OVIzPDF4NkWwOS=>
H128 NWrMS4tpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3JVlBKSzVyPU[5MlU2KG6P NF\heXUzPDF4NkWwOS=>
H146 M4XCdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfsRllKSzVyPUK4MlUyKG6P MXmyOFE3PjVyNR?=
H187 MmDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ2Lkm5JI5O NHXiSZkzPDF4NkWwOS=>
H526 M4Tkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{n3eWlEPTB;MkGuOlQhdk1? M2TZRlI1OTZ4NUC1
N592 NU\HWFRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojiTWM2OD1zND6xNkBvVQ>? MYSyOFE3PjVyNR?=
H620 NFjzW3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPFTWM2OD1|Mj62O{BvVQ>? Mnn2NlQyPjZ3MEW=
H792 M3jXOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTR3LkC3JI5O NHrafJgzPDF4NkWwOS=>
H1173 MoXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTF{Lk[yJI5O NEf4emwzPDF4NkWwOS=>
AC3 MlPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ3Lkmgcm0> NV;v[I51OjRzNk[1NFU>
H82 NXjqU|hzTnWwY4Tpc44hSXO|YYm= NGDLTm4{OCCwTR?= M{\QPVczKGh? NHjyN2lqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NXTrSms5OjRzNk[1NFU>
GLC4 NVPsUG1TTnWwY4Tpc44hSXO|YYm= NWO2VGZ4OzBibl2= M2P0bFczKGh? M1jxeIlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M1fjNFI1OTZ4NUC1
H146  NELBOGZHfW6ldHnvckBCe3OjeR?= NIPLd2E{OCCwTR?= MVK3NkBp NFPscI1qdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MVeyOFE3PjVyNR?=
OVCAR-5 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{PpWVAuOTByMDDuUS=> MWG3NkBp Mlq3bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MYKyN|kxODF|Nh?=
OVCAR-8 NEfzWodE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX;WToVrOC1zMECwJI5O MXS3NkBp M2fa[YlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MWeyN|kxODF|Nh?=
A1847 MmTaR4VtdCCYaXHibYxqfHliQYPzZZk> NFzMXVExNTFyMECgcm0> MYK3NkBp MmOxbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MnHGNlM6ODBzM{[=
SKOV-3 MojVR4VtdCCYaXHibYxqfHliQYPzZZk> NGL2fGMxNTFyMECgcm0> MUS3NkBp NHuyO5NqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M{fieFI{QTByMUO2
OVCAR-5 MX3BdI9xfG:|aYOgRZN{[Xl? Mk\YNVAuOTByIH7N MWeyOE81QC95MjDo M4DoXIlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MVeyN|kxODF|Nh?=
OVCAR-8 MmHwRZBweHSxc3nzJGF{e2G7 MkflNVAuOTByIH7N MXuyOE81QC95MjDo M2fPe4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= NUHvfXhVOjN7MECxN|Y>
A1847 MVfBdI9xfG:|aYOgRZN{[Xl? MYWxNE0yODBibl2= M3G2fVI1NzR6L{eyJIg> NY\IO5NEcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NX;aOVBUOjN7MECxN|Y>
H2228 M17MbGNmdGxiVnnhZoltcXS7IFHzd4F6 NIDqVFcxNTFyMECgcm0> NWTwW5lpPzJiaB?= NIHGfnlKSzVyPUGzJI5O NGL6WZYzOzV|M{K2OS=>
H3122 NVPGfnN3S2WubDDWbYFjcWyrdImgRZN{[Xl? M4XOeVAuOTByMDDuUS=> NVHq[Y9kPzJiaB?= MoXJTWM2OD1zMDDuUS=> NHrUXmgzOzV|M{K2OS=>
K008 M1vJTmNmdGxiVnnhZoltcXS7IFHzd4F6 MWXJR|UxRTZyIH7N MY[yN|QyQDV{Mx?=
K028 M3XWZ2NmdGxiVnnhZoltcXS7IFHzd4F6 MkLSTWM2OD16NDDuUS=> MkDENlM1OTh3MkO=
K029 NWH1OXVTS2WubDDWbYFjcWyrdImgRZN{[Xl? NX7OfGlDUUN3ME20OkBvVQ>? MonBNlM1OTh3MkO=
M23 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXrOR3d2UUN3ME2zO{42KG6P NIrvPVgzOzRzOEWyNy=>
K033 NYHPNoRYS2WubDDWbYFjcWyrdImgRZN{[Xl? NG\2[4FKSzVyPUe1MlUhdk1? MVeyN|QyQDV{Mx?=
K008 MlHNSpVv[3Srb36gRZN{[Xl? M4XaWVI2OCCwTR?= NEGzZVAzPCCq M4Hncolv\HWlZYOgS|Ih[XK{ZYP0 MnrFNlM1OTh3MkO=
K028 MVPGeY5kfGmxbjDBd5NigQ>? M33XcVI2OCCwTR?= NGPmdlEzPCCq MoLLbY5lfWOnczDHNkBienKnc4S= MnLJNlM1OTh3MkO=
K029 MkDkSpVv[3Srb36gRZN{[Xl? NVXac2c4OjVyIH7N MX:yOEBp MXzpcoR2[2W|IFexJIFzemW|dB?= NXjMc4FDOjN2MUi1NlM>
M23 NVnl[HJCTnWwY4Tpc44hSXO|YYm= M2TldFI2OCCwTR?= MmLpNlQhcA>? NHnZNoxqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> M1PQTlI{PDF6NUKz
K033 NEmzPG1HfW6ldHnvckBCe3OjeR?= MonXNlUxKG6P MljMNlQhcA>? NYXsNoJNcW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u MVmyN|QyQDV{Mx?=
K008 MlG0RZBweHSxc3nzJGF{e2G7 Mo\JNVAxKG6P NFPae|c4OiCq MX7zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NYHzV5BbOjN2MUi1NlM>
K028 MWrBdI9xfG:|aYOgRZN{[Xl? MUSxNFAhdk1? MmjNO|IhcA>? MnjTd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M2joOFI{PDF6NUKz
K029 NXm1OZVGSXCxcITvd4l{KEG|c3H5 M3TGc|ExOCCwTR?= Mme4O|IhcA>? M1G0[pNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MYWyN|QyQDV{Mx?=
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A549 NUnXWFNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv6VVhKSzVyPUSzJI5O Ml7oNlMxOTJ{NEi=
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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

相関HSP (e.g. HSP90)製品

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