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)は一種のHSP90阻害剤で、OSA 8細胞の中にIC50値が4 nMですが、OSA細胞アポトーシスを誘導して、正常な造骨細胞に影響を与えません。Ganetespib (STA-9090)も一種のSTA-1474の活性代謝物です。臨床3期。

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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)は一種のHSP90阻害剤で、OSA 8細胞の中にIC50値が4 nMですが、OSA細胞アポトーシスを誘導して、正常な造骨細胞に影響を与えません。Ganetespib (STA-9090)も一種のSTA-1474の活性代謝物です。臨床3期。
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 Mo\qRZBweHSxc3nzJGF{e2G7 MYOzNE85OC9zNUCvNlUxKG6P M3KwXFI1NzR6L{eyJIg> MYTpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= Ml21NlU5QDJ3NUC=
MV411 NFfaTWdCeG:ydH;zbZMhSXO|YYm= NIrQbnA{OC96MD:xOVAwOjVyIH7N M1HGelI1NzR6L{eyJIg> NITNNlRqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NX3BR45vOjV6OEK1OVA>
MGC-803 NXiyS49sS2WubDDWbYFjcWyrdImgRZN{[Xl? NH65WpUxNjFvMUCwNEBvVQ>? NHT3cFU4OiCq NH\aUZpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2HNTVI2PTlyOEC1
SGC-7901 NF7SdY1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXSwMlEuOTByMDDuUS=> NX\qTmxWPzJiaB?= MmHrbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MU[yOVU6ODhyNR?=
MKN-28 NX\tOI9ZS2WubDDWbYFjcWyrdImgRZN{[Xl? NEjmO48xNjFvMUCwNEBvVQ>? MlLZO|IhcA>? Mo\wbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NWPEe|hjOjV3OUC4NFU>
MGC-803 MYDGeY5kfGmxbjDBd5NigQ>? MlTZNE4yNTFyMECgcm0> MYCyOEBp NVLyR5JzcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 MUmyOVU6ODhyNR?=
HCT-116 MkHTSpVv[3Srb36gRZN{[Xl? M2LCSlUxdk1? MnzuNlQhcA>? M{iydmROW09? NWLPb2o4cW6mdXPl[EBIOC:JMTDhdpJme3R? M{nE[FI2OjFyN{m0
HT-29 NGfoWoZHfW6ldHnvckBCe3OjeR?= MorPOVBvVQ>? MWWyOEBp NF\RT29FVVOR NIHmelNqdmS3Y3XkJGcxN0dzIHHydoV{fA>? NEG4U5czPTJzMEe5OC=>
SCC25 NXvIWJIxS3m2b4jpZ4l1gSCDc4PhfS=> NHnRRVUyOC93MDDuUS=> NVPHSWdTOjRiaB?= MV;k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NIHhblczPTJyNUSzNC=>
FUDA M3HyVWN6fG:6aXPpeJkhSXO|YYm= NFz5d2EyOC93MDDuUS=> MYKyOEBp NH3OfIhl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NUnzWpRpOjV{MEW0N|A>
Detroit562 MlvWR5l1d3irY3n0fUBCe3OjeR?= NGHKSI4yOC93MDDuUS=> NYj1N3RnOjRiaB?= MUPk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M{HCV|I2OjB3NEOw
CAL27 NXfOOnVtS3m2b4jpZ4l1gSCDc4PhfS=> NU\VS2VsOTBxNUCgcm0> Mm\JNlQhcA>? Mlni[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NIPO[GszPTJyNUSzNC=>
DSH1 NYPOW5RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULu[Xh5UUN3ME22JI5O MUCyOFc5PDh|OR?=
SW-1710 Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILrVo9KSzVyPU[gcm0> NVT3Z4VIOjR5OES4N|k>
T24 NF\OWY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTdibl2= Ml\3NlQ4QDR6M{m=
RT112 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjBS2R2UUN3ME25JI5O M2n0[|I1Pzh2OEO5
639-V NHG1elZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPaTWM2OD1zMDDuUS=> NUjqSJJ{OjR5OES4N|k>
SCaBER MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvSXWFKSzVyPUGwJI5O NXvaOlVOOjR5OES4N|k>
BFTC NVHTSo05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTjU3FTUUN3ME2xO{BvVQ>? MWSyOFc5PDh|OR?=
J82 MoLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LVZWlEPTB;MUigcm0> M4fCRlI1Pzh2OEO5
HT-1376 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJzIH7N MkXxNlQ4QDR6M{m=
647-V NV7QU2RlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjrN5UxUUN3ME2yO{BvVQ>? MUKyOFc5PDh|OR?=
UM-UC3 MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITXRZVKSzVyPUOzJI5O MoGzNlQ4QDR6M{m=
LB831-BLC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzrbXBTUUN3ME2zOEBvVQ>? MlrYNlQ4QDR6M{m=
KU-19-19 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDjN4NKUUN3ME2zOkBvVQ>? Ml\LNlQ4QDR6M{m=
35612 NXfiZ5RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XrfWlEPTB;M{igcm0> MXWyOFc5PDh|OR?=
5637 NHjGVXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TKZWlEPTB;NESgcm0> M3fFc|I1Pzh2OEO5
HT-1197 NFXqVm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLoWYdKSzVyPUWzJI5O NV3QbmxoOjR5OES4N|k>
MGH-U3 M3H4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTV|IH7N NGDnR3MzPDd6NEizPS=>
TCCSUP NFvsOJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33Bd2lEPTB;MUSyJI5O MVeyOFc5PDh|OR?=
RT4 M4DtWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTF5M{Ogcm0> MnTqNlQ4QDR6M{m=
SW780 NGOxVY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTN2NUGgcm0> M1fUPFI1Pzh2OEO5
RKO MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NED4OIxKSzVyPUSgcm0> MXyyOFY5Ojd2Nx?=
LS-411 N MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTVibl2= M{TEfFI1Pjh{N{S3
SW620 NV3oNoJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHy4bVJKSzVyPUigcm0> NGnGVFYzPDZ6Mke0Oy=>
HCT-15 MlPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXUTWM2OD16IH7N NFLPe5UzPDZ6Mke0Oy=>
HuTu-80 MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTF|IH7N NIDtWo0zPDZ6Mke0Oy=>
HCT 116 M{DDTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\5PGlEPTB;MUSgcm0> M1z2blI1Pjh{N{S3
COLO-205 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPs[XlKSzVyPUG0JI5O NUXqUYIxOjR4OEK3OFc>
NCI-H747 NH;lbm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrYSYlKSzVyPUG3JI5O MVOyOFY5Ojd2Nx?=
COLO-678 MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\MeZl{UUN3ME2yNUBvVQ>? MYOyOFY5Ojd2Nx?=
LoVo M1nlemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJ{IH7N NGTH[4MzPDZ6Mke0Oy=>
LS-1034 M1fPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrZcXB4UUN3ME2zNUBvVQ>? NX;yfpVmOjR4OEK3OFc>
SNU-C2B MmHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUiySlZMUUN3ME20OUBvVQ>? NVzRWol7OjR4OEK3OFc>
LS-123 NWnhTIg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHrNHFKSzVyPUezJI5O NWqxVlNzOjR4OEK3OFc>
SK-CO-1 NVi1ZW0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET3XGtKSzVyPUixJI5O MYSyOFY5Ojd2Nx?=
HCC2998 NWPabYhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrUdYV2UUN3ME2xNlghdk1? M3;5ZVI1Pjh{N{S3
MDA-MB-231 NETlZo5HfW6ldHnvckBCe3OjeR?= MnPpNVAxKG6P M3PTZlMxKG2rbh?= Mm\jbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? MkD4NlQzPDh{NkW=
MDA-MB-435 M{nJcWZ2dmO2aX;uJGF{e2G7 M2\hSlExOCCwTR?= NILZR2w{OCCvaX6= NIDiVpJqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NWn0e3JZOjR{NEiyOlU>
BT-20  M3zkSmZ2dmO2aX;uJGF{e2G7 NHH4WHMyODBxMkWwJI5O M4nnc|I1KGh? MWfy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> M4XlR|I1OTd|NUSx
MDA-MB-231 MUTGeY5kfGmxbjDBd5NigQ>? MlOwNVAxKG6P M4T2TFI1KGh? MYjpcohq[mm2czD0bIUhdWmpcnH0c5J6KGGwZDDpcpZie2m4ZTDjZZBi[2m2edMg M4KxclI1OTd|NUSx
H82 NGrtbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TRbWlEPTB;M{CuNlchdk1? NEDKO20zPDF4NkWwOS=>
GLC4 NYfVbpJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjMR5hKSzVyPUKwMlQ4KG6P MlHkNlQyPjZ3MEW=
H69 NHrOSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL0[lZKSzVyPUizMlM3KG6P MUeyOFE3PjVyNR?=
H128 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[5NGI1UUN3ME22PU42PSCwTR?= NXyx[I5wOjRzNk[1NFU>
H146 M4fsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nCPGlEPTB;MkiuOVEhdk1? MlvYNlQyPjZ3MEW=
H187 NFnDWpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGr0OXdKSzVyPUK0Mlk6KG6P MmHhNlQyPjZ3MEW=
H526 NFvmUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJzLk[0JI5O M3u5SVI1OTZ4NUC1
N592 M1;iZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLaVHJKSzVyPUG0MlEzKG6P NIPrcIkzPDF4NkWwOS=>
H620 NWDpfGtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj1TWM2OD1|Mj62O{BvVQ>? MXKyOFE3PjVyNR?=
H792 M4XNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnZTXlyUUN3ME20OU4xPyCwTR?= M1exc|I1OTZ4NUC1
H1173 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO3TWM2OD1zMj62NkBvVQ>? NEHJVlMzPDF4NkWwOS=>
AC3 M3PtfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jUbGlEPTB;MkWuPUBvVQ>? Moj1NlQyPjZ3MEW=
H82 MnjPSpVv[3Srb36gRZN{[Xl? M{S2PFMxKG6P M4rCWVczKGh? NHSyZ2ZqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NHTFflgzPDF4NkWwOS=>
GLC4 NWm5S5BuTnWwY4Tpc44hSXO|YYm= NVPxXYpVOzBibl2= MWm3NkBp M3jVcYlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NX3HdWN3OjRzNk[1NFU>
H146  MXXGeY5kfGmxbjDBd5NigQ>? NXvFS4RPOzBibl2= M4Pw[FczKGh? MUTpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NFzUNYozPDF4NkWwOS=>
OVCAR-5 NUTBXFZ7S2WubDDWbYFjcWyrdImgRZN{[Xl? MWCwMVExODBibl2= NEXXW3g4OiCq M3G2SYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MX[yN|kxODF|Nh?=
OVCAR-8 MlfWR4VtdCCYaXHibYxqfHliQYPzZZk> NEn1UFMxNTFyMECgcm0> NUjycZFIPzJiaB?= MoX5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MVmyN|kxODF|Nh?=
A1847 M2DSemNmdGxiVnnhZoltcXS7IFHzd4F6 M1vq[FAuOTByMDDuUS=> MljjO|IhcA>? MnXibY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MX[yN|kxODF|Nh?=
SKOV-3 M3:yfWNmdGxiVnnhZoltcXS7IFHzd4F6 NIjnVYExNTFyMECgcm0> NVXzSm5bPzJiaB?= MkDtbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M33aflI{QTByMUO2
OVCAR-5 NVLtR5h7SXCxcITvd4l{KEG|c3H5 MmHnNVAuOTByIH7N MmfUNlQwPDhxN{KgbC=> MWXpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 M2\uZ|I{QTByMUO2
OVCAR-8 Mn;xRZBweHSxc3nzJGF{e2G7 MUCxNE0yODBibl2= MYCyOE81QC95MjDo M{OyTYlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MYGyN|kxODF|Nh?=
A1847 MnTIRZBweHSxc3nzJGF{e2G7 NUGySXNNOTBvMUCwJI5O NIHWb|gzPC92OD:3NkBp MUDpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MnzTNlM6ODBzM{[=
H2228 MorQR4VtdCCYaXHibYxqfHliQYPzZZk> M1;vUVAuOTByMDDuUS=> NWDBOmJYPzJiaB?= MY\JR|UxRTF|IH7N Mn\HNlM2OzN{NkW=
H3122 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mlm5NE0yODByIH7N M{nMWlczKGh? M2nSeGlEPTB;MUCgcm0> NWrxbYFROjN3M{OyOlU>
K008 M3;TSGNmdGxiVnnhZoltcXS7IFHzd4F6 MoCxTWM2OD14MDDuUS=> M2D0flI{PDF6NUKz
K028 MmjjR4VtdCCYaXHibYxqfHliQYPzZZk> NH;we4VKSzVyPUi0JI5O M2D0dlI{PDF6NUKz
K029 M2DGeGNmdGxiVnnhZoltcXS7IFHzd4F6 MlTZTWM2OD12NjDuUS=> M4[zZVI{PDF6NUKz
M23 NE\LWplE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlX2TWM2OD1|Nz61JI5O M2LKO|I{PDF6NUKz
K033 MkPOR4VtdCCYaXHibYxqfHliQYPzZZk> MWfJR|UxRTd3LkWgcm0> M3u0cFI{PDF6NUKz
K008 NEGwfnpHfW6ldHnvckBCe3OjeR?= NWq3SlZ6OjVyIH7N NInFcHYzPCCq NXPT[oFOcW6mdXPld{BIOiCjcoLld5Q> NY[5THVCOjN2MUi1NlM>
K028 NYDUXHYzTnWwY4Tpc44hSXO|YYm= M3HQV|I2OCCwTR?= M1XL[lI1KGh? MUXpcoR2[2W|IFeyJIFzemW|dB?= MWiyN|QyQDV{Mx?=
K029 MYPGeY5kfGmxbjDBd5NigQ>? M{HCbVI2OCCwTR?= MX2yOEBp NWL0N3lDcW6mdXPld{BIOSCjcoLld5Q> M2fReVI{PDF6NUKz
M23 NGDMV3VHfW6ldHnvckBCe3OjeR?= M4\1PVI2OCCwTR?= Mlf6NlQhcA>? M3XSRYlv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0 MnvzNlM1OTh3MkO=
K033 M4CyN2Z2dmO2aX;uJGF{e2G7 M3zRblI2OCCwTR?= MYqyOEBp MlXnbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w Mor0NlM1OTh3MkO=
K008 NHThWYJCeG:ydH;zbZMhSXO|YYm= NV\ibJN5OTByIH7N MV63NkBp MnXQd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? Mmn6NlM1OTh3MkO=
K028 M4nQOWFxd3C2b4Ppd{BCe3OjeR?= M2juSlExOCCwTR?= NHzNUIo4OiCq MmH6d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MkDaNlM1OTh3MkO=
K029 NH\1b4ZCeG:ydH;zbZMhSXO|YYm= Mn\YNVAxKG6P NHruUHk4OiCq NHfKc2d{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MknXNlM1OTh3MkO=
M23 NFHtbJlCeG:ydH;zbZMhSXO|YYm= NIDuTZAyODBibl2= NFfmbIo4OiCq M3rHR5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NEPiOGwzOzRzOEWyNy=>
K033 M1vXXmFxd3C2b4Ppd{BCe3OjeR?= MVWxNFAhdk1? M4LuZVczKGh? NV3LUJRxe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= M4H1OFI{PDF6NUKz
RD NWSwW5U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy4c3pKUUN3ME24JI5O NF61epIzOzNyM{e0NS=>
Rh41 NU\wT3QxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTFyLkSgcm0> NFPLdXozOzNyM{e0NS=>
Rh18 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGC4bXJKSzVyPU[uNkBvVQ>? NXrMdYtHOjN|MEO3OFE>
Rh30 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn5d4hKSzVyPUWuOkBvVQ>? MlTDNlM{ODN5NEG=
BT-12 NGTmOG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF2LkOgcm0> NXTOenJZOjN|MEO3OFE>
CHLA-266 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n5OmlEPTB;MkeuNUBvVQ>? MYGyN|MxOzd2MR?=
TC-71 MmniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTRwNTDuUS=> MkL1NlM{ODN5NEG=
CHLA-9 M{LDe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX6TWM2OD12Lk[gcm0> M3vuUlI{OzB|N{Sx
CHLA-10 M2DmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3SyWmlEPTB;NT63JI5O MUSyN|MxOzd2MR?=
CHLA-258 NV7CfYxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYju[YdXUUN3ME22MlQhdk1? MV6yN|MxOzd2MR?=
SJ-GBM2 NVXvU48xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUizepdRUUN3ME2xNk46KG6P NUjD[Xh7OjN|MEO3OFE>
NB-1643 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC3TGtoUUN3ME23MlQhdk1? MY[yN|MxOzd2MR?=
NB-EBc1 NVnyNZNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTF4Lkigcm0> NI\mTnczOzNyM{e0NS=>
CHLA-90 MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTJ{LkOgcm0> NYXVVHdFOjN|MEO3OFE>
CHLA-136 NH;xcWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULFdplIUUN3ME2yN{4zKG6P MYCyN|MxOzd2MR?=
NALM-6 M{niXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX1WGxKSzVyPUGxMlchdk1? Mn\oNlM{ODN5NEG=
COG-LL-317 NVy3NWVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG2TWM2OD12LkSgcm0> MWSyN|MxOzd2MR?=
RS4;11 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjCTWM2OD1zMz61JI5O M3j2b|I{OzB|N{Sx
MOLT-4 M2\MZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFyLk[gcm0> MV2yN|MxOzd2MR?=
CCRF-CEM (1) MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HzVmlEPTB;MUKuOUBvVQ>? MnTiNlM{ODN5NEG=
CCRF-CEM (2) NEPJ[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DBZmlEPTB;Nz6yJI5O MUOyN|MxOzd2MR?=
Kasumi-1 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVwODDuUS=> MViyN|MxOzd2MR?=
Karpas-299 NEDMN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK0TJlrUUN3ME25MlYhdk1? MVGyN|MxOzd2MR?=
Ramos-RA1 MmHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTdwNDDuUS=> M37wU|I{OzB|N{Sx
LNCaP NGrPd4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDqUWlKSzVyPUigcm0> NGTDOoszOzF3MkCwOC=>
VCaP MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn3UYxKSzVyPUegcm0> NUXPXFVqOjNzNUKwNFQ>
H1355 MnXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH2[HVKSzVyPUWgcm0> NF:5ZokzOzBzMkK0PC=>
H157 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXRU5ZKSzVyPUegcm0> NWK4N5U3OjNyMUKyOFg>
H460 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XkfGlEPTB;ODDuUS=> MXmyN|AyOjJ2OB?=
IA-LM MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFyIH7N NFfPS|gzOzBzMkK0PC=>
HOP-62 M33CW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\T[Wt{UUN3ME2xNUBvVQ>? MVOyN|AyOjJ2OB?=
H23 NF;4XG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXqVnc1UUN3ME2xNUBvVQ>? MWWyN|AyOjJ2OB?=
H2030 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF{IH7N MlrENlMxOTJ{NEi=
H441 NGHTTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XjOWlEPTB;MUSgcm0> M1XMeFI{ODF{MkS4
H2212 MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTjTWM2OD1zNzDuUS=> NX32UXJvOjNyMUKyOFg>
SK-LU-1 NWTPVHFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF6IH7N NXzkbWRKOjNyMUKyOFg>
H2009 M2XQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLOSHI4UUN3ME2xPUBvVQ>? M{X6e|I{ODF{MkS4
H1792 NWC4dnhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rieWlEPTB;MkCgcm0> MmTsNlMxOTJ{NEi=
COR-L23 M3\hOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTJ{IH7N NF36cIUzOzBzMkK0PC=>
H727 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn5NW41UUN3ME2yPEBvVQ>? NUPpc4hQOjNyMUKyOFg>
H1734 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HP[WlEPTB;Mkigcm0> MoWzNlMxOTJ{NEi=
H358 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjtZlB7UUN3ME2yPUBvVQ>? NIrXb2MzOzBzMkK0PC=>
A549 NFHwPHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPI[ItsUUN3ME20N{BvVQ>? MkjYNlMxOTJ{NEi=
H2122 M3LZVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTV|IH7N MXOyN|AyOjJ2OB?=
Calu-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LRbGlEPTB;NUigcm0> MV2yN|AyOjJ2OB?=
Calu-6 MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG3TWM2OD14NDDuUS=> NGPCZoIzOzBzMkK0PC=>
NCI-H1975 Ml3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvLOFghcA>? NV2zfYwyUUN3ME2xOkBvVQ>? M1nmXlIzOTR2Nk[1
NCI-H1975 M2\hdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDlO|IhcA>? MV3JR|UxRThibl2= Ml;UNlIyPDR4NkW=

多くの細胞株試験データを見る場合、クリックしてください

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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:
5% DMSO+45% PEG 300+ddH2O
11mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02192541 Completed Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 9, 2014 Phase 1
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 --
NCT02389751 Active, not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Synta Pharmaceuticals Corp. April 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
NCT02261805 Terminated Cancer|Small Cell Lung Cancer Georgetown University|Synta Pharmaceuticals Corp. October 2014 Phase 1|Phase 2
NCT02272478 Recruiting Acute Myeloid Leukaemia|Myelodysplastic Syndrome Cardiff University|Cancer Research UK October 2014 Phase 3

技術サポート

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。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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)信号経路図

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