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Ganetespib (STA-9090)

Ganetespib (STA-9090)是一種HSP90抑制劑，在OSA 8種細胞中IC50為4 nM，誘導OSA細胞凋亡，而不影響正常的成骨細胞；是STA-1474的活性代謝物。Phase 3。

Ganetespib (STA-9090) Chemical Structure

Ganetespib (STA-9090) Chemical Structure

CAS: 888216-25-9

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1392.3 現(xiàn)貨
5mg 1122.03 現(xiàn)貨
50mg 7944.3 現(xiàn)貨
1g 33554.43 現(xiàn)貨
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Ganetespib (STA-9090)相關(guān)產(chǎn)品

相關(guān)信號通路圖

HSP (HSP90) Signaling Pathways

HSP (HSP90)信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
A1847 Apoptosis Assay 10-100 nM 24/48/72 h induces apoptosis time and dose dependently 23900136
H2228 Cell Viability Assay 0-1000 nM 72 h IC50=13 nM 23533265
H3122 Cell Viability Assay 0-1000 nM 72 h IC50=10 nM 23533265
K008 Function Assay 250 nM 24 h induces G2 arrest 23418523
K028 Function Assay 250 nM 24 h induces G2 arrest 23418523
K029 Function Assay 250 nM 24 h induces G1 arrest 23418523
M23 Function Assay 250 nM 24 h induces G1 and G2/M arrest 23418523
K033 Function Assay 250 nM 24 h induces a modest increase in G1 population 23418523
K008 Apoptosis Assay 100 nM 72 h significantly induces apoptosis 23418523
K028 Apoptosis Assay 100 nM 72 h significantly induces apoptosis 23418523
K029 Apoptosis Assay 100 nM 72 h significantly induces apoptosis 23418523
M23 Apoptosis Assay 100 nM 72 h significantly induces apoptosis 23418523
K033 Apoptosis Assay 100 nM 72 h significantly induces apoptosis 23418523
OVCAR-8 Apoptosis Assay 10-100 nM 24/48/72 h induces apoptosis time and dose dependently 23900136
OVCAR-5 Apoptosis Assay 10-100 nM 24/48/72 h induces apoptosis time and dose dependently 23900136
SKOV-3 Cell Viability Assay 0-1000 nM 72 h inhibits cell viability dose dependently 23900136
A1847 Cell Viability Assay 0-1000 nM 72 h inhibits cell viability dose dependently 23900136
OVCAR-8 Cell Viability Assay 0-1000 nM 72 h inhibits cell viability dose dependently 23900136
OVCAR-5 Cell Viability Assay 0-1000 nM 72 h inhibits cell viability dose dependently 23900136
H146? Function Assay 30 nM 72 h induces persistent G2/M phase arrest 24166505
GLC4 Function Assay 30 nM 72 h induces persistent G2/M phase arrest 24166505
H82 Function Assay 30 nM 72 h induces persistent G2/M phase arrest 24166505
MDA-MB-231 Function Assay 100 nM 24 h inhibits the migratory and invasive capacity? 24173541
BT-20? Function Assay 100/250 nM 24 h resulted in a dose-dependent destabilization of EGFR, IGF-IR, MET, and CRAF 24173541
MDA-MB-435 Function Assay 100 nM 30 min inhibits accumulation of HIF-1α 24248265
MDA-MB-231 Function Assay 100 nM 30 min inhibits accumulation of HIF-1α 24248265
CAL27 Cytoxicity Assay 10/50 nM 24 h decreases cell proliferation dose dependently 25205430
Detroit562 Cytoxicity Assay 10/50 nM 24 h decreases cell proliferation dose dependently 25205430
FUDA Cytoxicity Assay 10/50 nM 24 h decreases cell proliferation dose dependently 25205430
SCC25 Cytoxicity Assay 10/50 nM 24 h decreases cell proliferation dose dependently 25205430
HT-29 Function Assay 50nM 24 h induced G0/G1 arrest 25210794
HCT-116 Function Assay 50nM 24 h induced G0/G1 arrest 25210794
MGC-803 Function Assay 0.1-1000 nM 24 h induces G2/M cell-cycle arrest 25590805
MKN-28 Cell Viability Assay 0.1-1000 nM 72 h inhibits cell viability dose dependently 25590805
SGC-7901 Cell Viability Assay 0.1-1000 nM 72 h inhibits cell viability dose dependently 25590805
MGC-803 Cell Viability Assay 0.1-1000 nM 72 h inhibits cell viability dose dependently 25590805
MV411 Apoptosis Assay 30/80/150/250 nM 24/48/72 h induces dose dependant induction of apoptosis 25882550
HL60 Apoptosis Assay 30/80/150/250 nM 24/48/72 h induces dose dependant induction of apoptosis 25882550
NCI-H1975 Growth Inhibition Assay 48 h IC50=16 nM 22144665
NCI-H1975 Growth Inhibition Assay 72 h IC50=8 nM 22144665
K008 Cell Viability Assay IC50=60 nM 23418523
K028 Cell Viability Assay IC50=84 nM 23418523
K029 Cell Viability Assay IC50=46 nM 23418523
M23 Cell Viability Assay IC50=37.5 nM 23418523
K033 Cell Viability Assay IC50=75.5 nM 23418523
RD Growth Inhibition Assay IC50=8 nM 23303741
Rh41 Growth Inhibition Assay IC50=10.4 nM 23303741
Rh18 Growth Inhibition Assay IC50=6.2 nM 23303741
Rh30 Growth Inhibition Assay IC50=5.6 nM 23303741
BT-12 Growth Inhibition Assay IC50=14.3 nM 23303741
CHLA-266 Growth Inhibition Assay IC50=27.1 nM 23303741
TC-71 Growth Inhibition Assay IC50=4.5 nM 23303741
CHLA-9 Growth Inhibition Assay IC50=4.6 nM 23303741
CHLA-10 Growth Inhibition Assay IC50=5.7 nM 23303741
CHLA-258 Growth Inhibition Assay IC50=6.4 nM 23303741
SJ-GBM2 Growth Inhibition Assay IC50=12.9 nM 23303741
NB-1643 Growth Inhibition Assay IC50=7.4 nM 23303741
NB-EBc1 Growth Inhibition Assay IC50=16.8 nM 23303741
CHLA-90 Growth Inhibition Assay IC50=22.3 nM 23303741
CHLA-136 Growth Inhibition Assay IC50=23.2 nM 23303741
NALM-6 Growth Inhibition Assay IC50=11.7 nM 23303741
COG-LL-317 Growth Inhibition Assay IC50=4.4 nM 23303741
RS4;11 Growth Inhibition Assay IC50=13.5 nM 23303741
MOLT-4 Growth Inhibition Assay IC50=10.6 nM 23303741
CCRF-CEM (1) Growth Inhibition Assay IC50=12.5 nM 23303741
CCRF-CEM (2) Growth Inhibition Assay IC50=7.2 nM 23303741
Kasumi-1 Growth Inhibition Assay IC50=5.8 nM 23303741
Karpas-299 Growth Inhibition Assay IC50=9.6 nM 23303741
Ramos-RA1 Growth Inhibition Assay IC50=7.4 nM 23303741
LNCaP Growth Inhibition Assay IC50=8 nM 23152004
VCaP Growth Inhibition Assay IC50=7 nM 23152004
H1355 Growth Inhibition Assay IC50=5 nM 23012248
H157 Growth Inhibition Assay IC50=7 nM 23012248
H460 Growth Inhibition Assay IC50=8 nM 23012248
IA-LM Growth Inhibition Assay IC50=10 nM 23012248
HOP-62 Growth Inhibition Assay IC50=11 nM 23012248
H23 Growth Inhibition Assay IC50=11 nM 23012248
H2030 Growth Inhibition Assay IC50=12 nM 23012248
H441 Growth Inhibition Assay IC50=14 nM 23012248
H2212 Growth Inhibition Assay IC50=17 nM 23012248
SK-LU-1 Growth Inhibition Assay IC50=18 nM 23012248
H2009 Growth Inhibition Assay IC50=19 nM 23012248
H1792 Growth Inhibition Assay IC50=20 nM 23012248
COR-L23 Growth Inhibition Assay IC50=22 nM 23012248
H727 Growth Inhibition Assay IC50=28 nM 23012248
H1734 Growth Inhibition Assay IC50=28 nM 23012248
H358 Growth Inhibition Assay IC50=29 nM 23012248
A549 Growth Inhibition Assay IC50=43 nM 23012248
H2122 Growth Inhibition Assay IC50=53 nM 23012248
Calu-1 Growth Inhibition Assay IC50=58 nM 23012248
Calu-6 Growth Inhibition Assay IC50=64 nM 23012248
AC3 Growth Inhibition Assay IC50=25.9 nM 24166505
H1173 Growth Inhibition Assay IC50=12.62 nM 24166505
H792 Growth Inhibition Assay IC50=45.07 nM 24166505
H620 Growth Inhibition Assay IC50=32.67 nM 24166505
N592 Growth Inhibition Assay IC50=14.12 nM 24166505
H526 Growth Inhibition Assay IC50=21.64 nM 24166505
H187 Growth Inhibition Assay IC50=24.99 nM 24166505
H146 Growth Inhibition Assay IC50=28.51 nM 24166505
H128 Growth Inhibition Assay IC50=69.55 nM 24166505
H69 Growth Inhibition Assay IC50=83.36 nM 24166505
GLC4 Growth Inhibition Assay IC50=20.47 nM 24166505
H82 Growth Inhibition Assay IC50=30.27 nM 24166505
HCC2998 Growth Inhibition Assay IC50=128 nM 24682747
SK-CO-1 Growth Inhibition Assay IC50=81 nM 24682747
LS-123 Growth Inhibition Assay IC50=73 nM 24682747
SNU-C2B Growth Inhibition Assay IC50=45 nM 24682747
LS-1034 Growth Inhibition Assay IC50=31 nM 24682747
LoVo Growth Inhibition Assay IC50=22 nM 24682747
COLO-678 Growth Inhibition Assay IC50=21 nM 24682747
NCI-H747 Growth Inhibition Assay IC50=17 nM 24682747
COLO-205 Growth Inhibition Assay IC50=14 nM 24682747
HCT 116 Growth Inhibition Assay IC50=14 nM 24682747
HuTu-80 Growth Inhibition Assay IC50=13 nM 24682747
HCT-15 Growth Inhibition Assay IC50=8 nM 24682747
SW620 Growth Inhibition Assay IC50=8 nM 24682747
LS-411?N Growth Inhibition Assay IC50=5 nM 24682747
RKO Growth Inhibition Assay IC50=4 nM 24682747
SW780 Growth Inhibition Assay IC50=3451 nM 24784839
RT4 Growth Inhibition Assay IC50=1733 nM 24784839
TCCSUP Growth Inhibition Assay IC50=142 nM 24784839
MGH-U3 Growth Inhibition Assay IC50=53 nM 24784839
HT-1197 Growth Inhibition Assay IC50=53 nM 24784839
5637 Growth Inhibition Assay IC50=44 nM 24784839
35612 Growth Inhibition Assay IC50=38 nM 24784839
KU-19-19 Growth Inhibition Assay IC50=36 nM 24784839
LB831-BLC Growth Inhibition Assay IC50=34 nM 24784839
UM-UC3 Growth Inhibition Assay IC50=33 nM 24784839
647-V Growth Inhibition Assay IC50=27 nM 24784839
HT-1376 Growth Inhibition Assay IC50=21 nM 24784839
J82 Growth Inhibition Assay IC50=18 nM 24784839
BFTC Growth Inhibition Assay IC50=17 nM 24784839
SCaBER Growth Inhibition Assay IC50=10 nM 24784839
639-V Growth Inhibition Assay IC50=10 nM 24784839
RT112 Growth Inhibition Assay IC50=9 nM 24784839
T24 Growth Inhibition Assay IC50=7 nM 24784839
SW-1710 Growth Inhibition Assay IC50=6 nM 24784839
DSH1 Growth Inhibition Assay IC50=6 nM 24784839
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
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生物活性

產(chǎn)品描述 Ganetespib (STA-9090)是一種HSP90抑制劑，在OSA 8種細胞中IC50為4 nM，誘導OSA細胞凋亡，而不影響正常的成骨細胞；是STA-1474的活性代謝物。Phase 3。
靶點
HSP90 [1]
(OSA 8 cells)
4 nM
體外研究(In Vitro)
體外研究活性 Ganetespib對惡性肥大細胞系的50%抑制濃度(IC50)比對17-AAG低10-15倍，表明三唑酮類HSP90抑制劑可能比格爾德霉素類抑制劑具有更高的效能。[1] Ganetespib抑制MG63細胞系，IC50為43 nM。[1] Ganetespib結(jié)合于Hsp90的N末端ATP結(jié)合域，通過引起多重致瘤性Hsp90受體蛋白，包括HER2/neu，突變型EGFR，Akt，c-Kit，IGF-1R，PDGFRα，Jak1，Jak2，STAT3，STAT5，HIF-1α，CDC2和c-Met 以及Wilms' tumor 1的降解，成為一種有效的Hsp90的抑制劑。[2] Ganetespib，在納摩爾級低濃度下，有效阻滯細胞增殖，并誘導廣泛的人腫瘤細胞系凋亡，并且對許多受體酪氨酸激酶抑制劑-和tanespimycin-耐受的細胞系也具有作用。Ganetespib在一系列固體和血液腫瘤細胞系，包括那些對小分子酪氨酸激酶抑制劑耐受的表達突變激酶的細胞系，都表現(xiàn)出有效的細胞毒性。[3] Ganetespib治療快速引起已知的Hsp90受體蛋白降解，表現(xiàn)出高于ansamycin抑制劑17-AAG的效能，并且在較短的暴露時間下也具有持續(xù)的活性。[3]在另一個研究中，Ganetespib誘導惡性犬肥大細胞系凋亡。Ganetespib在非常低的濃度下，有效作用于C2和BR犬惡性肥大細胞，IC50分別為19和4 nM，而17-AAG抑制C2和BR犬惡性肥大細胞的IC50分別為958和44 nM。[4]100 nM Ganetespib處理24小時后，所有處理過的細胞系，包括C2和BMCMCs細胞中WT和突變型Kit的表達被下調(diào)。然而，Ganetespib處理后不影響PI3K或HSP90的表達。[4]
細胞實驗 細胞系 OSA細胞
濃度 0.001-1μM
孵育時間 5天
方法 將1.5 × 103 OSA細胞接種于96孔板，在包含10%血清的完全培養(yǎng)基中培養(yǎng)過夜，以測定50%抑制濃度。板在第5天采集，隨后用0.001，0.005，0.01，0.05，0.1，0.5和1 μM Ganetespib處理并分析。熒光測量使用酶標儀在485 nm激發(fā)波長和530 nm發(fā)射檢測波長下進行。相對細胞數(shù)以對照孔的百分比計算：樣品吸光度/DMSO處理的細胞吸光度× 100。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot EGFR / c-Met / IGF-1Rβ/ Akt / p-Akt / ERK / p-ERK

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