Ganetespib (STA-9090)

製品コード：S1159 純度：99.97%

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.

CAS No. 888216-25-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 52000	国内在庫あり
5mg	JPY 40500	国内在庫あり
50mg	JPY 145500	国内在庫あり
1g	JPY 748500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（67）

製品安全説明書

現在のバッチを見る：純度： 99.97%

99.97

Ganetespib (STA-9090)関連製品

関連ターゲット	HSP40 HSP70 HSP90 HSP105 HSF1	もっと見る
関連製品	Tanespimycin (17-AAG) Luminespib (NVP-AUY922) Elesclomol (STA-4783) Alvespimycin (17-DMAG) HCl VER155008 BIIB021 Onalespib (AT13387) NVP-BEP800 KRIBB11 SNX-2112 HA15 Zelavespib (PU-H71) HSP990 (NVP-HSP990) NMS-E973 Apoptozole XL888 PF-04929113 (SNX-5422) KNK437 Teprenone TRC051384 VER-50589 Rocaglamide VER-49009 Pimitespib (TAS-116) JG98 DTHIB KW-2478	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Angiogenesis Related compound Library TGF-beta/Smad compound library Cytoskeletal Signaling Pathway Compound Library Anti-Cardiovascular Disease Compound Library	もっと見る

シグナル伝達経路

HSP (HSP90)シグナル伝達経路

HSP (HSP90)阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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

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.

Targets

HSP90 ^[1]
(OSA 8 cells)

4 nM

In Vitro
In vitro	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]
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	EGFR / c-Met / IGF-1Rβ/ Akt / p-Akt / ERK / p-ERK p27(Kip1) / p21 (Cip1) / Cyclin D1 / Cyclin E / Cyclin B1 / CDK1 / CDK2 / CDK4 Survivin / Bcl-2 / Bcl-xl / Mcl-1 B-RAF / C-RAF / N-RAS HER2 / p-STAT3 / BIM CDK1 / Cyclin D1 / Cyclin B1 / p27 c-PARP / c-caspase 3 / caspase 8 / c-caspase 8 / caspase 9 / c-caspase 9 ErbB2 / pErbB2 / Src / pSrc / mTOR / pmTOR / Bad / pBad / GSK3 / pGSK3 Wee1 / p-Wee1 / Chk1 / p-Chk1		23418523
	Growth inhibition assay	Cell viability		23418523

In Vivo
In Vivo	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]
動物実験	動物モデル	Female severe combined immune-deficient (SCID) mice
	投与量	25 mg/kg/day for 3 days
	投与経路	Tail vein injection

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02192541	Terminated	Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	December 2 2014	Phase 1
NCT02008877	Completed	Malignant Peripheral Nerve Sheath Tumors (MPNST)\|Sarcoma	Sarcoma Alliance for Research through Collaboration\|Synta Pharmaceuticals Corp.\|United States Department of Defense	December 2013	Phase 1\|Phase 2

参考
[1] McCleese Jk, et al. Int J Cancer. 2009, 125(12), 2792-2801. [2] Wang Y, et al. Curr Opin Investig Drugs. 2010 , 11(12), 1466-1476. [3] Ying W, et al. Mol Cancer Ther. 2012, 11(2), 475-484. [4] Lin TY, et al. Exp Hematol. 2008, 36(10), 1266-1277. + 展開

参考

[4] Lin TY, et al. Exp Hematol. 2008, 36(10), 1266-1277.

+ 展開

化学情報

分子量	364.4	化学式	C₂₀H₂₀N₄O₃
CAS No.	888216-25-9	SDF	Download Ganetespib (STA-9090) SDFをダウンロードする
Smiles	CC(C)C1=C(C=C(C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)O)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 40 mg/mL ( (109.76 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 9 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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

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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/

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):