Ganetespib Inhibitor CAS No. 888216-25-9

Cat. No.	Name	Size	Price
KI0115	Ganetespib	5 mg	$340
	Ganetespib	10 mg	$555.4
	Ganetespib	50 mg	$1731.52
	Ganetespib	200 mg	$3724

Chemical Characteristic

Product Name	Ganetespib
Synonyms	STA-9090
CAS No.	888216-25-9
Molecular Weight	364.4
Formula	C₂₀H₂₀N₄O₃
Chemical Name	5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one
Smiles	n1nc(n(c1O)c1cc2ccn(c2cc1)C)c1c(cc(c(c1)C(C)C)O)O
Chemical Structure
Documents	HPLC MS COA

Biological activities

Ganetespib is a novel small molecule heat shock protein 90 (Hsp90) inhibitor with an IC50 of 4 nM in osteosarcoma (OSA) 8 cells. ^[1] Ganetespib inhibits JAK2-mediated signal transduction and proliferation in hematological cancers. Ganetespib abrogates JAK/signal transducers and activators of transcription (STAT) signaling in solid tumors. Ganetespib possesses decided advantages over JAK-specific inhibitors for controlling STAT-driven malignancies. Ganetespib treatment also selectively alters the expression of a large set of genes involved in cell cycle-related activities, including DNA replication and repair, cell cycle regulation, centrosome/spindle activities, chromosome condensation, and replication.^[2] Ganetespib induces apoptosis and inhibits the proliferation of a panel NSCLC cell lines with a median IC50 of 8.75 nM. Ganetespib induces BaF3 cell lines cytotoxicity with an average IC50 of 9.9 nM. In addition, ganetespib reduces cell viability in a chemosensitive H69 SCLC cell line and a multidrug-resistant variant of H69, H69AR with IC50 of 8 and 7 nM, respectively. Ganetespib potently inhibits the growth of solid tumor and hematological cancer cell lines, including MDA-MB-231 (breast cancer), DU145 (prostate cancer) and HEL9217 (human erythroleukemia). Ganetespib induces HEL9217 cell death with an IC50 of 20 nM and reduces cell viability with an IC50 of 15 nM. Ganetespib potently inhibits the proliferation and induces cell death of gastrointestinal stromal tumor (GIST) cell lines with IC50 ranging from 20 to 40 nM. Ganetespib demonstrates superior growth inhibition and apoptosis induction in C2 and BR cell lines, with IC50 of 19 and 4 nM, respectively. Ganetespib at 50 or 250 nM arrests HEL9217 cells in G1 and G2 phase and significantly reduces the length of the S phase. ^[3] In vivo, ganetespib?? coordinate impact on both cell growth and cell division results in potent antitumor activity in JAK/STAT-driven models of human leukemia. ^[2] In vivo, in mouse xenograft models bearing tumors developed by implantation of human MV411, Kasumil and K562 acute myeloid leukemia cell lines, ganetespib (25 mg/kg iv, five doses per week) treatment significantly attenuates tumor growths compared with vehicle controls. ^[3]

Protocols

Ganetespib is dissolved in DMSO, aliquoted and stored at -20°C. ^[2]

References

[1] McCleese JK, et al. The novel HSP90 inhibitor STA-1474 exhibits biologic activity against osteosarcoma cell lines. Int J Cancer. 2009, 125(12): 2792-2801. [2] Proia DA, et al. Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090) in cancer cells with activated JAK/STAT signaling. PLoS One. 2011, 6(4): e18552. [3] Wang Y, et al. STA-9090, a small-molecule Hsp90 inhibitor for the potential treatment of cancer. Curr Opin Investig Drugs. 2010, 11(12): 1466-1476.

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