Ganetespib - CAS 888216-25-9
Catalog number:
888216-25-9
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H20N4O3
Molecular Weight:
364.40
COA:
Inquire
Targets:
Hsp90 | HSP
Description:
Ganetespib, also known as STA-9090, is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional Hsp90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.
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Brife Description:
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.
Purity:
>98%
Appearance:
White solid powder
Synonyms:
STA-9090;   STA 9090; STA9090
Solubility:
DMSO > 40 mg/mL
Storage:
3 years -20oC powder, 6 months-80oC in solvent.
MSDS:
Inquire
Quality Standard:
In-house
Quantity:
Grams-Kilos
InChIKey:
MWTUOSWPJOUADP-XDJHFCHBSA-N
InChI:
InChI=1S/C20H20N4O3/c1-11(2)14-9-15(18(26)10-17(14)25)19-21-22-20(27)24(19)13-4-5-16-12(8-13)6-7-23(16)3/h4-11,21,25H,1-3H3,(H,22,27)/b19-15+
Canonical SMILES:
CC(C)C1=CC(=C2NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)C(=O)C=C1O
Current Developer:
Synta
1.A phase II trial of ganetespib, a heat shock protein 90 Hsp90) inhibitor, in patients with docetaxel-pretreated metastatic castrate-resistant prostate cancer (CRPC)-a prostate cancer clinical trials consortium (PCCTC) study.
Thakur MK1, Heilbrun LK1, Sheng S1, Stein M2, Liu G3, Antonarakis ES4, Vaishampayan U1, Dzinic SH1, Li X1, Freeman S1, Smith D1, Heath EI5. Invest New Drugs. 2016 Feb;34(1):112-8. doi: 10.1007/s10637-015-0307-6. Epub 2015 Nov 18.
Introduction Heat shock protein 90 (Hsp90) has been studied as a therapeutic target in many cancers. In preclinical trials, the Hsp90 ATPase inhibitor ganetespib demonstrated potent inhibition of solid tumor growth, with superior potency than prior Hsp90 inhibitors. Given the promising preclinical outcome and favorable pharmacologic properties of ganetespib, we conducted a phase II trial of single-agent ganetespib in patients with metastatic, castrate-resistant prostate cancer (mCRPC). The primary objective of the study was to determine the 6-month progression-free survival (PFS) rate. Methods Patients with mCRPC who had been previously treated with docetaxel were enrolled after meeting eligibility criteria. All patients received ganetespib at 200 mg/m(2) on days 1, 8, and 15 of every 28 days (one cycle). Subjects who tolerated therapy were continued on ganetespib until disease progression. Considering that Hsp90 acetylation may confer insensitivity to Hsp90 inhibitors and maspin inhibits protein deacetylation, maspin-associated molecular markers were evaluated.
2.Targeting the Janus-activated kinase-2-STAT3 signalling pathway in pancreatic cancer using the HSP90 inhibitor ganetespib.
Nagaraju GP1, Mezina A1, Shaib WL1, Landry J2, El-Rayes BF3. Eur J Cancer. 2016 Jan;52:109-19. doi: 10.1016/j.ejca.2015.10.057. Epub 2015 Dec 9.
BACKGROUND: Pancreatic cancer (PC) is an aggressive malignancy characterised by chemoresistance. HSP90 is important for stabilisation of proteins, cell signalling and malignant growth. We hypothesised that ganetespib, an HSP90 inhibitor, can inhibit PC cell growth by interfering with multiple signalling cascades, including the Janus-activated kinase (JAK)-STAT pathway, and act synergistically with chemotherapeutic drugs.
3.Ganetespib: research and clinical development.
Jhaveri K1, Modi S1. Onco Targets Ther. 2015 Jul 24;8:1849-58. doi: 10.2147/OTT.S65804. eCollection 2015.
Under stressful conditions, the heat shock protein 90 (HSP90) molecular chaperone protects cellular proteins (client proteins) from degradation via the ubiquitin-proteasome pathway. HSP90 expression is upregulated in cancers, and this contributes to the malignant phenotype of increased proliferation and decreased apoptosis and maintenance of metastatic potential via conservation of its client proteins, including human epidermal growth factor receptor 2, anaplastic lymphoma kinase, androgen receptor, estrogen receptor, Akt, Raf-1, cell cycle proteins, and B-cell lymphoma 2 among others. Hence, inhibition of HSP90 leads to the simultaneous degradation of its many clients, thereby disrupting multiple oncogenic signaling cascades. This has sparked tremendous interest in the development of HSP90 inhibitors as an innovative anticancer strategy. Based on the wealth of compelling data from preclinical studies, a number of HSP90 inhibitors have entered into clinical testing.
4.Ganetespib radiosensitization for liver cancer therapy.
Chettiar ST1, Malek R1, Annadanam A1, Nugent KM1, Kato Y2,3, Wang H1, Cades JA1, Taparra K1,4, Belcaid Z5, Ballew M1, Manmiller S1, Proia D6, Lim M3,5, Anders RA7, Herman JM1,3, Tran PT1,3,4,8. Cancer Biol Ther. 2016 Apr 2;17(4):457-66. doi: 10.1080/15384047.2016.1156258.
Therapies for liver cancer particularly those including radiation are still inadequate. Inhibiting the stress response machinery is an appealing anti-cancer and radiosensitizing therapeutic strategy. Heat-shock-protein-90 (HSP90) is a molecular chaperone that is a prominent effector of the stress response machinery and is overexpressed in liver cancer cells. HSP90 client proteins include critical components of pathways implicated in liver cancer cell survival and radioresistance. The effects of a novel non-geldanamycin HSP90 inhibitor, ganetespib, combined with radiation were examined on 3 liver cancer cell lines, Hep3b, HepG2 and HUH7, using in vitro assays for clonogenic survival, apoptosis, cell cycle distribution, γH2AX foci kinetics and client protein expression in pathways important for liver cancer survival and radioresistance. We then evaluated tumor growth delay and effects of the combined ganetespib-radiation treatment on tumor cell proliferation in a HepG2 hind-flank tumor graft model.
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CAS 888216-25-9 Ganetespib

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