Onalespib lactate
Based on 11 publication(s) in Google Scholar
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC).
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- CAS 番号: 1019889-35-0
- 分子式: C27H37N3O6
- 分子量:499.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Onalespib lactate
More- Theranostics. 2019 Aug 12;9(20):5769-5783. [Abstract]
- Nano Res. 07 May 2022.
- Immunology. 2021 Jan;162(1):84-91. [Abstract]
- Sci Rep. 2017 Mar 15;7(1):201. [Abstract]
- J Appl Toxicol. 2017 Nov;37(11):1325-1332. [Abstract]
- Prostate. 2022 Jun;82(8):917-932. [Abstract]
- J Labelled Comp Radiopharm. 2025 Apr;68(4):e4144. [Abstract]
- Research Square Preprint. 2024 Oct 10.
- Research Square Print. December 12th, 2022.
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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Histological Imaging/Staining
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Bio/Physico-chemical Assay
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Apoptosis Analysis
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
生物活性
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HSP90 0.71 nM (Kd) |
Onalespib lactate (0-0.4 µM; 72 h, 48 h) inhibits the proliferation, survival and migration of glioma cells[2].
Onalespib lactate (0-0.4 µM; 48 h) decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LN229, U251 and A172 cells
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Concentration:0.1, 0.2, 0.4 µM
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Incubation Time:72 h
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Result:Inhibited cell proliferation in a dose-dependent manner.
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Cell Line:LN229, U251 and A172 cells
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Concentration:0.1, 0.2, 0.4 µM
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Incubation Time:48 h
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Result:Decreased the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner.
Onalespib lactate (0.5 µM; from 5 to 10 days post-transplant) and TMZ (10 µM) reduce tumor growth and extend survival in zebrafish embryos[2].
Onalespib lactate (5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts; i.p.; daily for 3 days) shows anti-tumor activity in HCT116 and A431 xenografts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nu/nu Balb/c mice (HCT116 and A431 xenografts)[3]
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Dosage:5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts
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Administration:I.p.; on day 1, 2, and 3 days
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Result:Inhibited tumor growth and had a median survival of 9.5 days and the maximum survival was 14 days in HCT116 xenografts, reduced the tumor size significantly by 32% in A431 xenografts.
化学情報
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CAS 番号 1019889-35-0
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分子量 499.60
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分子式 C27H37N3O6
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SMILES
C[C@H](O)C(O)=O.O=C(N1CC2=C(C=C(CN3CCN(C)CC3)C=C2)C1)C4=CC(C(C)C)=C(O)C=C4O
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別名
AT13387 lactate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (11)
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Journal Impact Factor
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Most Recent
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Theranostics
Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]2019 Aug 12;9(20):5769-5783. PMID: 31534518 -
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Immunology
2021 Jan;162(1):84-91. PMID: 32954500 -
Sci Rep
Proteomic analysis of proteome and histone post-translational modifications in heat shock protein 90 inhibition-mediated bladder cancer therapeutics. [Abstract]2017 Mar 15;7(1):201. PMID: 28298630
Onalespib lactate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201. [Abstract]
5637 and SV-HUC cells (1 × 104 per well) were evenly distributed in 96-well plates overnight. Cells were incubated with AUY922 (10 nM), ganetespib (10 nM), SNX2112 (100 nM), or AT13387 (Onalespib) (100 nM) for 48 h. For the caspase 3/7 assay, the HSP90 inhibitor-treated 5637 or SV-HUC cells are stained with Nexcelom ViaStain Caspase 3/7 reagent and Hoechst 33342. Caspase 3/7 positive cells are identified using the Celigo imaging cytometer, and the percentage of apoptotic caspase 3/7 positive cells is calculated with the Celigo software.
Onalespib lactate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201. [Abstract]
Heat shock protein 90 (HSP90) inhibitors suppress cell growth and proliferation in human bladder carcinoma cells. 5637 cells were evenly distributed in 96-well plates (5 × 103 cells/well) and treated for 72 h with AUY922, ganetespib (STA9090), SNX2112, AT13387 (Onalespib), or CUDC395 at the indicated concentrations. The ability of HSP90 inhibitors to inhibit cell growth and proliferation was determined by the MTS assay.
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J Appl Toxicol
2017 Nov;37(11):1325-1332. PMID: 28543094
Onalespib lactate purchased from MedChemExpress. Usage Cited in: J Appl Toxicol. 2017 Nov;37(11):1325-1332. [Abstract]
Alleviation of graphene toxicity by using chemical inhibitors (Onalespib (AT13387 et al; 20 nM pretreatment 2 h)) after 48 h exposure of NRK-52E cells with graphene (50 μg/ml). Quantification of TUNEL-positive cells in NRK-52E cells treated with graphene in the presence of chemical inhibitors for HO-1, HSP90, caspase 3, DNase I and EndoG (p < 0.01 for all bars vs. Gn).
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Prostate
Diptoindonesin G antagonizes AR signaling and enhances the efficacy of antiandrogen therapy in prostate cancer. [Abstract]2022 Jun;82(8):917-932. PMID: 35322879 -
J Labelled Comp Radiopharm
Radiosynthesis and Evaluation of [18F]FEHSP990 as Novel PET Tracer for Hsp90 PET Imaging. [Abstract]2025 Apr;68(4):e4144. PMID: 40219580
Onalespib lactate purchased from MedChemExpress. Usage Cited in: J Labelled Comp Radiopharm. 2025 Apr;68(4):e4144. [Abstract]
In vitro autoradiography study. Slices were incubated with [18F]FEHSP990 (11 kBq/mL). Binding specificity was assessed by preincubation with authentic reference compound (FEHSP990), homologous (HSP990) and heterologous (Onalespib, PU‐H71) inhibitors (10 μM; 10 min) at RT. Rat brain slices (n = 3 per preincubation condition) and U87 tumour slices (n = 3 per preincubation condition).
Onalespib lactate purchased from MedChemExpress. Usage Cited in: J Labelled Comp Radiopharm. 2025 Apr;68(4):e4144. [Abstract]
In vitro cell binding study. U87 cells were incubated with [18F]FEHSP990 (84 kBq/mL). Binding specificity was assessed by preincubation with homologous (HSP990) and heterologous (Onalespib, PU‐H71) inhibitors (100 μM; 60 min) at 37°C (n = 3 per preincubation condition).
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
Methods Mol Biol
2018:1711:351-398. PMID: 29344898
純度とドキュメンテーション
参考文献
[1]. Riess JW, et al. Erlotinib and Onalespib Lactate Focused on EGFR Exon 20 Insertion Non-Small Cell Lung Cancer (NSCLC): A California Cancer Consortium Phase I/II Trial (NCI 9878). Clin Lung Cancer. 2021 Nov;22(6):541-548. [Content Brief]
[2]. Canella A, et al. Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas. Clin Cancer Res. 2017 Oct 15;23(20):6215-6226. [Content Brief]
[3]. Spiegelberg D, et al. The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach. Sci Rep. 2020 Apr 3;10(1):5923. [Content Brief]
[4]. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53(16):5956-69. [Content Brief]
Calculators
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Onalespib lactate 関連分類
HY-113916 関連分類
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