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Formula | C31H43N3O8 |
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Molecular Weight | 585.69 | CAS No. | 75747-14-7 | ||||
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (170.73 mM) | ||||
Ethanol | 10 mg/mL (17.07 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3. | ||
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Targets |
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In vitro | 17-AAG, an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. [1] 17-AAG causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. [2] In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, 17-AAG has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants. [3] | ||
In vivo | 17-AAG displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. [1] Administration of 17-AAG (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively. [2] | ||
Features | Displays very low toxicity toward normal cells. |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[2] |
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Data from [Data independently produced by Mol Cancer, 2014, 13, 150]
Data from [Data independently produced by Oncotarget, 2014, 5, 4269-82]
Data from [Mol Cell Biol, 2013, 33(12), 2375-87]
Data from [Age, 2013, 35, 549-62]
Amyloid aggregates induced by the p53-R280T mutation lead to loss of p53 function in nasopharyngeal carcinoma [ Cell Death Dis, 2024, 15(1):35] | PubMed: 38212344 |
RIOK3 sustains colorectal cancer cell survival under glucose deprivation via an HSP90α-dependent pathway [ Oncogenesis, 2024, 13(1):12] | PubMed: 38453884 |
HSP90 inhibition suppresses tumor glycolytic flux to potentiate the therapeutic efficacy of radiotherapy for head and neck cancer [ Sci Adv, 2024, 10(8):eadk3663] | PubMed: 38394204 |
Albumosomes formed by cytoplasmic pre-folding albumin maintain mitochondrial homeostasis and inhibit nonalcoholic fatty liver disease [ Signal Transduct Target Ther, 2023, 8(1):229] | PubMed: 37321990 |
The molecular and functional landscape of resistance to immune checkpoint blockade in melanoma [ Nat Commun, 2023, 14(1):1516] | PubMed: 36934113 |
FACS-based genome-wide CRISPR screens define key regulators of DNA damage signaling pathways [ Mol Cell, 2023, 83(15):2810-2828.e6] | PubMed: 37541219 |
Mutant p53-ENTPD5 control of the calnexin/calreticulin cycle: a druggable target for inhibiting integrin-α5-driven metastasis [ J Exp Clin Cancer Res, 2023, 42(1):203] | PubMed: 37563605 |
Steppogenin suppresses tumor growth and sprouting angiogenesis through inhibition of HIF-1α in tumors and DLL4 activity in the endothelium [ Phytomedicine, 2023, 108:154513] | PubMed: 36332389 |
Proteomics Profiling Reveals the Molecular Signatures and Potential Therapeutic Targets of Human Nasopharyngeal Carcinoma [ Mol Cell Proteomics, 2023, 22(6):100567] | PubMed: 37172717 |
Inhibition of HSP90 in Driver Oncogene-Defined Lung Adenocarcinoma Cell Lines: Key Proteins Underpinning Therapeutic Efficacy [ Int J Mol Sci, 2023, 24(18)13830] | PubMed: 37762133 |
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