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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 | 117 mg/mL (199.76 mM) | |
Ethanol | 5 mg/mL (8.53 mM) | |||
Water | Insoluble | |||
* <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 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] |
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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] |
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Features | Displays very low toxicity toward normal cells. |
Kinase Assay: |
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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]
Pan-cancer proteogenomics expands the landscape of therapeutic targets [ Cell, 2024, S0092-8674(24)00583-X] | PubMed: 38917788 |
Pan-cancer proteogenomics expands the landscape of therapeutic targets [ Cell, 2024, S0092-8674(24)00583-X] | PubMed: 38917788 |
The HSP90 inhibitor HVH-2930 exhibits potent efficacy against trastuzumab-resistant HER2-positive breast cancer [ Theranostics, 2024, 14(6):2442-2463] | PubMed: 38646654 |
The HSP90 inhibitor HVH-2930 exhibits potent efficacy against trastuzumab-resistant HER2-positive breast cancer [ Theranostics, 2024, 14(6):2442-2463] | PubMed: 38646654 |
Caspase-2 protects against ferroptotic cell death [ Cell Death Dis, 2024, 15(3):182] | PubMed: 38429264 |
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 |
Up-regulation of HSP90α in HDM-induced asthma causes pyroptosis of airway epithelial cells by activating the cGAS-STING-ER stress pathway [ Int Immunopharmacol, 2024, 131:111917] | PubMed: 38527402 |
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 |
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