| Company Name: |
Shanghai Topbiochem Technology Co., Ltd
|
| Tel: |
021-58170097 |
| Email: |
info@topbiochem.com |
| Products Intro: |
Product Name:17-AAG hydrochloride
CAS:911710-03-7
Purity:98% Package:25g;100g;500g;1kg
|
| Company Name: |
Haoyuan Chemexpress Co., Ltd.
|
| Tel: |
021-58950125 |
| Email: |
info@chemexpress.com |
| Products Intro: |
Product Name:17-AAG (Hydrochloride)
CAS:911710-03-7
Purity:>98% Package:700RMB/10mg
|
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Email: |
info@musechem.com |
| Products Intro: |
Product Name:17-AAG Hydrochloride
CAS:911710-03-7
Purity:>98% HPLC Package:10mg;100mg;1g Remarks:Reagent Grade
|
|
| | 17-AAG (Hydrochloride) Basic information |
| Product Name: | 17-AAG (Hydrochloride) | | Synonyms: | 17-AAG (Hydrochloride);CP 127374 Hydrochloride;NSC 330507 Hydrochloride;TanespiMycin Hydrochloride;17-(Allylamino)-17-desmethylgeldanamycin hydrochloride;Tanespimycin (17-AAG) HCl;Tanespimycin (17-AAG) hydrochloride;TANESPIMYCIN HYDROCHLORIDE;NSC 330507 HYDROCHLORIDE;CP 127374 HYDROCHLORIDE;17AAG HYDROCHLORIDE;17 AAG HYDROCHLORIDE | | CAS: | 911710-03-7 | | MF: | C31H44ClN3O8 | | MW: | 622.16 | | EINECS: | | | Product Categories: | | | Mol File: | 911710-03-7.mol |  |
| | 17-AAG (Hydrochloride) Chemical Properties |
| solubility | Soluble in DMSO | | form | Powder |
| | 17-AAG (Hydrochloride) Usage And Synthesis |
| Description | 17-AAG Hydrochloride is a potent HSP90 inhibitor with IC50 of 5 nM, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. | | in vitro | In Vitro:17-AAG causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. 17-AAG inhibits prostate cancer cell lines with IC50s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)[1]. Combination of 17-AAG (10 nM) and Trastuzumab induces more effective ErbB2-degradation. 17-AAG (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. 17-AAG inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP[3]. | | in vivo | In Vivo:17-AAG (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. 17-AAG treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity[1]. 17-AAG (60 mg/kg) with paclitaxel (60 mg/kg) and rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth far more potently than paclitaxel-containing micelles and effected tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4]. | | References | References:[1]. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993.
[2]. Raja, Srikumar M., et al. A combination of Trastuzumab and 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163
[3]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7.
[4]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29.
[5]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10. |
| | 17-AAG (Hydrochloride) Preparation Products And Raw materials |
|