Creative Biolabs

17-AAG [Hsp90 Inhibitor]

[CAT#: MOD2005ZP66]

Selective Hsp90 inhibitor. Also protects neuroprogenitor cells against apoptosis.

Target:
HSP90 alpha

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Description
Selective Hsp90 inhibitor. potent, less toxic geldanamycin analogue. It also an inhibitor of telomerase activity. Show anti-tumor activity and induce apoptosis. It also protect neural progenitor cells from apoptosis.
Synonyms
Tanespimycin
Chemical Name
17-Demethoxy-17-(2-propenylamino)geldanamycin
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
Tanespimycin leads to the degradation of HER2, Akt and mutant and wild-type AR and prostate cancer cell-dependent G1 growth arrest in retinoblastoma. Tanespimycin inhibits prostate cancer cell lines with an IC50 range of 25-45 nM (LNCaP is 25 nM; LAPC-4 is 40 nM; DU-145 is 45 nM; PC-3 is 25 nM) [1]. Tanespimycin (0.1-1 μM) induces almost complete ErbB2 loss on breast cancer cells overexpressing ErbB2 [2]. Tanespimycin inhibits cell growth and induces GCA/M cell cycle arrest and apoptosis in CCA cells, while down-regulating Bcl-2, Survivin and Cyclin B1 and up-regulating lytic PARP [3].
Reference
[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. 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.
Assay Description
Tanespimycin (25-200 mg/kg, i.p.) caused a dose-dependent decrease in the expression of AR, HER2 and Akt in prostate cancer xenografts. Tennisin treatment at a dose sufficient to induce AR, HER2 and Akt degradation can dose-dependently inhibit the growth of androgen-dependent and independent prostate cancer xenografts [1]. Paeoniomycin (60 mg/kg) and rapamycin (30 mg/kg) inhibit the growth of A549 and MDA-MB-231 tumors of M549-MDA-MB-231 tumor-bearing animals and cure the tumor by tail vein injection [ 2].
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]. 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.
Molecular Weight
585.7
Form
Powder
Chemical Formula
C31H43N3O8
Source
Synthetic
SMILES
CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)C)OC)OC(=O)N)C)C)O)OC
Solubility
Soluble in DMSO (100 mM)
IC50
5 nM
CAS NO.
75747-14-7
PubChem Substance ID
433449
Purity
>98%
Storage
-20°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.
Research Use Only
For research use only
Target
HSP90 alpha
Official Name
Hsp90
Full Name
heat shock protein 90
Alternative Names
HATPase
Gene ID
3326(Human); 15516(Mouse); 301252(Rat)
Uniprot ID
P08238(Human); P11499(Mouse); P34058(Rat)

For Research Use Only. Not For Clinical Use.
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