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Alvespimycin

(Synonyms: 17-DMAG; KOS-1022; NSC 707545)

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Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC₅₀ of 62 nM.

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Pureté: 99.52%
CAS No.: 467214-20-6
Formule: C₃₂H₄₈N₄O₈
Masse moléculaire:616.75

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Alvespimycin Chemical Structure

CAS No.: 467214-20-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (16)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC₅₀ of 62 nM.

IC₅₀ & Target^[1]

HSP90

62 nM (EC₅₀)

GRP94

65 nM (EC₅₀)

Voir tous les produits spécifiques à Isoform HSP :

Cellular Effect

Cell Line	Type	Value	Description	References
A2058	EC₅₀	7.9 nM Compound: 17-DMAG	Inhibition of Hsp90 in human A2058 cells Inhibition of Hsp90 in human A2058 cells	[PMID: 18929486]
A2058	IC₅₀	2.1 nM Compound: 17-DMAG	Cytotoxicity against human A2058 cells by MTT assay Cytotoxicity against human A2058 cells by MTT assay	[PMID: 18929486]
A2058	IC₅₀	24.3 nM Compound: 17-DMAG	Inhibition of Hsp90 in human A2058 cells assessed as Akt degradation Inhibition of Hsp90 in human A2058 cells assessed as Akt degradation	[PMID: 18929486]
A549	IC₅₀	68 nM Compound: 1e, 17-DMAG	Cytotoxicity against human A549 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human A549 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
AGS	IC₅₀	0.0036 μM Compound: page 2621, table 2 footnote	Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay	[PMID: 18359631]
AGS	IC₅₀	0.036 μM Compound: 17-DMAG	Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay	[PMID: 17583950]
AGS	IC₅₀	16 μM Compound: 17-DMAG	Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay	[PMID: 17583950]
AGS	IC₅₀	16 μM Compound: page 2621, table 2 footnote	Cytotoxicity against human AGS cells by MTT assay Cytotoxicity against human AGS cells by MTT assay	[PMID: 18359631]
BT-549	IC₅₀	17.1 μM Compound: 47; 17-DMAG	Anticancer activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Anticancer activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 33650861]
CCRF-CEM	IC₅₀	2500 nM Compound: 1e, 17-DMAG	Cytotoxicity against human paclitaxel-resistant CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay Cytotoxicity against human paclitaxel-resistant CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay	[PMID: 19405528]
CCRF-CEM	IC₅₀	540 nM Compound: 1e, 17-DMAG	Cytotoxicity against human CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay Cytotoxicity against human CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay	[PMID: 19405528]
HCT-116	IC₅₀	0.05 μM Compound: 36, 17-DMAG	Cytotoxicity against human HCT116 cells by Alamar blue assay Cytotoxicity against human HCT116 cells by Alamar blue assay	[PMID: 20662534]
HCT-116	IC₅₀	0.78 μM Compound: 17-DMAG	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTT assay	[PMID: 24582477]
HCT-116	IC₅₀	1.21 μM Compound: 17-DMAG	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 24763261]
HCT-116	IC₅₀	57 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against human HCT116 cells after 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs	[PMID: 19231864]
HeLa	IC₅₀	0.15 μM Compound: page 2621, table 2 footnote	Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells	[PMID: 18359631]
HeLa	IC₅₀	2.06 μM Compound: page 2621, table 2 footnote	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 18359631]
Hep 3B2	IC₅₀	>30 μM Compound: 17-DMAG	Inhibition of hypoxia-induced HIF1 activation in human Hep3B cells by pGL3-HRE-luciferase reporter gene assay Inhibition of hypoxia-induced HIF1 activation in human Hep3B cells by pGL3-HRE-luciferase reporter gene assay	[PMID: 19072214]
Hep 3B2	IC₅₀	>50 μM Compound: 17-DMAG	Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay	[PMID: 17583950]
Hep 3B2	IC₅₀	0.057 μM Compound: 17-DMAG	Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis	[PMID: 20469887]
Hep 3B2	IC₅₀	0.061 μM Compound: 17-DMAG	Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay	[PMID: 17583950]
Hep 3B2	IC₅₀	0.079 μM Compound: 17-DMAG	Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA	[PMID: 20469887]
Hep 3B2	IC₅₀	57.2 nM Compound: 17-DMAG	Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis	[PMID: 19072214]
Hep 3B2	IC₅₀	79.5 nM Compound: 17-DMAG	Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA	[PMID: 19072214]
Hs-578T	IC₅₀	8.4 nM Compound: 47; 17-DMAG	Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 33650861]
Huh-7	EC₅₀	1.2 nM Compound: 17-DMAG	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis	[PMID: 18936191]
Huh-7	EC₅₀	3.1 nM Compound: 17-DMAG	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis	[PMID: 18936191]
MCF7	IC₅₀	0.39 μM Compound: 17-DMAG	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by MTT assay	[PMID: 24582477]
MCF7	IC₅₀	0.5 μM Compound: 17-DMAG	Anti-cancer activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay Anti-cancer activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay	[PMID: 39042910]
MCF7	IC₅₀	0.8 μM Compound: 17-DMAG	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 24763261]
MCF7	IC₅₀	230 nM Compound: 1e, 17-DMAG	Cytotoxicity against human MCF7 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human MCF7 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
MCF7	IC₅₀	71 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against human MCF7 cells after 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs	[PMID: 19231864]
MCF7	IC₅₀	862 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
MDA-MB-231	IC₅₀	17.6 nM Compound: 17-DMAG	Inhibition of Hsp90 in human MDA-MB-231 cells assessed as Akt degradation Inhibition of Hsp90 in human MDA-MB-231 cells assessed as Akt degradation	[PMID: 18929486]
MDA-MB-231	IC₅₀	4.5 nM Compound: 17-DMAG	Inhibition of Hsp90 in human MDA-MB-231 cells assessed as her2 degradation Inhibition of Hsp90 in human MDA-MB-231 cells assessed as her2 degradation	[PMID: 18929486]
MDA-MB-231	IC₅₀	45.7 μM Compound: 47; 17-DMAG	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 33650861]
MDA-MB-231	IC₅₀	5.8 nM Compound: 17-DMAG	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	[PMID: 18929486]
MDA-MB-468	IC₅₀	1600 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs	[PMID: 19231864]
NCI-H1299	IC₅₀	0.1 μM Compound: 1c, DMAG	Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay	[PMID: 21438541]
NCI-H596	IC₅₀	1100 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs	[PMID: 19231864]
NCI-N87	EC₅₀	62 nM Compound: 17-DMAG	Antitumor activity against human NCI-N87 cells assessed as reduction in cell growth Antitumor activity against human NCI-N87 cells assessed as reduction in cell growth	[PMID: 38232464]
PC-9	IC₅₀	0.01 μM Compound: 3; 17-DMAG	Cytotoxicity against HGF-induced erlotinib-resistant human PC9 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against HGF-induced erlotinib-resistant human PC9 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 26844689]
SK-BR-3	EC₅₀	4 nM Compound: 4b, 17-DMAG	Upregulation of Hsp70 in SKBR3 cells Upregulation of Hsp70 in SKBR3 cells	[PMID: 16854066]
SK-BR-3	EC₅₀	8 nM Compound: 4b, 17-DMAG	Degradation of Her2 in SKBR3 cells Degradation of Her2 in SKBR3 cells	[PMID: 16854066]
SK-BR-3	GI₅₀	29 nM Compound: 4b, 17-DMAG	Inhibition of human SKBR3 cell growth Inhibition of human SKBR3 cell growth	[PMID: 16854066]
SK-BR-3	IC₅₀	1.34 μM Compound: 17-DMAG	Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell viability after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell viability after 48 hrs by MTT assay	[PMID: 24582477]
SK-BR-3	IC₅₀	230 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
SK-BR-3	IC₅₀	24 nM Compound: 1e, 17-DMAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
SK-BR-3	IC₅₀	24 nM Compound: 1	Cytotoxicity against SKBr3 cells Cytotoxicity against SKBr3 cells	[PMID: 16165354]
SK-BR-3	IC₅₀	24 nM Compound: 3, 17-DMAG	Binding affinity to Hsp90 in human SKBR3 cells Binding affinity to Hsp90 in human SKBR3 cells	[PMID: 19017562]
SK-BR-3	IC₅₀	3.11 μM Compound: 17-DMAG	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 24763261]
SK-BR-3	IC₅₀	58 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against human SKBR3 cells after 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs	[PMID: 19231864]
SK-OV-3	EC₅₀	14 nM Compound: 4b, 17-DMAG	Upregulation of Hsp70 in SKOV3 cells Upregulation of Hsp70 in SKOV3 cells	[PMID: 16854066]
SK-OV-3	EC₅₀	46 nM Compound: 4b, 17-DMAG	Degradation of Her2 in SKOV3 cells Degradation of Her2 in SKOV3 cells	[PMID: 16854066]
SK-OV-3	GI₅₀	32 nM Compound: 4b, 17-DMAG	Inhibition of human SKOV3 cell growth Inhibition of human SKOV3 cell growth	[PMID: 16854066]
SK-OV-3	IC₅₀	122 nM Compound: alvespimycin, 17-DMAG	Cytotoxicity against human SKOV3 cells after 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs	[PMID: 19231864]
SK-OV-3	IC₅₀	220 nM Compound: 1e, 17-DMAG	Cytotoxicity against human SKOV3 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human SKOV3 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]

In Vitro

Alvespimycin (17-DMAG) inhibits the growth of the human cancer cell lines SKBR3 and SKOV3, which overexpress Hsp90 client protein Her2, and causes down-regulation of Her2 as well as induction of Hsp70 consistent with Hsp90 inhibition, for Her2 degradation with EC₅₀ of 8 nM and 46 nM in SKBR3 and SKOV3 cells, respectively; for Hsp70 induction with EC₅₀ of 4 nM and 14 nM in SKBR3 and SKOV3 cells, respectively^[1].
Compared with the vehicle control, Alvespimycin (17-DMAG) dose-dependent apoptosis (P<0.001 averaged across 24- and 48-hour time points) at concentrations of 50 nM to 500 nM, which represent pharmacologically attainable doses. Similar to many other agents, Alvespimycin (17-DMAG) also demonstrates time-dependent apoptosis (P <0.001, averaged across all doses) in chronic lymphocytic leukemia (CLL) cells with extended exposure from 24 to 48 hours. In addition,Alvespimycin (17-DMAG) is much more potent after 24 and 48 hours of treatment than 17-AAG^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The tumors are grown for two months before the start of i.p. injections every four days over one month with 0, 50, 100 and 200 mg/kg dipalmitoyl-radicicol or 0, 5, 10 and 20 mg/kg Alvespimycin (17-DMAG). Despite sample heterogeneity, the HSP90 inhibitor-treated animals have significantly lower tumour volumes than the vehicle control-treated animals^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 467214-20-6
Appearance Solid
Masse moléculaire 616.75
Formule C₃₂H₄₈N₄O₈
Color Pale purple to purple
SMILES

C/C1=C\C=C/[C@@H]([C@H](/C(C)=C/[C@@H]([C@H]([C@H](C[C@@H](CC(C(C(NC1=O)=CC2=O)=O)=C2NCCN(C)C)C)OC)O[H])C)OC(N)=O)OC
Synonyms

17-DMAG; KOS-1022; NSC 707545
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (16)

All WB

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Journal Impact Factor

Nat Commun

Oncogenic enhancers drive esophageal squamous cell carcinogenesis and metastasis. [Abstract]

2021 Jul 22;12(1):4457. PMID: 34294701
Adv Sci (Weinh)

A Prion-Like Domain in EBV EBNA1 Promotes Phase Separation and Enables SRRM1 Splicing. [Abstract]

2025 Jul 29:e01977. PMID: 40729735
Theranostics

Hsp90 inhibitor HSP990 in very low dose upregulates EAAT2 and exerts potent antiepileptic activity. [Abstract]

2020 Jul 9;10(18):8415-8429. PMID: 32724478

Alvespimycin purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 9;10(18):8415-8429. [Abstract]

Western blot analysis of three proteins of interest in astrocytes treated with the Alvespimycin (17DMAG) for 24 h. Alvespimycin treatment increases EAAT2 and Hsp70 levels in a dose-dependent manner.
Pharmacol Res

Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]

2020 Jan;151:104512. PMID: 31726100
Cell Death Dis

RNA binding protein NKAP protects glioblastoma cells from ferroptosis by promoting SLC7A11 mRNA splicing in an m6A-dependent manner. [Abstract]

2022 Jan 21;13(1):73. PMID: 35064112
NPJ Precis Oncol

Refined high-content imaging-based phenotypic drug screening in zebrafish xenografts. [Abstract]

2023 May 18;7(1):44. PMID: 37202469
Br J Pharmacol

Inhibition of heat shock protein (HSP) 90 reverses signal transducer and activator of transcription (STAT) 3-mediated muscle wasting in cancer cachexia mice. [Abstract]

2021 Nov;178(22):4485-4500. PMID: 34265073
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
ACS Biomater Sci Eng

Biomimetic Platform Based on Mesoporous Platinum for Multisynergistic Cancer Therapy. [Abstract]

2021 Nov 8;7(11):5154-5164. PMID: 34636537
Front Pharmacol

Targeting HSP90 Inhibits Proliferation and Induces Apoptosis Through AKT1/ERK Pathway in Lung Cancer. [Abstract]

2022 Jan 14:12:724192. PMID: 35095481
Sci Rep

Functional characterization of a loss-of-function mutant I324M of arginine vasopressin receptor 2 in X-linked nephrogenic diabetes insipidus. [Abstract]

2021 May 26;11(1):11057. PMID: 34040143
Biochim Biophys Acta Mol Cell Res

Microbial imidazole propionate affects glomerular filtration rate in patients with diabetic nephropathy through association with HSP90α. [Abstract]

2024 Apr;1871(4):119703. PMID: 38453032
Exp Ther Med

Role of HSP90α in osteoclast formation and osteoporosis development. [Abstract]

2022 Apr;23(4):273. PMID: 35251339
Authorea

April 10, 2021.
bioRxiv

2021 Jan 27.
Friedrich-Alexander University Erlangen-Nuremberg

2016 Sep 14.

Alvespimycin purchased from MedChemExpress. Usage Cited in: Friedrich-Alexander University Erlangen-Nuremberg. 2016 Sep 14.

pJAK2 and JAK2 expression upon TGFβ stimulation and JAK inhibitors incubation. pJAK2 and JAK2 expression in healthy human fibroblasts after stimulation with TGFβ for 3 days and incubation with TG101209, 17-DMAG or Ruxolitinib.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (162.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6214 mL

8.1070 mL

16.2140 mL

5 mM

0.3243 mL

1.6214 mL

3.2428 mL

10 mM

0.1621 mL

0.8107 mL

1.6214 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[2]

MTT assays are performed to determine cytotoxicity. A total of 1×10⁶ CD19-selected B cells from CLL patients are incubated for 24 or 48 hours in Alvespimycin, 17-AAG, or vehicle. MTT reagent is then added, and plates are incubated for an additional 24 hours before spectrophotometric measurement. Apoptosis is determined by staining with annexin V-fluorescein isothiocyanate and propidium iodide (PI). After exposure to drugs, cells are washed with phosphate-buffered saline and stained in 1 time binding buffer. Cell death is assessed by flow cytometry. Data are analyzed with the System II software package. A total of 10000 cells are counted for each sample. Mitochondrial membrane potential changes are assessed by staining with the lipophilic cationic dye JC-1 and analysis by flow cytometry^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
Young male CB-17/IcrHsd-Prkdc-SCID mice are used. Recombinant xenografts are made by mixing 1×10⁵ BPH1 cells and 2.5×10⁵ CAF per graft in collagen solution, allowed to gel, covered with medium and cultured overnight. Tumors are allowed to form over eight weeks, and then treated for four weeks with three different doses of dipalmitoyl-radicicol (50, 100 and 200 mg/kg) and Alvespimycin (5, 10 and 20 mg/kg) via intraperitoneal injections of compounds in sesame oil every four days. After 12 weeks in total, the mice are sacrificed, their kidneys resected, grafts cut in half and photographed before processing for histology. Graft dimensions are measured and the resultant tumour volume is calculated using the formula; volume=width × length × depth × π/6. This formula represents a conservative approach to evaluate tumour volumes, as it understates the volume of large, invasive tumours compared with smaller, non-invasive tumours. Resected grafts are fixed in 10% formalin, embedded in paraffin and processed for immunohistochemistry.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Ge J, et al. Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. J Med Chem. 2006 Jul 27;49(15):4606-15. [Content Brief]

[2]. Hertlein E, et al. 17-DMAG targets the nuclear factor-kappaB family of proteins to induce apoptosis in chronic lymphocytic leukemia: clinical implications of HSP90 inhibition. Blood. 2010 Jul 8;116(1):45-53. [Content Brief]

[3]. Henke A, et al. Reduced Contractility and Motility of Prostatic Cancer-Associated Fibroblasts after Inhibition of Heat Shock Protein 90. Cancers (Basel). 2016 Aug 24;8(9). pii: E77. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6214 mL	8.1070 mL	16.2140 mL	40.5351 mL
	5 mM	0.3243 mL	1.6214 mL	3.2428 mL	8.1070 mL
	10 mM	0.1621 mL	0.8107 mL	1.6214 mL	4.0535 mL
	15 mM	0.1081 mL	0.5405 mL	1.0809 mL	2.7023 mL
	20 mM	0.0811 mL	0.4054 mL	0.8107 mL	2.0268 mL
	25 mM	0.0649 mL	0.3243 mL	0.6486 mL	1.6214 mL
	30 mM	0.0540 mL	0.2702 mL	0.5405 mL	1.3512 mL
	40 mM	0.0405 mL	0.2027 mL	0.4054 mL	1.0134 mL
	50 mM	0.0324 mL	0.1621 mL	0.3243 mL	0.8107 mL
	60 mM	0.0270 mL	0.1351 mL	0.2702 mL	0.6756 mL
	80 mM	0.0203 mL	0.1013 mL	0.2027 mL	0.5067 mL
	100 mM	0.0162 mL	0.0811 mL	0.1621 mL	0.4054 mL

Keywords

Alvespimycin

16 Cited Publications

100 mg Obtenir un devis

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Alvespimycin

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Alvespimycin

Voir tous les produits spécifiques à Isoform HSP

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Alvespimycin

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Alvespimycin

Voir tous les produits spécifiques à Isoform HSP

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Alvespimycin Related Classifications

Cat. No.: HY-10389