Cat. No.: HY-148877

AT-533

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AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs).

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Pureté: 98.38%
CAS No.: 908112-37-8
Formule: C₂₃H₃₀N₄O₃
Masse moléculaire:410.51

Stockage:

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

AT-533 Chemical Structure

CAS No.: 908112-37-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

HSP90

HSV-1

ERK1

ERK2

NF-κB

Akt

HIF-1α

VEGF/VEGFR-2

Voir tous les produits spécifiques à Isoform HSP :

Voir tous les produits spécifiques à Isoform HSV :

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase :

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform NF-κB :

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform Akt :

Cellular Effect

Cell Line	Type	Value	Description	References
AU565	IC₅₀	30 μM Compound: 25a	Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening	[PMID: 19552433]
MRC5	CC₅₀	54.13 μM Compound: SNX-25a	Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay	[PMID: 22704890]
Vero	CC₅₀	27.06 μM Compound: SNX-25a	Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay	[PMID: 22704890]
Vero	EC₅₀	1.75 μM Compound: SNX-25a	Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay	[PMID: 22704890]
Vero	EC₅₀	2.24 μM Compound: SNX-25a	Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay	[PMID: 22704890]

In Vitro

AT-533 (0-1350 nM; 24 h or 48 h) inhibits 20 ng/mL VEGF-induced tube formation, cell migration, and invasion of HUVECs^[1].
AT-533 (2 μM or 75 μM; 24 h) inhibits the HIF-1α/VEGF signaling pathway in hypoxia-induced breast cancer cells, as well as inhibiting Akt/mTOR/p70S6K, Erk1/2, and FAK phosphorylation^[1].
AT-533 (10 nM, 50 nM; 48 h) shows anti-angiogenic ability in chorioallantoic membrane (CAM) model^[1].
AT-533 (0.5 μM; 2 h, 4 h) decreases TNF-α, IL-1β and IL-6 production in RAW264.7 and BV2 cells induced by HSV-1^[2].

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

Cell Viability Assay^[1]

Cell Line:

Human umbilical vein endothelial cells (HUVECs): MCF-7 and MDA-MB-231
Concentration:

0, 5.6, 16.7, 50, 150, 450, and 1350 nM
Incubation Time:

12 h, 24 h, 48 h, and 72 h
Result:

Inhibited cell viability at 48 h with an IC₅₀ value of 50.1 nM.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells and MDA-MB-231 cells
Concentration:

5 nM, 10 nM, 50 nM, and 75 nM
Incubation Time:

24 h
Result:

Inhibited the phosphorylation of VEGF-2, Akt, mTOR, Erk1/2, FAK.

In Vivo

AT-533 (10 mg/kg; i.p.; once daily for 21 d) suppresses the expression of the HIF-1α/VEGF signaling pathway-related proteins in MDA-MB-231 breast cancer xenografts tumor model in mouse^[1].
AT-533 (1, 2 and 4 mg/kg; i.p.; once daily for 30 d) has no mortality, loss of appetite and body weight, adverse reactions in Sprague-Dawley rats in subacute toxicity test^[3].

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

Animal Model:

Male C57BL/6 mice with MDA-MB-231 breast cancer xenografts^[1]
Dosage:

10 mg/kg;
Administration:

Intraperitoneal injection; once daily for 21 days
Result:

Significantly downregulated HIF-1α and VEGF expression.

Chemical Information

CAS No. 908112-37-8
Appearance Solid
Masse moléculaire 410.51
Formule C₂₃H₃₀N₄O₃
Color Off-white to light yellow
SMILES

CC1=NN(C2=CC(N[C@@H]3CC[C@H](CC3)O)=C(C=C2)C(N)=O)C(CC(C)(C4)C)=C1C4=O
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

Solvant et solubilité

In Vitro:

DMSO : 33.33 mg/mL (81.19 mM; ultrasonic and warming and heat to 60°C; 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

2.4360 mL

12.1800 mL

24.3599 mL

5 mM

0.4872 mL

2.4360 mL

4.8720 mL

10 mM

0.2436 mL

1.2180 mL

2.4360 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 (6.09 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.09 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
Number of Animals Number of Animals

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.
%
+
+
%
Tween-80 + +
%
Saline +

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang PC, et al. AT-533, a novel Hsp90 inhibitor, inhibits breast cancer growth and HIF-1α/VEGF/VEGFR-2-mediated angiogenesis in vitro and in vivo. Biochem Pharmacol. 2020 Feb;172:113771. [Content Brief]

[2]. Li F, et al. AT-533, a Hsp90 inhibitor, attenuates HSV-1-induced inflammation. Biochem Pharmacol. 2019 Aug;166:82-92. [Content Brief]

[3]. Wu Y, et al. Subacute toxicological evaluation of AT-533 and AT-533 gel in Sprague-Dawley rats. Exp Ther Med. 2021 Jun;21(6):632. [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	2.4360 mL	12.1800 mL	24.3599 mL	60.8999 mL
	5 mM	0.4872 mL	2.4360 mL	4.8720 mL	12.1800 mL
	10 mM	0.2436 mL	1.2180 mL	2.4360 mL	6.0900 mL
	15 mM	0.1624 mL	0.8120 mL	1.6240 mL	4.0600 mL
	20 mM	0.1218 mL	0.6090 mL	1.2180 mL	3.0450 mL
	25 mM	0.0974 mL	0.4872 mL	0.9744 mL	2.4360 mL
	30 mM	0.0812 mL	0.4060 mL	0.8120 mL	2.0300 mL
	40 mM	0.0609 mL	0.3045 mL	0.6090 mL	1.5225 mL
	50 mM	0.0487 mL	0.2436 mL	0.4872 mL	1.2180 mL
	60 mM	0.0406 mL	0.2030 mL	0.4060 mL	1.0150 mL
	80 mM	0.0304 mL	0.1522 mL	0.3045 mL	0.7612 mL

Keywords

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AT-533

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Endoplasmic Reticulum Stress Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform HSP

Voir tous les produits spécifiques à Isoform HSV

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform NF-κB

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

AT-533 Related Classifications

HY-148877 Related Classifications