1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Anti-infection Protein Tyrosine Kinase/RTK NF-κB Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR
  2. HSP HSV HIF/HIF Prolyl-Hydroxylase VEGFR NF-κB ERK Akt FAK
  3. AT-533

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).

For research use only. We do not sell to patients.

AT-533 Chemical Structure

AT-533 Chemical Structure

CAS No. : 908112-37-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 880 In-stock
50 mg USD 1400 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1][2][3].

IC50 & Target[1]

HSP90

 

HSV-1

 

ERK1

 

ERK2

 

NF-κB

 

Akt

 

HIF-1α

 

VEGF/VEGFR-2

 

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.
Molecular Weight

410.51

Formula

C23H30N4O3

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4360 mL 12.1800 mL 24.3599 mL
5 mM 0.4872 mL 2.4360 mL 4.8720 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AT-533
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