AT-533
Based on 1 Customer Validation
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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.38%
- CAS No.: 908112-37-8
- 화학식: C23H30N4O3
- 분자량:410.51
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All VEGFR Isoforms
More
Biological Activity
|
HSP90 |
HSV-1 |
ERK1 |
ERK2 |
NF-κB |
Akt |
HIF-1α |
VEGF/VEGFR-2 |
|
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] |
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 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.
-
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.
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
-
분자량 410.51
-
화학식 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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
-
Data Sheet (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)
-
Handling Instructions (2659 KB)
References
[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]
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 |