- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Inhibitors
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 908112-37-8] AT-533
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-148877 |
| Brand: | MCE |
| CAS: | 908112-37-8 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 410.51 |
| Molecular Formula | C23H30N4O3 |
| 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 |
Summary
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
|
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]
.
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 IC 50 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]
.
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. |
Appearance
Solid
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
DMSO : 33.33 mg/mL ( 81.19 mM ; ultrasonic and warming and heat to 60°C)
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 |
| 10 mM | 0.2436 mL | 1.2180 mL | 2.4360 mL |
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.
- [2] Li F, et al. AT-533, a Hsp90 inhibitor, attenuates HSV-1-induced inflammation. Biochem Pharmacol. 2019 Aug;166:82-92.
- [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.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.