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ARV-771
🥰Excellent
Catalog No. T5435Cas No. 1949837-12-0
ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.
ARV-771
🥰Excellent
Purity: 99.69%
Catalog No. T5435Cas No. 1949837-12-0
ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $55 | In Stock | |
| 5 mg | $122 | In Stock | |
| 10 mg | $197 | In Stock | |
| 25 mg | $393 | In Stock | |
| 50 mg | $586 | In Stock | |
| 100 mg | $838 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $213 | In Stock |
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CitedSelect Batch
Purity:99.69%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM. |
| Targets&IC50 | BRD2(1):34 nM (Kd), BRD3(1):8.3 nM (Kd), BRD4(1):9.6 nM (Kd), BRD2(2):4.7 nM (Kd), BRD3(2):7.6 nM (Kd), BRD4(2):7.6 nM (Kd) |
| In vitro | METHODS: ARV-771 (0.01/0.025/0.05/0.1/0.25/0.5/1/2μM) was used to culture Hep3B, HepG and HCCLM3 cells to observe whether ARV-771 inhibits the growth of these cancer cells. RESULTS ARV-771 had a dose-dependent inhibition on cancer cell viability when the concentration reached 0.25 μM in Hep3B and HepG2 cells and 0.5 μM in HCCLM3 cells. [1] |
| In vivo | METHODS: Nude mice successfully bearing transplanted HepG2 cell tumors were randomly divided into two groups and treated with ARV-771 (20 mg/kg/day, subcutaneous injection) every other day for 25 days. Tumor volume and body weight of mice were measured every 5 days. Immediately after extraction of xenografts from mice, tumor weight was measured by an electronic balance. RESULTS After ARV-771 treatment, tumor volume and tumor weight were significantly reduced. Immunochemical detection results showed that ARV-771 reduced the expression of Ki67 and increased the expression of cleaved Caspase 3 in xenograft tissues. [1] |
| Molecular Weight | 986.64 |
| Formula | C49H60ClN9O7S2 |
| Cas No. | 1949837-12-0 |
| Smiles | CC=1C2=C(N3C([C@H](CC(NCCOCCCOCC(N[C@H](C(=O)N4[C@H](C(N[C@@H](C)C5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)C(C)(C)C)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C |
| Relative Density. | 1.39 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mM | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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