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A947
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Catalog No. T74686Cas No. 2378056-80-3
Alias A 947
A947 is a potent and selective SMARCA2 protein hydrolysis-targeted chimeric molecule (PROTAC) that induces the degradation of SMARCA2 by binding to VHL E3 ubiquitin ligase, with significant antitumor activity in vivo and in vitro, especially in SMARCA4-mutant non-small cell lung cancer (NSCLC) cells.
A947
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Purity: 98.84%
Catalog No. T74686Alias A 947Cas No. 2378056-80-3
A947 is a potent and selective SMARCA2 protein hydrolysis-targeted chimeric molecule (PROTAC) that induces the degradation of SMARCA2 by binding to VHL E3 ubiquitin ligase, with significant antitumor activity in vivo and in vitro, especially in SMARCA4-mutant non-small cell lung cancer (NSCLC) cells.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $1,070 | - | In Stock | |
| 5 mg | $2,357 | - | In Stock | |
| 10 mg | $3,535 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
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.
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Purity:98.84%
Appearance:Solid
Color:White to Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | A947 is a potent and selective SMARCA2 protein hydrolysis-targeted chimeric molecule (PROTAC) that induces the degradation of SMARCA2 by binding to VHL E3 ubiquitin ligase, with significant antitumor activity in vivo and in vitro, especially in SMARCA4-mutant non-small cell lung cancer (NSCLC) cells. |
| Targets&IC50 | SMARCA4:65 nM (Kd), SMARCA2:93 nM (Kd) |
| In vitro | Methods: SW1573 cells were treated with A947 (500 nM) and quantitative diglycine residue analysis was performed by mass spectrometry to ensure maximal degradation of SMARCA2/4. Results: Ubiquitination of multiple lysines was observed on SMARCA2 and SMARCA4, with the strongest ubiquitination at K1450 mapping to the bromodomain of SMARCA2/4. This suggests that A947 is highly specific in degrading the intended target proteins at high concentrations. [1] |
| In vivo | Methods: SMARCA4mut HCC515 xenograft mice were treated with A947 (40 mg/kg, intravenous injection, two weeks) to evaluate the pharmacodynamic (PD) effect. Results: A947 caused a rapid decrease in tumor SMARCA2 protein levels (96% reduction in 4 hours) and achieved the maximum reduction at 24 hours, indicating its anti-tumor activity. [1] |
| Synonyms | A 947 |
| Molecular Weight | 1121.4 |
| Formula | C61H76N12O7S |
| Cas No. | 2378056-80-3 |
| Smiles | O(C1=CC(N2C3CN(CC2CC3)C=4C=C(N=NC4N)C5=C(O)C=CC=C5)=CC=N1)[C@H]6C[C@H](OC7CCN(CC8CCN(CC8)C=9C=C([C@H](C(=O)N%10[C@H](C(N[C@@H](C)C%11=CC=C(C=C%11)C=%12SC=NC%12C)=O)C[C@@H](O)C%10)C(C)C)ON9)CC7)C6 |
| Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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