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A947
🥰Excellent
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
🥰Excellent
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $1,070 | In Stock | |
| 5 mg | $2,357 | In Stock | |
| 10 mg | $3,535 | In Stock |
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Purity:98.84%
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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 | 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 | SMARCA2:93 nM (Kd), SMARCA4:65 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] |
| Alias | 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 & Solubility Information
| 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. |
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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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