A-485 [1889279-16-6]
Referência NB-64-05602-5mg
Tamanho : 5mg
Marca : Neo Biotech
A-485
Catalog No. T14073 Copy Product Info
Purity: 99.98%
A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.
A-485
Copy Product InfoA-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.
Cas No. 1889279-16-6
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP. |
| Targets&IC50 | p300:9.8 nM, CBP:2.6 nM |
| In vitro | METHODS: 124 tumor cells were treated with A-485 for 3-5 days and cell viability was measured by the CellTiter-Glo Luminescent Cell Viability Assay. RESULTS: The broadest sensitivity was observed in hematologic tumors, where A-485 exhibited potent activity in most multiple myeloma (MM) cell lines, acute myeloid leukemia (AML) cell lines, and non-Hodgkin's lymphoma (NHL) cell lines. In contrast, several solid tumor lines, including melanoma, small cell lung cancer (SCLC), and triple-negative breast cancer (TNBC), showed significantly reduced sensitivity to A-485. [1] METHODS: H1650 and H1650-ER cells were treated with A-485 (20 µM) overnight, followed by TRAIL (10-100 ng/mL) overnight, and apoptosis was detected by apoptotic kit. RESULTS: The combination of A-485 and TRAIL significantly increased the total number of apoptotic cells in H1650 and H1650-ER cells compared to TRAIL alone.A-485 enhanced TRAIL-induced apoptosis. [2] |
| In vivo | METHODS: To assay in vivo anti-tumor activity, A-485 (100 mg/kg) was administered intraperitoneally twice daily for 21 days to SCID mice bearing LuCaP-77 CR xenografts. RESULTS: A-485 induced 54% tumor growth inhibition (TGI) after 21 days of administration. [1] |
| Molecular Weight | 536.48 |
| Formula | C25H24F4N4O5 |
| Cas No. | 1889279-16-6 |
| Smiles | CNC(=O)Nc1ccc2c(CC[C@@]22OC(=O)N(CC(=O)N(Cc3ccc(F)cc3)[C@@H](C)C(F)(F)F)C2=O)c1 |
| Relative Density. | 1.46 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 252.5 mg/mL (470.66 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.32 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
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