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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $89 | In Stock | |
2 mg | $122 | In Stock | |
5 mg | $179 | In Stock | |
10 mg | $320 | In Stock | |
25 mg | $538 | In Stock | |
50 mg | $779 | In Stock | |
100 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $219 | In Stock |
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 | CBP:2.6 nM, p300:9.8 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (111.84 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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