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GNE-272
Contact us for more batch information
GNE-272
Catalog No. T15400Cas No. 1936428-93-1
GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
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. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $107 | 6-8 weeks | |
| 25 mg | $728 | 6-8 weeks | |
| 50 mg | $946 | 6-8 weeks | |
| 100 mg | $1,490 | 6-8 weeks |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300. |
| In vitro | GNE-272 does not inhibit any target at >30% when tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel. GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. The compound has good potency in the BRET cellular assay. GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) (EC50: 0.91 μM) and a good correlation between the BRET and MYC cellular assays is observed. |
| In vivo | GNE-272 displays a marked antiproliferative effect in hematologic cancer cell lines. Which modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. GNE-272 shows low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. |
| Molecular Weight | 424.47 |
| Formula | C22H25FN6O2 |
| Cas No. | 1936428-93-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (235.59 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
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