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XYD198

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Catalog No. T209713

XYD198 (Compound 14h) is an orally active degrader of CBP/p300. It inhibits the CBP/p300 bromodomain with an IC50 of 213.5 nM and exhibits antitumor activity against acute myeloid leukemia.

XYD198

XYD198

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Catalog No. T209713
XYD198 (Compound 14h) is an orally active degrader of CBP/p300. It inhibits the CBP/p300 bromodomain with an IC50 of 213.5 nM and exhibits antitumor activity against acute myeloid leukemia.
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Product Introduction

Bioactivity
Description
XYD198 (Compound 14h) is an orally active degrader of CBP/p300. It inhibits the CBP/p300 bromodomain with an IC50 of 213.5 nM and exhibits antitumor activity against acute myeloid leukemia.
In vitro
XYD198 effectively inhibits the proliferation of acute myeloid leukemia (AML) cells MV4;11, MOLM-13, and MOLM-16 at concentrations ranging from 0 to 1 μM over 72 to 120 hours, with IC50 values of 0.9, 47, and 5.5 nM, respectively. Additionally, XYD198 at 0 to 150 nM over 6 hours induces degradation of the bromodomain proteins CBP and p300 in a CRBN and proteasome-dependent manner.
In vivo
In a MV4;11 xenograft mouse model, CBP/p300 ligand 4 (5 mg/kg, orally, administered once every two days for two weeks) demonstrated antitumor activity, achieving a tumor growth inhibition (TGI) rate of 93%.
Chemical Properties
FormulaC54H49F2N11O7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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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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