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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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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| 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%. |
| Formula | C54H49F2N11O7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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