XYD198
XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia.
(Pink: CBP/p300 ligand (HY-161495); Blue: Cereblon ligand (HY-41547); Black: linker (HY-161499)).
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- Fòrmula: C54H49F2N11O7
- Peso molecular:1002.03
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
47 nM
Compound: 14h; XYD198
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Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell-Titer Glo assay
Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell-Titer Glo assay
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[PMID: 38649304] |
| MOLM-16 | IC50 |
5.5 nM
Compound: 14h; XYD198
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Antiproliferative activity against human MOLM16 cells incubated for 72 hrs by Cell-Titer Glo assay
Antiproliferative activity against human MOLM16 cells incubated for 72 hrs by Cell-Titer Glo assay
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[PMID: 38649304] |
| MV4-11 | IC50 |
0.9 nM
Compound: 14h; XYD198
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Antiproliferative activity against human MV4-11 cells incubated for 120 hrs by Cell-Titer Glo assay
Antiproliferative activity against human MV4-11 cells incubated for 120 hrs by Cell-Titer Glo assay
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[PMID: 38649304] |
XYD198 (0-1 μM, 72-120 h) inhibits proliferations of acute myeloid leukemia (AML) cells MV4;11, MOLM-13 and MOLM-16, with the IC50 of 0.9, 47 and 5.5 nM, respectively[1].
XYD198 (0-150 nM, 6 h) induces CBP and p300 degradation in bromodomain family proteins in a CRBN- and proteasome-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4;11 AML, MOLM-13 and MOLM-16
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Concentration:0-1 μM
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Incubation Time:3 days for MOLM-13, 4 days for MV4;11 AML and MOLM-16
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Result:Inhibited cell proliferation.
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Cell Line:MV4;11 AML, MOLM-13 and MOLM-16
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Concentration:0-150 nM
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Incubation Time:6 h
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Result:Degraded CBP and p300 proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4;11 xenograft NOD-SCID mice model[1]
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Dosage:5 mg/kg
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Administration:p.o., every other day for 2 weeks
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Result:Inhibited tumor growth with a TGI of 93%.
Chemical Information
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Peso molecular 1002.03
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Fòrmula C54H49F2N11O7
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SMILES
O=C1CCC[C@H](N1C2=CC=C(C(F)=C2)F)C3=NC4=C(C=CC(C5=C(ON=C5C)C)=C4)N3C6CCN(CC6)CC(NC7=CN=C(N=C7)C8=CC=C(C=C8)CNC9=CC=CC(C(N%10C%11C(NC(CC%11)=O)=O)=O)=C9C%10=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XYD198 Related Classifications
HY-161498 Related Classifications
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