XYD190
XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia.
(Pink: CBP/p300 ligand (HY-161495); Blue: Cereblon ligand (HY-41547); Black: linker (HY-161496)).
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- CAS. Nr.: 3040121-23-8
- Formel: C55H50F2N10O7
- Molecular Weight:1001.05
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
26.9 nM
Compound: 14g; XYD190
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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 |
4.6 nM
Compound: 14g; XYD190
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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 |
1.8 nM
Compound: 14g; XYD190
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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] |
In Vitro
XYD190 (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 1.8, 26.9 and 4.6 nM, respectively[1].
XYD190 (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. Further protocols information, click here.
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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.
In Vivo
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 88%.
Chemical Information
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CAS. Nr. 3040121-23-8
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Molecular Weight 1001.05
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Formel C55H50F2N10O7
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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=CC=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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
XYD190 Related Classifications
HY-161494 Related Classifications
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