XYD129
XYD129 is a CBP/p300 PROTAC degrader. XYD129 potently binds to CBP, p300 and CRBN proteins, with IC50 values of 0.021 μM, 0.03 μM and 0.18 μM, respectively. XYD129 forms a ternary CRBN-CBP/p300 complex and induces CBP/p300 degradation via the ubiquitin-proteasome system. XYD129 inhibits tumor growth and suppresses the proliferation of acute myeloid leukemia cells. XYD129 can be used in studies related to acute myeloid leukemia.
(Pink: CBP and p300 ligand (HY-161711); Blue: Cereblon ligand (HY-41547); Black: linker (HY-40178)).
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- Formule: C41H39FN8O9
- Masse moléculaire:806.79
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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CBP 0.021 μM (IC50) |
p300 0.03 μM (IC50) |
Cereblon 0.18 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| KG-1 | IC50 |
0.57 μM
Compound: 11c
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Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
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[PMID: 38829718] |
| L02 | IC50 |
>100 μM
Compound: 11c
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Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
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[PMID: 38829718] |
| MOLM-16 | IC50 |
0.007 μM
Compound: 11c
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Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
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[PMID: 38829718] |
| MV4-11 | IC50 |
0.044 μM
Compound: 11c
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 120 hrs by celltiter glo luminescence analysis
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 120 hrs by celltiter glo luminescence analysis
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[PMID: 38829718] |
XYD129 (1 μM; 1.5 h) strongly binds to CBP, p300, and CRBN proteins, and effectively forms ternary complexes between CBP/p300 and CRBN[1].
XYD129 (12-1000 nM; 6-24 h) potently degrades CBP and p300 proteins in MOLM-16 cells in vitro in a concentration- and time-dependent manner, with near-complete degradation at 333 nM after 24 h and maximum degradation at 24 h when treated with 500 nM[1].
XYD129 (500 nM; 18 h, with 2 h pretreatment) mediated degradation of CBP and p300 in MOLM-16 cells is dependent on the ubiquitin-proteasome system and involves binding to CRBN[1].
XYD129 (serially diluted concentrations; 72-120 h) potently inhibits the growth of acute myeloid leukemia cell lines MV4-11 (IC50 = 0.049 μM), MOLM-16 (IC50 = 7.4 nM), and KG-1 (IC50 = 0.57 μM) without affecting normal HL-7702 cell growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-16
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Concentration:12, 37, 111, 333, 1000 nM (24 h incubation); 500 nM (time-dependent analysis)
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Incubation Time:24 h (concentration-dependent analysis); 6, 12, 15, 18, 21, 24 h (time-dependent analysis)
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Result:Induced concentration-dependent degradation of CBP and p300; near-complete degradation of both proteins was observed at 333 nM after 24 h.
Time-dependent analysis showed significant degradation within 12 h at 500 nM, with maximum degradation achieved at 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID (male, 4 weeks old, subcutaneous xenograft of MOLM-16 tumor cells)[1]
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Dosage:30 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Achieved a tumor growth inhibition (TGI) value of 60%.
Caused no significant reduction in mouse body weight.
Induced degradation of CBP and p300 proteins in tumor tissue.
Resulted in no abnormal changes in major organs compared to the vehicle group.
Chemical Information
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Masse moléculaire 806.79
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Formule C41H39FN8O9
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SMILES
O=C(C1=CC(C(NC2=C(C(C3=CN(N=C3)C)=CC(CO)=C2)F)=O)=C4N1C=CC(OCC(NCCCCNC5=CC=CC6=C5C(N(C7CCC(NC7=O)=O)C6=O)=O)=O)=C4)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XYD129 Related Classifications
HY-161710 Related Classifications
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