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)).
For research use only. We do not sell to patients.
- CAS No.: 3040121-23-8
- Formula: C55H50F2N10O7
- Molecular Weight:1001.05
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
26.9 nM
Compound: 14g; XYD190
|
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
|
[PMID: 38649304] |
| MOLM-16 | IC50 |
4.6 nM
Compound: 14g; XYD190
|
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
|
[PMID: 38649304] |
| MV4-11 | IC50 |
1.8 nM
Compound: 14g; XYD190
|
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
|
[PMID: 38649304] |
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.
-
Cell Line:MV4;11 AML, MOLM-13 and MOLM-16
-
Concentration:0-1 μM
-
Incubation Time:3 days for MOLM-13, 4 days for MV4;11 AML and MOLM-16
-
Result:Inhibited cell proliferation.
-
Cell Line:MV4;11 AML, MOLM-13 and MOLM-16
-
Concentration:0-150 nM
-
Incubation Time:6 h
-
Result:Degraded CBP and p300 proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MV4;11 xenograft NOD-SCID mice model[1]
-
Dosage:5 mg/kg
-
Administration:p.o., every other day for 2 weeks
-
Result:Inhibited tumor growth with a TGI of 88%.
Chemical Information
-
CAS No. 3040121-23-8
-
Molecular Weight 1001.05
-
Formula C55H50F2N10O7
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz