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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C54H49F2N11O7
- 分子量:1002.03
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
47 nM
Compound: 14h; XYD198
|
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 |
5.5 nM
Compound: 14h; XYD198
|
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 |
0.9 nM
Compound: 14h; XYD198
|
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] |
体外実験
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. 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.
体内実験
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%.
化学情報
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分子量 1002.03
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)