PROTAC CDK9 degrader-8
PROTAC CDK9 degrader-8 is a CDK9 PROTAC degrader that recruits cereblon. PROTAC CDK9 degrader-8 inhibits the growth of acute myeloid leukemia cells by inducing the degradation of CDK9 protein. PROTAC CDK9 degrader-8 can be used in studies related to CDK9-targeted degradation and acute myeloid leukemia.
(Pink: CDK9/Cyclin T ligand (HY-50940); Blue: Cereblon ligand (HY-103596); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- CAS 番号: 2994191-89-6
- 分子式: C44H52Cl2N10O7
- 分子量:903.85
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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
IC50 & Target
[1]|
CDK9 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
0.01 μM
|
Inhibition of MV4-11 AML cell growth in standard conditions.
Inhibition of MV4-11 AML cell growth in standard conditions.
|
37465296 |
| MV4-11 | IC50 |
8.8 nM
|
Inhibition of MV4-11 AML cell growth in fetal bovine serum (FBS).
Inhibition of MV4-11 AML cell growth in fetal bovine serum (FBS).
|
37465296 |
| MV4-11 | IC50 |
28.6 nM
|
Inhibition of MV4-11 AML cell growth in human serum (HS).
Inhibition of MV4-11 AML cell growth in human serum (HS).
|
37465296 |
体外実験
PROTAC CDK9 degrader-8 (compound 21) induces CDK9 degradation in MOLM-13 cells, with a DC50 of 0.04 μM and a Dmax of 88.6%[1].
PROTAC CDK9 degrader-8 inhibits cell growth in MV4-11 acute myeloid leukemia cells, with an IC50 of 0.01 μM[1].
PROTAC CDK9 degrader-8 (6 h exposure followed by washout; total incubation time: 48 h) maintains cellular activity after washout in MV4-11 cells[1].
PROTAC CDK9 degrader-8 exhibits an IC50 of 8.8 nM in MV4-11 cells under FBS conditions and an IC50 of 28.6 nM under human serum conditions, showing an approximately 3-fold serum shift, while still maintaining high cellular activity within this series under both conditions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2994191-89-6
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分子量 903.85
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分子式 C44H52Cl2N10O7
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SMILES
O=C(C1=NNC=C1NC(C2=C(Cl)C=CC=C2Cl)=O)NC3CCN(CCCCCCCCCCC4=CN(CCCOC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)CC3
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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)