(±)-Enitociclib
Based on 1 Customer Validation
(±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.
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。
- 純度: 99.23%
- CAS 番号: 1610358-53-6
- 分子式: C19H18F2N4O2S
- 分子量:404.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
HY-L009
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Blood Cancer Compound Library
HY-L079
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Cancer Stem Cells Compound Library
HY-L135
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Anti-Hematopathy Compound Library
HY-L171
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Anti-Ovarian Cancer Compound Library
HY-L173
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
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High-Efficiency Gene Editing Compound Library
HY-L244
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
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RNA Polymerase |
CDK9 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
29 nM
Compound: 8; BAY-1251152
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Antiproliferative activity against human MOLM-13 cells
Antiproliferative activity against human MOLM-13 cells
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[PMID: 32866383] |
| T-cell | IC50 |
3 nM
Compound: 53; BAY-1251152
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Inhibition of CDK9/Cyclin T (unknown origin)
Inhibition of CDK9/Cyclin T (unknown origin)
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[PMID: 35485642] |
(±)-Enitociclib (12.5-200 nM; 96 h) inhibits cell viability in multiple myeloma (MM) cell lines (NCI-H929, MM1.S, OPM-2, U266B1) in a concentration-dependent manner with an IC50 of 36-78 nM[2].
(±)-Enitociclib (0.5-1 μM; 6-24 h) induces apoptosis in MM cell lines (NCI-H929, OPM-2), as evidenced by increased cleavage of apoptotic markers caspase-3 and PARP, and down-regulates expression of the anti-apoptotic protein Mcl-1 and oncogenic protein c-Myc[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H929, MM1.S, OPM-2, U266B1
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Concentration:12.5-200 nM
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Incubation Time:96 h
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Result:Reduced cell viability in a concentration-dependent manner, with IC50s ranging from 36 nM-78 nM across the tested cell lines.
Enitociclib (15 mg/kg; intravenous injection; once a week) combined with Lenalidomide (HY-A0003) (50 mg/kg, oral, once a day) or Bortezomib (HY-10227) (0.8 mg/kg, intraperitoneal injection, twice a week), synergistically inhibits tumor growth in the OPM-2 xenograft model, with better effect than single factor treatment group[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID/Beige mice (6-8 weeks old) with JJN-3 xenografts; female NOD/SCID mice (6-8 weeks old) with NCI-H929 or OPM-2 xenografts[2]
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Dosage:15 mg/kg
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Administration:Intravenous (IV) injection, once weekly, for 3 weeks
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Result:Significantly reduced tumor volumes and prolonged survival compared to vehicle control.
In JJN-3 xenografts, single-dose treatment transiently inhibited transcription of MYC, MCL1, and PCNA, induced caspase-3 and PARP cleavage, and reduced c-Myc protein levels for up to 24 hours.
化学情報
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CAS 番号 1610358-53-6
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性状 Solid
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分子量 404.43
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分子式 C19H18F2N4O2S
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Color White to light yellow
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SMILES
N=S(CC1=CC(NC2=NC=C(F)C(C3=CC=C(F)C=C3OC)=C2)=NC=C1)(C)=O
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別名
(±)-BAY-1251152; (±)-VIP152
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 50 mg/mL (123.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (396 KB)
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- Deutsch - DE (396 KB)
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- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4726 mL | 12.3631 mL | 24.7262 mL | 61.8154 mL |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9452 mL | 12.3631 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL | 6.1815 mL | |
| 15 mM | 0.1648 mL | 0.8242 mL | 1.6484 mL | 4.1210 mL | |
| 20 mM | 0.1236 mL | 0.6182 mL | 1.2363 mL | 3.0908 mL | |
| 25 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4726 mL | |
| 30 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0605 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6182 mL | 1.5454 mL | |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 1.2363 mL | |
| 60 mM | 0.0412 mL | 0.2061 mL | 0.4121 mL | 1.0303 mL | |
| 80 mM | 0.0309 mL | 0.1545 mL | 0.3091 mL | 0.7727 mL | |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.6182 mL |
(±)-Enitociclib 関連分類
HY-103019A 関連分類
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