Mevociclib
Based on 7 publication(s) in Google Scholar
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
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- 純度: 99.73%
- CAS 番号: 1816989-16-8
- 分子式: C31H35ClN8O2
- 分子量:587.12
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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
MedChemExpress（MCE）の使用を引用している文献 Mevociclib
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生物活性
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CDK7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | EC50 |
8 nM
Compound: SY-1365
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Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 31477350] |
Mevociclib exhibits inhibition for CDK7/CycH/MAT1 with an IC50 of 20 nM[2].
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Mevociclib is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells[2].
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Mevociclib exhibits activity in breast, ovarian, colorectal and lung cancer cells that exhibited low nM EC50 and rapid induction of apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? Mevociclib induces unique transcriptional signature[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice, HCC70 xenograft model[2]
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Dosage:20 mg/kg
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Administration:Intravenous injection, twice weekly, for 35 days
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Result:Inhibited tumor volume in vivo.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1816989-16-8
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性状 Solid
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分子量 587.12
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分子式 C31H35ClN8O2
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Color White to off-white
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SMILES
O=C(C1=NC=C(NC(/C=C/CN(C)C)=O)C=C1)N[C@@]2(C)CCC[C@@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)C2
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別名
SY-1365
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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
Publications (7)
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Journal Impact Factor
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Most Recent
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Clin Cancer Res
Selective CDK7 inhibition suppresses cell cycle progression and MYC signaling while enhancing apoptosis in therapy-resistant estrogen receptor positive breast cancer. [Abstract]2024 May 1;30(9):1889-1905. PMID: 38381406 -
EMBO J
Resistance to CDK7 inhibitors directed by acquired mutation of a conserved residue in cancer cells. [Abstract]2025 Sep 8. PMID: 40921851 -
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Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
mBio
Functional insight into cyclin-dependent kinase (CDK)7 via chemical inhibition of the priority fungal pathogen Cryptococcus neoformans. [Abstract]2025 Dec 10;16(12):e0289825. PMID: 41171060 -
J Biol Chem
TGF-β/activin signaling promotes CDK7 inhibitor resistance in triple-negative breast cancer cells through upregulation of multidrug transporters. [Abstract]2021 Oct;297(4):101162. PMID: 34481843 -
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (170.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.08 mg/mL (3.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (271 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 | 1.7032 mL | 8.5161 mL | 17.0323 mL | 42.5807 mL |
| 5 mM | 0.3406 mL | 1.7032 mL | 3.4065 mL | 8.5161 mL | |
| 10 mM | 0.1703 mL | 0.8516 mL | 1.7032 mL | 4.2581 mL | |
| 15 mM | 0.1135 mL | 0.5677 mL | 1.1355 mL | 2.8387 mL | |
| 20 mM | 0.0852 mL | 0.4258 mL | 0.8516 mL | 2.1290 mL | |
| 25 mM | 0.0681 mL | 0.3406 mL | 0.6813 mL | 1.7032 mL | |
| 30 mM | 0.0568 mL | 0.2839 mL | 0.5677 mL | 1.4194 mL | |
| 40 mM | 0.0426 mL | 0.2129 mL | 0.4258 mL | 1.0645 mL | |
| 50 mM | 0.0341 mL | 0.1703 mL | 0.3406 mL | 0.8516 mL | |
| 60 mM | 0.0284 mL | 0.1419 mL | 0.2839 mL | 0.7097 mL | |
| 80 mM | 0.0213 mL | 0.1065 mL | 0.2129 mL | 0.5323 mL | |
| 100 mM | 0.0170 mL | 0.0852 mL | 0.1703 mL | 0.4258 mL |
Mevociclib 関連分類
HY-128587 関連分類
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