1. Cell Cycle/DNA Damage
  2. CDK
  3. Mevociclib

Mevociclib  (Synonyms: SY-1365)

製品番号: HY-128587 純度: 99.27%
COA 取扱説明書

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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Mevociclib 構造式

Mevociclib 構造式

CAS 番号 : 1816989-16-8

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 452 在庫あり
Solution
10 mM * 1 mL in DMSO USD 452 在庫あり
Solid
1 mg USD 166 在庫あり
5 mg USD 350 在庫あり
10 mg USD 650 在庫あり
50 mg USD 2000 在庫あり
100 mg USD 3500 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

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製品説明

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[1][2].

IC50 & Target[1]

CDK7

 

Cellular Effect
Cell Line Type Value Description References
HL-60 EC50
8 nM
Compound: SY-1365
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
[PMID: 31477350]
体外実験

Mevociclib exhibits inhibition for CDK7/CycH/MAT1 with an IC50 of 20 nM[2].
? Mevociclib is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells[2].
? 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.

体内実験

Mevociclib (20mg/kg; i.v.; biw; for 35 days) inhibits tumor growth in TNBC in vivo models[2].
? Mevociclib induces unique transcriptional signature[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice, HCC70 xenograft model[2]
Dosage: 20 mg/kg
Administration: Intravenous injection, twice weekly, for 35 days
Result: Inhibited tumor volume in vivo.
臨床実験
分子量

587.12

分子式

C31H35ClN8O2

CAS 番号
Appearance

Solid

Color

White to off-white

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (212.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7032 mL 8.5161 mL 17.0323 mL
5 mM 0.3406 mL 1.7032 mL 3.4065 mL
10 mM 0.1703 mL 0.8516 mL 1.7032 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

純度: 99.27%

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
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Mevociclib
製品番号:
HY-128587
数量:
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