2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis CDK Apoptosis
  4. (±)-Enitociclib

(±)-Enitociclib  (Synonyms: (±)-BAY-1251152; (±)-VIP152)

製品番号: HY-103019A 純度: 99.23%
COA 取扱説明書 Technical Support

(±)-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.

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(±)-Enitociclib

(±)-Enitociclib 構造式

CAS 番号 : 1610358-53-6

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 110 在庫あり
Solution
10 mM * 1 mL in DMSO USD 110 在庫あり
Solid
5 mg $100 在庫あり
10 mg $150 在庫あり
50 mg $450 在庫あり
100 mg $720 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 0 publication(s) in Google Scholar

Other Forms of (±)-Enitociclib:

(±)-Enitociclib 関連抗体

Top Publications Citing Use of Products

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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製品説明

(±)-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[1][2].

IC50 & Target

RNA Polymerase

 

CDK9

 

Cellular Effect
Cell Line Type Value Description References
MOLM-13 IC50
29 1
Compound: 8; BAY-1251152
Antiproliferative activity against human MOLM-13 cells
Antiproliferative activity against human MOLM-13 cells
[PMID: 32866383]
T-cell IC50
3 1
Compound: 53; BAY-1251152
Inhibition of CDK9/Cyclin T (unknown origin)
Inhibition of CDK9/Cyclin T (unknown origin)
[PMID: 35485642]
MOLM-13 IC50
29 1
Compound: 8; BAY-1251152
Antiproliferative activity against human MOLM-13 cells
Antiproliferative activity against human MOLM-13 cells
[PMID: 32866383]
T-cell IC50
3 1
Compound: 53; BAY-1251152
Inhibition of CDK9/Cyclin T (unknown origin)
Inhibition of CDK9/Cyclin T (unknown origin)
[PMID: 35485642]
体外実験

(±)-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.

(±)-Enitociclib 関連抗体

Cell Viability Assay[2]

Cell Line: NCI-H929, MM1.S, OPM-2, U266B1
Concentration: 12.5-200 nM
Incubation Time: 96 h
Result: Reduced cell viability in a concentration-dependent manner, with IC50s ranging from 36 nM-78 nM across the tested cell lines.
体内実験

Enitociclib (15 mg/kg; intravenous injection; once a week; 3 weeks) significantly inhibits tumor growth in mouse multiple myeloma (MM) xenograft models (JJN-3, NCI-H929, OPM-2), reduces tumor volume and prolonged mouse survival[2].
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.

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]
Dosage: 15 mg/kg
Administration: Intravenous (IV) injection, once weekly, for 3 weeks
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.
分子量

404.43

分子式

C19H18F2N4O2S
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

N=S(CC1=CC(NC2=NC=C(F)C(C3=CC=C(F)C=C3OC)=C2)=NC=C1)(C)=O
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 : 50 mg/mL (123.63 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 2.4726 mL 12.3631 mL 24.7262 mL
5 mM 0.4945 mL 2.4726 mL 4.9452 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 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

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

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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

濃度 （開始）

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体積 （開始）

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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: ≥ 2.5 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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
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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% 
+
%
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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: 99.23%

COA (247 KB) LCMS (96 KB)

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
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(±)-Enitociclib Related Classifications

  • 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.

Keywords:

(±)-Enitociclib1610358-53-6(±)-BAY-1251152 (±)-VIP152DNA/RNA SynthesisCDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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