Art. -Nr.: HY-103019

Enitociclib

(Synonyms: (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC₅₀=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma.

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Reinheit: 99.89%
CAS. Nr.: 1610408-97-3
Formel: C₁₉H₁₈F₂N₄O₂S
Molecular Weight:404.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Enitociclib Chemical Structure

CAS. Nr.: 1610408-97-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RNA Polymerase

CDK9/CycT1

3 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	52 nM Compound: 32	Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay	[PMID: 34264057]
MOLM-13	IC₅₀	29 nM Compound: 13; VIP152	Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38564299]
MOLM-13	IC₅₀	29 nM Compound: 8; BAY-1251152	Antiproliferative activity against human MOLM-13 cells Antiproliferative activity against human MOLM-13 cells	[PMID: 32866383]
MOLM-13	IC₅₀	42 nM Compound: 32	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay	[PMID: 34264057]
T-cell	IC₅₀	3 nM Compound: 53; BAY-1251152	Inhibition of CDK9/Cyclin T (unknown origin) Inhibition of CDK9/Cyclin T (unknown origin)	[PMID: 35485642]

In Vitro

Enitociclib effectively reduces the viability of a panel of human lymphoma cell lines, including the DLBCL cell lines SU-DHL-4 (IC₅₀=43 nmol/L) and SU-DHL-10 (IC₅₀=74 nmol/L)^[1].
Enitociclib (0.25-1 μM; 4 h) induces transcriptomic changes dominated by significant downregulation in SU-DHL-4 and SU-DHL-10 DLBCL cell lines, including marked downregulation of novel targets PHF23 and TP53RK, as well as enrichment of the RNA polymerase II-mediated transcription pathway^[1].
Enitociclib (0.6-800 nM; 6-48 h) potently inhibits the viability of primary mantle cell lymphoma (MCL) cells, MCL cell lines, and diffuse large B-cell lymphoma (DLBCL) cell lines, and induces caspase-3-dependent apoptosis in these cells, with an IC₅₀ of 11.5-172.3 nM^[2].
Enitociclib (12.5-200 nM; 96 h) significantly reduces the cell viability of multiple myeloma cell lines MM1.S, NCI-H929, OPM-2 and U266B1, with an IC₅₀ ranging from 36 to 78 nM after 96 hours of treatment^[3].
Enitociclib (0.5-1 μM; 1-24 h) inhibits phosphorylation of RNA Pol II CTD at Ser2/Ser5 sites in a dose- and time-dependent manner, induces apoptosis, and suppresses oncoprotein expression in NCI-H929 and OPM-2 multiple myeloma cell lines^[3].
Enitociclib (25-500 nM; combined with paclitaxel) synergistically inhibits the growth of paclitaxel-resistant L3.6pl pancreatic cancer cells^[4].

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

Western Blot Analysis^[1]

Cell Line:

SU-DHL-4, SU-DHL-10 (DLBCL) cell lines
Concentration:

0.25 μmol/L; 1 μmol/L
Incubation Time:

4 h (treatment); up to 48 h post-washout (SU-DHL-4); up to 24 h post-washout (SU-DHL-10)
Result:

Decreased p-Ser2 levels by 50% for up to 48 hours post-washout in SU-DHL-4 cells treated with 0.25 μmol/L.
Caused a greater extent of p-Ser2 inhibition that sustained for 48 hours post-washout in SU-DHL-4 cells treated with 1 μmol/L.
Achieved a 50% reduction of p-Ser2 for up to 24 hours post-washout in SU-DHL-10 cells treated with 1 μmol/L.

Real Time qPCR^[1]

Cell Line:

SU-DHL-4, SU-DHL-10 (DLBCL) cell lines
Concentration:

0.25 μmol/L; 1 μmol/L
Incubation Time:

4 h (treatment); up to 48 h post-washout
Result:

Inhibited MYC and MCL1 mRNA levels by approximately 75% for 16 to 48 hours post-washout in SU-DHL-10 cells.
Maintained durable depletion of MYC and MCL1 mRNA levels over the 48-hour time course in SU-DHL-4 cells treated with 1 μmol/L.

Cell Viability Assay^[3]

Cell Line:

MM1.S, NCI-H929, OPM-2, U266B1 multiple myeloma cell lines
Concentration:

12.5-50 nM (in combination with other agents)
Incubation Time:

96 h
Result:

Exhibited synergistic effects (ZIP synergy score >10) with bortezomib in OPM-2 cells at 50 nM enitociclib and 1 nM bortezomib.
Showed synergistic effects with lenalidomide in MM1.S, NCI-H929, and U266B1 cells at 12.5 to 25 nM enitociclib and 313 nM to 5 μM lenalidomide.
Demonstrated synergistic effects with pomalidomide in NCI-H929 and U266B1 cells at 12.5 nM enitociclib and 12.5 to 50 nM pomalidomide.

In Vivo

Enitociclib (5-15 mg/kg; i.v.; single dose/once weekly; 3 weeks) exerts dose-dependent antitumor efficacy in SU-DHL-10 DLBCL xenografts, with 15 mg/kg once weekly dosing inducing complete tumor regression, and all tested doses driving pharmacodynamic effects including reduced p-Ser2, depleted MYC/MCL1 expression, and activated apoptosis^[1].
Enitociclib (10 mg/kg; i.v.; twice a week) potently inhibits tumor growth and prolongs survival in JeKo-1 MCL cell line-derived xenografts in NSG mice (p < 0.0001 for both endpoints) without significant toxicity^[2].
Enitociclib (15 mg/kg; i.v.; once per week) significantly reduces JJN-3 multiple myeloma tumor volumes in SCID/Beige mice, and a single dose (15 mg/kg; i.v.) transiently suppresses oncogene transcription and induces tumor apoptosis^[3].
Enitociclib (15 mg/kg; i.v.; once per week) significantly reduces OPM-2 multiple myeloma tumor volumes in NOD/SCID mice, and enhances efficacy when combined with lenalidomide or bortezomib^[3].
Enitociclib (10 mg/kg; i.v.; once weekly; 4 weeks) does not reduce tumor size as a single agent, but in combination with paclitaxel, it induces significant tumor shrinkage in a paclitaxel-resistant PDAC patient-derived xenograft model^[4].

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

Animal Model:

C.B-17 SCID (female, 10-12 weeks old at study start)^[1]
Dosage:

5 mg/kg (mechanistic single dose); 10 mg/kg (i.v. once weekly for 3 weeks; mechanistic single dose); 15 mg/kg (i.v. once weekly for 3 weeks; mechanistic single dose)
Administration:

i.v.; single dose (mechanistic studies); once weekly; 3 weeks (antitumor efficacy)
Result:

Achieved a tumor growth inhibition (T/C) value of 0.19 on day 16/20, with sustained tumor growth control at 10 mg/kg once weekly.
Induced complete tumor regression during the 3-week treatment period, with a T/C value of 0.005 on day 16/20 at 15 mg/kg once weekly; tumors regrew after treatment cessation, but a second cycle of 15 mg/kg once weekly dosing induced tumor regression again.
Reduced RNA polymerase II Ser2 phosphorylation (p-Ser2) by >50% for 8 hours postdose; depleted MYC and MCL1 mRNA levels by 4 hours postdose, with depletion sustained for 8 hours at 5 mg/kg single dose.
Depleted p-Ser2 levels within 8 hours postdose; depleted MYC and MCL1 mRNA levels by 4 hours postdose, with depletion sustained for 8 hours; reduced Myc protein levels by 50% and Mcl-1 protein levels robustly within 4-8 hours postdose; increased cleaved PARP (apoptosis marker) levels postdose at 10 mg/kg and 15 mg/kg single dose.

Animal Model:

NSG (NOD.Cg-Prkdc^scid Il2rg^tm1Wjl/SzJ) (immunodeficient)^[2]
Dosage:

10 mg/kg
Administration:

i.v.; twice a week
Result:

Markedly inhibited tumor growth.
Significantly prolonged mouse survival.
Caused no significant body weight loss or other apparent adverse effects.\nEfficaciously inhibited PDX-1 tumor growth.
Caused no significant body weight loss.\nEfficaciously inhibited PDX-2 tumor growth.
Caused no significant body weight loss.\nEfficaciously inhibited PDX-3 tumor growth.
Caused no significant body weight loss.

Animal Model:

NOD/SCID (gender not specified; injected subcutaneously with 5.0×10⁶ OPM-2 MM cells)^[3]
Dosage:

15 mg/kg (monotherapy); 15 mg/kg (in combination with lenalidomide or bortezomib)
Administration:

i.v.; once per week
Result:

Significantly reduced OPM-2 tumor volumes compared with vehicle-treated mice as monotherapy.
Further enhanced antitumor efficacy compared with lenalidomide or bortezomib alone when combined with 50 mg/kg Lenalidomide (p.o.
daily) or 0.8 mg/kg Bortezomib (i.p.
twice weekly).

Chemical Information

CAS. Nr. 1610408-97-3
Appearance Solid
Molecular Weight 404.43
Formel C₁₉H₁₈F₂N₄O₂S
Color Off-white to yellow
SMILES

COC1=C(C2=C(F)C=NC(NC3=CC(C[S@@](=O)(C)=N)=CC=N3)=C2)C=CC(F)=C1
Synonyms

(+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Acta Pharm Sin B

Predicting and overcoming resistance to CDK9 inhibitors for cancer therapy. [Abstract]

2023 Sep;13(9):3694-3707. PMID: 37719386
Oncotarget

The pharmacodynamic and mechanistic foundation for the antineoplastic effects of GFH009, a potent and highly selective CDK9 inhibitor for the treatment of hematologic malignancies. [Abstract]

2023 Dec 20:14:997-1008. PMID: 38117531

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 113.3 mg/mL (280.15 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (254 KB)
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- Deutsch - DE (254 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Frigault MM, et al. Enitociclib, a Selective CDK9 Inhibitor, Induces Complete Regression of MYC+ Lymphoma by Downregulation of RNA Polymerase II Mediated Transcription. Cancer Res Commun. 2023;3(11):2268-2279. [Content Brief]

[2]. Jiang V, et al. The CDK9 inhibitor enitociclib overcomes resistance to BTK inhibition and CAR-T therapy in mantle cell lymphoma. Biomark Res. 2024;12(1):62. Published 2024 Jun 18. [Content Brief]

[3]. Tran S, et al. Enitociclib, a selective CDK9 inhibitor: in vitro and in vivo preclinical studies in multiple myeloma. Blood Neoplasia. 2024;2(1):100050. Published 2024 Oct 24. [Content Brief]

[4]. Hamdan FH, et al. Interactive enhancer hubs (iHUBs) mediate transcriptional reprogramming and adaptive resistance in pancreatic cancer. Gut. 2023;72(6):1174-1185. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

2 Cited Publications

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Enitociclib

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) Enitociclib

Alle CDK Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Enitociclib

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) Enitociclib

Alle CDK Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Enitociclib Related Classifications

Art. -Nr.: HY-103019