Art. -Nr.: HY-103019A

(±)-Enitociclib

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

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(±)-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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Reinheit: 99.23%
CAS. Nr.: 1610358-53-6
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.: 1610358-53-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RNA Polymerase

CDK9

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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 (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.

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.

In Vivo

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.

Chemical Information

CAS. Nr. 1610358-53-6
Appearance Solid
Molecular Weight 404.43
Formel C₁₉H₁₈F₂N₄O₂S
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
Synonyms

(±)-BAY-1251152; (±)-VIP152
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

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 (275 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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)
LCMS (2659 KB)
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 Nov 9;3(11):2268-2279. [Content Brief]

[2]. Tran S, et al. Enitociclib, a selective CDK9 inhibitor: in vitro and in vivo preclinical studies in multiple myeloma[J]. Blood Neoplasia, 2025, 2(1): 100050.

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

Keywords

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(±)-Enitociclib

Apoptosis Compound Library

Cell Cycle/DNA Damage 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

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor 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

Alle CDK Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(±)-Enitociclib

Apoptosis Compound Library

Cell Cycle/DNA Damage 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

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor 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

Alle CDK Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(±)-Enitociclib Related Classifications

HY-103019A Related Classifications