Art. -Nr.: HY-12871

Atuveciclib Racemate

(Synonyms: BAY-1143572 Racemate)

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Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC₅₀ of 13 nM.

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Reinheit: 98.34%
CAS. Nr.: 1414943-88-6
Formel: C₁₈H₁₈FN₅O₂S
Molecular Weight:387.43

Speicherung:

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

Atuveciclib Racemate Chemical Structure

CAS. Nr.: 1414943-88-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1] ^[1]

CDK9

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	380 nM Compound: Atuveciclib	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]
A549	IC₅₀	3.29 μM Compound: BAY-1143572	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]
B16	IC₅₀	1.47 μM Compound: BAY-1143572	Antiproliferative activity against mouse B16 cells incubated for 72 hrs by MTT assay Antiproliferative activity against mouse B16 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]
HCT-116	IC₅₀	2.94 μM Compound: BAY-1143572	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]
HepG2	IC₅₀	2.7 μM Compound: BAY-1143572	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]
MCF7	IC₅₀	5.52 μM Compound: BAY-1143572	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]
MOLM-13	IC₅₀	0.2 μM Compound: BAY-1143572	Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]
MOLM-13	IC₅₀	310 nM Compound: Atuveciclib	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]
MV4-11	IC₅₀	0.56 μM Compound: BAY-1143572	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay	[PMID: 33338869]

In Vitro

Atuveciclib (BAY-1143572) inhibits the proliferation of 7 MLL-rearrangements positive and negative AML cell lines with a median IC₅₀ of 385 nM (range 230-1100 nM) and induces apoptosis^[1]. Atuveciclib (BAY-1143572) has potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs. Atuveciclib (BAY-1143572) shows a favorable selectivity against a panel of non-CDK kinases. It shows broad antiproliferative activity against a panel of tumor cell lines with sub-micromolar IC₅₀ values. The concentration-dependent inhibition of the phosphorylation of the RNA polymerase II and downstream reduction of MYC mRNA and protein levels is observed^[2].

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

In Vivo

Atuveciclib (BAY-1143572) exhibits single agent efficacy at tolerated doses in 4 out of 5 AML xenograft tumor models in mice and in 2 out of 2 AML xenograft tumor models in rats upon once daily oral administration. Partial or even complete remissions could be achieved in several models^[1].The inhibition of MYC mRNA is also observed in blood cells of Atuveciclib (BAY-1143572)-treated rats indicating the potential clinical utility of MYC in blood cells as a pharmacodynamic marker in clinical development. The in vivo efficacy of Atuveciclib (BAY-1143572) is significantly enhanced in combination with several chemotherapeutics in different solid tumor models^[2].

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

Chemical Information

CAS. Nr. 1414943-88-6
Appearance Solid
Molecular Weight 387.43
Formel C₁₈H₁₈FN₅O₂S
Color White to off-white
SMILES

N=S(CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O
Synonyms

BAY-1143572 Racemate
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 (1)

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Haematologica

Setd2 regulates quiescence and differentiation of adult hematopoietic stem cells by restricting RNA polymerase II elongation. [Abstract]

2018 Jul;103(7):1110-1123. PMID: 29650642

Atuveciclib Racemate purchased from MedChemExpress. Usage Cited in: Haematologica. 2018 Jul;103(7):1110-1123. [Abstract]

Treat c-Kit⁺ BM cells from Setd2^f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400nM for 24 hours. Then cells are collected to determined the proteins levels of H3K36me1/2, H3K4me3, H3K79me2, H3K27me3, H3, RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (258.11 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

2.5811 mL

12.9056 mL

25.8111 mL

5 mM

0.5162 mL

2.5811 mL

5.1622 mL

10 mM

0.2581 mL

1.2906 mL

2.5811 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 (6.45 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 (6.45 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 (6.45 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 (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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]. Scholz A, et al. BAY 1143572, a first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, shows convincing anti-tumor activity in preclinical models of acute myeloid leukemia (AML). [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 3022.

[2]. Scholz A, et al. BAY 1143572: A first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr DDT02-02. doi:10.1158/1538-7445.AM2015-DDT02-02

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	2.5811 mL	12.9056 mL	25.8111 mL	64.5278 mL
	5 mM	0.5162 mL	2.5811 mL	5.1622 mL	12.9056 mL
	10 mM	0.2581 mL	1.2906 mL	2.5811 mL	6.4528 mL
	15 mM	0.1721 mL	0.8604 mL	1.7207 mL	4.3019 mL
	20 mM	0.1291 mL	0.6453 mL	1.2906 mL	3.2264 mL
	25 mM	0.1032 mL	0.5162 mL	1.0324 mL	2.5811 mL
	30 mM	0.0860 mL	0.4302 mL	0.8604 mL	2.1509 mL
	40 mM	0.0645 mL	0.3226 mL	0.6453 mL	1.6132 mL
	50 mM	0.0516 mL	0.2581 mL	0.5162 mL	1.2906 mL
	60 mM	0.0430 mL	0.2151 mL	0.4302 mL	1.0755 mL
	80 mM	0.0323 mL	0.1613 mL	0.3226 mL	0.8066 mL
	100 mM	0.0258 mL	0.1291 mL	0.2581 mL	0.6453 mL

Keywords

Atuveciclib Racemate

1 Cited Publications

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Atuveciclib Racemate

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Publications Citing Use of MedChemExpress (MCE) Atuveciclib Racemate

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Atuveciclib Racemate

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

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase 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) Atuveciclib Racemate

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Atuveciclib Racemate Related Classifications

Art. -Nr.: HY-12871