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Atuveciclib Racemate

Catalog No. T10464L CAS 1414943-88-6

Synonyms: BAY-1143572 Racemate

Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib, which 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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Atuveciclib Racemate, CAS 1414943-88-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 112.00
2 mg	In stock	$ 165.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 462.00
25 mg	In stock	$ 867.00
50 mg	In stock	$ 1,160.00
100 mg	In stock	$ 1,570.00
1 mL * 10 mM (in DMSO)	In stock	$ 318.00

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Biological Description

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Description	Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib, which is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
Targets&IC50	Apoptosis:385 nM(AML cell lines), P-TEFb/CDK9:13 nM, Antiproliferative:310 nM(MOLM-13 cells), Antiproliferative:920 nM(HeLa cells)
In vitro	Atuveciclib (BAY-1143572) exhibits a potent and highly selective inhibitory effect on PTEFb-kinase, specifically against PTEFb/CDK9, in the low nanomolar range, demonstrating at least 50-fold higher selectivity over other CDKs. The compound effectively inhibits the proliferation of seven AML cell lines, both with and without MLL rearrangements, evidenced by a median IC50 of 385 nM (ranging between 230-1100 nM), and it also triggers apoptosis[1]. Furthermore, Atuveciclib (BAY-1143572) differentiates itself by showing significant selectivity against a broad array of non-CDK kinases, coupled with wide-ranging antiproliferative effects across various tumor cell lines indicated by sub-micromolar IC50 values. Notably, it leads to the concentration-dependent inhibition of RNA polymerase II phosphorylation, subsequently diminishing MYC mRNA and protein levels[2].
In vivo	Atuveciclib (BAY-1143572) significantly enhances its effectiveness when used with various chemotherapeutics across different solid tumor models. Additionally, it reduces MYC mRNA levels in the blood cells of treated rats, suggesting the potential of using MYC as a pharmacodynamic marker during clinical trials. When administered orally once daily, Atuveciclib demonstrates efficacy as a single agent, achieving partial or complete remission in most AML (acute myeloid leukemia) xenograft models in both mice and rats, proving its potency and tolerability at certain doses.

Synonyms	BAY-1143572 Racemate
Molecular Weight	387.43
Formula	C18H18FN5O2S
CAS No.	1414943-88-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (285.11 mM)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Orally Active Compound Library Bioactive Compound Library Kinase Inhibitor Library Anti-Breast Cancer Compound Library

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Keywords

Atuveciclib Racemate 1414943-88-6 Cell Cycle/Checkpoint CDK BAY-1143572 Racemate Atuveciclib BAY1143572 Cyclin dependent kinase inhibit Inhibitor BAY 1143572 BAY-1143572 inhibitor

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