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1414943-88-6

1414943-88-6 structure
1414943-88-6 structure
  • Name: BAY-1143572 Racemate
  • Chemical Name: atuveciclib
  • CAS Number: 1414943-88-6
  • Molecular Formula: C18H18FN5O2S
  • Molecular Weight: 387.431
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
  • Create Date: 2018-05-20 08:00:00
  • Modify Date: 2024-01-02 16:15:41
  • BAY-1143572 Racemate is the racemate mixture of BAY-1143572. BAY-1143572 is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
Name atuveciclib
Synonyms 4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine
atuveciclib
1,3,5-Triazin-2-amine, 4-(4-fluoro-2-methoxyphenyl)-N-[3-[(S-methylsulfonimidoyl)methyl]phenyl]-
BAY1143572
BAY-1143572 Racemate
Description BAY-1143572 Racemate is the racemate mixture of BAY-1143572. BAY-1143572 is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
Related Catalog
Target

CDK9

In Vitro 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]. 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. 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].
In Vivo 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 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 BAY 1143572 is significantly enhanced in combination with several chemotherapeutics in different solid tumor models[2].
References

[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
Density 1.4±0.1 g/cm3
Boiling Point 589.9±60.0 °C at 760 mmHg
Molecular Formula C18H18FN5O2S
Molecular Weight 387.431
Flash Point 310.6±32.9 °C
Exact Mass 387.116516
LogP 1.03
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.639
Storage condition -20℃

Chemsrc provides CAS#:1414943-88-6 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 1414943-88-6 | Chemsrc address: https://www.chemsrc.com/en/baike/1467557.html

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