Introduction：Basic information about CAS 1414943-88-6|BAY-1143572 Racemate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | BAY-1143572 Racemate |
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| CAS Number | 1414943-88-6 | Molecular Weight | 387.431 |
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| Density | 1.4±0.1 g/cm3 | Boiling Point | 589.9±60.0 °C at 760 mmHg |
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| Molecular Formula | C18H18FN5O2S | Melting Point | / |
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| MSDS | / | Flash Point | 310.6±32.9 °C |
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Names
| Name | atuveciclib |
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| Synonym | More Synonyms |
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BAY-1143572 Racemate BiologicalActivity
| 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. |
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| Related Catalog | Signaling Pathways >>Cell Cycle/DNA Damage >>CDKResearch Areas >>Cancer |
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| Target | CDK9 |
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| 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]. |
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| 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]. |
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| 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 |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Boiling Point | 589.9±60.0 °C at 760 mmHg |
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| Molecular Formula | C18H18FN5O2S |
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| Molecular Weight | 387.431 |
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| Flash Point | 310.6±32.9 °C |
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| Exact Mass | 387.116516 |
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| LogP | 1.03 |
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| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
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| Index of Refraction | 1.639 |
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| Storage condition | -20℃ |
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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 |
