BAY-1143572 Racemate
Modify Date: 2024-01-02 16:15:41
BAY-1143572 Racemate structure
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Common Name | BAY-1143572 Racemate | ||
|---|---|---|---|---|
| CAS Number | 1414943-88-6 | Molecular Weight | 387.431 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 589.9±60.0 °C at 760 mmHg | |
| Molecular Formula | C18H18FN5O2S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 310.6±32.9 °C | |
Use of BAY-1143572 RacemateBAY-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 |
|---|---|
| Synonym | More Synonyms |
| 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 | |
| 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 |
| 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℃ |
| 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 |