| CAS NO: | 1414943-88-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| Molecular Weight (MW) | 387.43 |
|---|---|
| Formula | C18H18FN5O2S |
| CAS No. | N/A |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO:>80 mg/mL |
| Water: <1mg/mL | |
| Ethanol:<1mg/mL | |
| Chemical Name | (3-((4-(4-fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)benzyl)(imino)(methyl)-l6-sulfanone |
| Synonyms | BAY1143572; BAY 1143572; BAY-1143572 |
| In Vitro | In vitro activity: Atuveciclib (formerly known as BAY-1143572) is novel, potent, oral and highly selective PTEFb/CDK9 inhibitor. It inhibits CDK9/CycT1 with an IC50 of 13 nM and is more than 100-fold more selective for CDK9 over CDK2. It also inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively. Atuveciclib is currently in Phase I clinical trial. Kinase Assay: Atuveciclib (formerly known as BAY-1143572) is novel, potent, oral and highly selective PTEFb/CDK9 inhibitor. It inhibits CDK9/CycT1 with an IC50 of 13 nM and is more than 100-fold more selective for CDK9 over CDK2. It also inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively. Cell Assay: BAY 1143572 demonstrates antiproliferative activity against HeLa cells (IC50 = 920 nM) and MOLM-13 cells (IC50 = 310 nM). It also demonstrates improved Caco-2 permeability and a decreased efflux ratio (PappA→B: 35 nm/s, ER: 6) relative to lead compound BAY‐958 (PappA→B: 22 nm/s, ER: 15). |
|---|---|
| In Vivo | In an in vivo pharmacokinetic study in rats, BAY 1143572 showed low blood clearance (CLb 1.1 L/h/kg). The volumes of distribution (V ss) of BAY 1143572 is 1.0 L/kg. BAY 1143572 shows significantly improved oral bioavailability of 54 %. The blood/plasma ratios is about 1. It does not show significant inhibition of cytochrome P450 activity, with IC50 values>20 μM. The administration of BAY 1143572 in immunocompromized NOD/Shi-scid/IL-2Rγ null (NOG) mice xenografted with patient-derived ATL cells greatly reduced the infiltration of ATL cells into organs, such as liver and bone marrow. Decreased human soluble IL2R levels in serum were also observed, which indicated a reduction of ATL tumor burden. |
| Animal model | Immunocompromized NOD/Shi-scid/IL-2Rγ null (NOG) mice xenografted with patient-derived ATL cells and in vivo pharmacokinetic in rats |
| Formulation & Dosage | NA |
| References | ChemMedChem. 2017 Nov 8;12(21):1776-1793.; Molecules. 2018, 23(5). pii: E1057. |
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