BAY-1251152
BAY-1251152 Basic information
- Product Name:
- BAY-1251152
- Synonyms:
-
- BAY-1251152
- BAY 1251152 ((+)-BAY 1251152 )
- (rac)-5-fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine
- (+)-BAY-1251152
- (+)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-[4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl]pyridin-2-amine
- (+)-Enitociclib
- (+)Enitociclib,(+) Enitociclib
- (+)-5-fluoro-4-(4-fluoro-2-methoxy-phenyl)-N-[4-[(methylsulfonimidoyl)methyl]-2-pyridyl]pyridin-2-amine
- CAS:
- 1610358-56-9
- MF:
- C19H18F2N4O2S
- MW:
- 404.43
- Mol File:
- 1610358-56-9.mol
BAY-1251152 Chemical Properties
- Boiling point:
- 494.2±55.0 °C(Predicted)
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:97.15(Max Conc. mg/mL);240.21(Max Conc. mM)
- form
- Solid
- color
- Off-white to yellow
BAY-1251152 Usage And Synthesis
Uses
(+)-Enitociclib ((+)-BAY-1251152) is an enanthiomer of BAY-1251152 with rotation (+). Enitociclib is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. Enitociclib has anti-tumour activity[1][2].
in vivo
(+)-Enitociclib (Compound A’; 10 mg/kg; intravenous injection; once every seven days; for 14 days; female SCID mice) reaches a Treatment to Control ratios (T/C) by area of 0.29 and a T/C by weight of 0.24. Enitociclib inhibits tumour growth and had good tolerability[2].
| Animal Model: | Female SCID mice with OCI-LY-3 cells[2] |
| Dosage: | 10 mg/kg |
| Administration: | Intravenous injection; once every seven days; for 14 days |
| Result: | Inhibited tumour growth and had good tolerability. |
IC 50
CDK9/CycT1: 3 nM (IC50)
References
[1] Ulrich LüCKING, et al. 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group. WO2014076091A1.
[2] Use of Arne Scholz, et al. 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma. WO2019158517A1.
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