BAY-2402234
BAY-2402234 Basic information
- Product Name:
- BAY-2402234
- Synonyms:
-
- BAY-2402234
- Benzamide, N-(2-chloro-6-fluorophenyl)-4-[4-ethyl-4,5-dihydro-3-(hydroxymethyl)-5-oxo-1H-1,2,4-triazol-1-yl]-5-fluoro-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]-
- N-(2-chloro-6-fluorophenyl)-4-[4-ethyl-3-(hydroxymethyl)-5-oxo-1,2,4-triazol-1-yl]-5-fluoro-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxybenzamide
- inhibit,BAY 2402234,Inhibitor,DHODH,DNA/RNA Synthesis,BAY2402234,BAY-2402234,Dihydroorotate Dehydrogenase
- (S)-N-(2-Chloro-6-fluorophenyl)-4-(4-ethyl-3-(hydroxymethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)-5-fluoro-2-((1,1,1-trifluoropropan-2-yl)oxy)benzamide
- BAY-2402234, 10 mM in DMSO
- Orludodstat (BAY 2402234)
- Orludodstat (BAY 2402234) ，S8847
- CAS:
- 2225819-06-5
- MF:
- C21H18ClF5N4O4
- MW:
- 520.84
- Mol File:
- 2225819-06-5.mol
BAY-2402234 Chemical Properties
- Density
- 1.52±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Store in freezer, under -20°C
- solubility
- DMF:10.0(Max Conc. mg/mL);19.2(Max Conc. mM)
DMSO:78.33(Max Conc. mg/mL);150.39(Max Conc. mM)
Ethanol:31.5(Max Conc. mg/mL);60.48(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.48(Max Conc. mM) - form
- A crystalline solid
- pka
- 10.57±0.70(Predicted)
- color
- White to light yellow
- InChIKey
- KNVJMHHAXCPZHF-JTQLQIEISA-N
- SMILES
- C(NC1=C(F)C=CC=C1Cl)(=O)C1=CC(F)=C(N2C(=O)N(CC)C(CO)=N2)C=C1O[C@@H](C)C(F)(F)F
BAY-2402234 Usage And Synthesis
Uses
BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
in vivo
BAY-2402234 exhibits strong in vivo anti-tumor efficacy in monotherapy in several subcutaneous and disseminated AML xenografts as well as AML patient-derived xenograft (PDX) models. Target engagement of the novel DHODH inhibitor BAY-2402234 can be observed by increase of tumoral and plasma dihydroorotate levels after treatment with the inhibitor. Consistent with the in vitro data BAY-2402234 induces AML differentiation in vivo as detected by upregulation of differentiation cell surface markers in xenograft and PDX models after treatment with the inhibitor. Furthermore, differentiation-associated transcriptomic changes are evident following a single administration of BAY-2402234 in vivo[1].
References
[1] Andreas Janzer, et al. Abstract DDT02-04: BAY 2402234: A novel, selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies. AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL.
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