A DHODH inhibitor
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BAY-2402234

Item No. 33259

Technical Information
Formal Name
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]-benzamide
CAS Number
2225819-06-5
Synonyms
  • Orludodstat
Molecular Formula
C21H18ClF5N4O4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
O=C1N(C2=CC(O[C@@H](C)C(F)(F)F)=C(C=C2F)C(NC3=C(C=CC=C3F)Cl)=O)N=C(CO)N1CC
InChi Code
InChI=1S/C21H18ClF5N4O4/c1-3-30-17(9-32)29-31(20(30)34)15-8-16(35-10(2)21(25,26)27)11(7-14(15)24)19(33)28-18-12(22)5-4-6-13(18)23/h4-8,10,32H,3,9H2,1-2H3,(H,28,33)/t10-/m0/s1
InChi Key
KNVJMHHAXCPZHF-JTQLQIEISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BAY-2402234 is an inhibitor of dihydroorotate dehydrogenase (DHODH; IC50 = 1.2 nM).1 It induces upregulation of the cell differentiation marker CD11b in MOLM-13 and HEL acute myeloid leukemia (AML) cells (EC50s = 3.16 and 0.96 nM, respectively) and inhibits the proliferation of nine leukemia cell lines (IC50s = 0.08-8.2 nM). BAY-2402234 induces cell cycle arrest at the G2/M phase and apoptosis in TF-1 cells in a concentration-dependent manner. In vivo, BAY-2402234 (1.25, 2.5, and 5 mg/kg) reduces tumor volume in an MV4-11 mouse xenograft model. It also increases survival in patient-derived xenograft (PDX) mouse models of AML.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Christian, S., Merz, C., Evans, L., et alThe novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies. Leukemia 33(10), 2403-2415 (2019).