| Bioactivity | Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice[1][2]. | ||||||||||||
| Invitro | Farudodstat (0.01-100 μM; for 48 hours) inhibits leukemic cell proliferation. The cell viability is maintained at ~50% at Farudodstat 1 μM and higher[1]. Farudodstat (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8[1]. Farudodstat (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples[1]. Farudodstat (1, 2 μM; pretreatment 1 h before OPP for 1 h) inhibits protein synthesis, as demonstrated by the reduced incorporation of O-propargyl-puromycin (OPP) at protein translation sites in both MOLM-14 and KG-1 cells. Farudodstat causes the downregulation of EIF4B, and RPL6 proteins[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| Name | Farudodstat | ||||||||||||
| CAS | 1035688-66-4 | ||||||||||||
| Formula | C19H14F2N2O3 | ||||||||||||
| Molar Mass | 356.32 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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Farudodstat
CAS: 1035688-66-4 F: C19H14F2N2O3 W: 356.32
Farudodstat (ASLAN003) is an orally active and potentDihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 n
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