产品
编 号：F015598
分子式：C19H14F2N2O3
分子量：356.32
分子式：C19H14F2N2O3
分子量：356.32
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
200
In-stock
5mg
400
In-stock
10mg
640
In-stock
25mg
1280
In-stock
50mg
2080
In-stock
100mg
3280
In-stock
结构图
CAS No: 1035688-66-4
产品详情
生物活性：
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.
体内研究：
Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival. Animal Model:Female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells
Dosage:50 mg/kg
Administration:Oral gavage; once daily; from the day 3 to 30
Result:Substantially reduced the number of disseminated tumors and the size of these tumors. Survival was significantly prolonged.
体外研究：
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. Farudodstat (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8. Farudodstat (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples. 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.
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.
体内研究：
Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival. Animal Model:Female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells
Dosage:50 mg/kg
Administration:Oral gavage; once daily; from the day 3 to 30
Result:Substantially reduced the number of disseminated tumors and the size of these tumors. Survival was significantly prolonged.
体外研究：
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. Farudodstat (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8. Farudodstat (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples. 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备