产品
编 号:F454100
分子式:C19H22O8
分子量:378.37
产品类型
结构图
CAS No: 76958-67-3
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产品详情
生物活性:
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
体内研究:
Hypothemycin (10 mg/kg) kills T. brucei in infected mice, completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects.Animal Model:Adult female Balb/c mice (weighing 18–22 g) infected with T. brucei
Dosage:10 mg/kg
Administration:Administered once daily via intraperitoneal injection for 7 days.
Result:Showed a dose-dependent reduction in parasitemia in infected mice.Prolonged survival of infected mice over 30 days, with a cure rate of 33%.
体外研究:
Hypothemycin inhibits eosinophilic EOL1 cell carrying mutations in FIP1L1-PDGFRα, acute myeloid leukemia MV-4-11 cell carrying mutations in FLT3-ITD, melanoma COLO829 cell carrying mutations in BRAF V600E, HUVEC cell carrying mutations in VEGFR, mastocytoma P815 cell carrying mutations in c-KIT D814Y, NSCLC A459 cell carrying mutations in KRAS, and ovarian SKOV-3 cell carrying mutations in HER2 with IC50s of 0.4 nM, 6 nM, 50 nM, 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively.